Most-cited articles · 2022

The 100 most-cited articles in Molecules, 2022

Ranked by OpenAlex citation count on 29 October 2026, out of 9,060 eligible articles Molecules published in 2022. Ranks are frozen; this page will not change. Number one, with 1,480 citations: Determination of Antioxidants by DPPH Radical Scavenging Activity and Quantitative Phytochemical Analysis of Ficus religiosa.

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2026-10-29

The most-cited articles from Molecules in 2022 are dominated by reviews of natural products and their biological activities, drug delivery systems, and plant-derived compounds with therapeutic potential. The top paper, on determining antioxidants in Ficus religiosa by DPPH radical scavenging activity and quantitative phytochemical analysis, has 1480 citations. Other highly cited works address liposomes as drug delivery systems, hydrogels in biomedicine, and flavonoids as anti-inflammatory molecules.

Readers can use this list to identify the topics and specific papers that attracted the most citations among the 9060 eligible articles published in the journal that year. The ranking reflects citation counts recorded by OpenAlex and covers themes including natural product discovery, pharmaceutical development, and food science.

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    Determination of Antioxidants by DPPH Radical Scavenging Activity and Quantitative Phytochemical Analysis of Ficus religiosa

    Siddartha Baliyan, Riya Mukherjee, Anjali Priyadarshini, Arpana Vibhuti, Archana Anshuman Gupta and 2 more

    1,480 citationsOpen access (CC-BY)doi:10.3390/molecules27041326OpenAlex

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    The use of F. religiosa might be beneficial in inflammatory illnesses and can be used for a variety of health conditions. In this article, we studied the identification of antioxidants using (DPPH) 2,2-Diphenyl-1-picrylhydrazylradical scavenging activity in Ficus religiosa, as F. religiosa is an important herbal plant, and every part of it has various medicinal properties such as antibacterial properties that can be used by the researchers in the development and design of various new drugs. The 2,2-Diphenyl-1-picrylhydrazyl (DPPH) is a popular, quick, easy, and affordable approach for the measurement of antioxidant properties that includes the use of the free radicals used for assessing the potential of substances to serve as hydrogen providers or free-radical scavengers (FRS). The technique of DPPH testing is associated with the elimination of DPPH, which would be a stabilized free radical. The free-radical DPPH interacts with an odd electron to yield a strong absorbance at 517 nm, i.e., a purple hue. An FRS antioxidant, for example, reacts to DPPH to form DPPHH, which has a lower…

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    A Review of Liposomes as a Drug Delivery System: Current Status of Approved Products, Regulatory Environments, and Future Perspectives

    Peng Liu, Guiliang Chen, Jingchen Zhang

    1,332 citationsOpen access (CC-BY)doi:10.3390/molecules27041372OpenAlex

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    Liposomes have been considered promising and versatile drug vesicles. Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. Given these merits, several liposomal drug products have been successfully approved and used in clinics over the last couple of decades. In this review, the liposomal drug products approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) are discussed. Based on the published approval package in the FDA and European public assessment report (EPAR) in EMA, the critical chemistry information and mature pharmaceutical technologies applied in the marketed liposomal products, including the lipid excipient, manufacturing methods, nanosizing technique, drug loading methods, as well as critical quality attributions (CQAs) of products, are introduced. Additionally, the current regulatory guidance and future perspectives related to…

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    Hydrogels: Properties and Applications in Biomedicine

    Tzu‐Chuan Ho, Chin-Chuan Chang, Hung-Pin Chan, Tze‐Wen Chung, Chih‐Wen Shu and 4 more

    1,107 citationsOpen access (CC-BY)doi:10.3390/molecules27092902OpenAlex

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    Hydrogels are crosslinked polymer chains with three-dimensional (3D) network structures, which can absorb relatively large amounts of fluid. Because of the high water content, soft structure, and porosity of hydrogels, they closely resemble living tissues. Research in recent years shows that hydrogels have been applied in various fields, such as agriculture, biomaterials, the food industry, drug delivery, tissue engineering, and regenerative medicine. Along with the underlying technology improvements of hydrogel development, hydrogels can be expected to be applied in more fields. Although not all hydrogels have good biodegradability and biocompatibility, such as synthetic hydrogels (polyvinyl alcohol, polyacrylamide, polyethylene glycol hydrogels, etc.), their biodegradability and biocompatibility can be adjusted by modification of their functional group or incorporation of natural polymers. Hence, scientists are still interested in the biomedical applications of hydrogels due to their creative adjustability for different uses. In this review, we first introduce the basic…

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    Flavonoids as Potential Anti-Inflammatory Molecules: A Review

    Jameel Mohammed Al-Khayri, Gandasi Ravikumar Sahana, Praveen Nagella, Biljo V. Joseph, Fatima Mohammed Alessa and 1 more

    1,097 citationsOpen access (CC-BY)doi:10.3390/molecules27092901OpenAlex

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    Hydroxylated polyphenols, also called flavonoids, are richly present in vegetables, fruits, cereals, nuts, herbs, seeds, stems, and flowers of numerous plants. They possess numerous medicinal properties such as antioxidant, anti-cancer, anti-microbial, neuroprotective, and anti-inflammation. Studies show that flavonoids activate antioxidant pathways that render an anti-inflammatory effect. They inhibit the secretions of enzymes such as lysozymes and β-glucuronidase and inhibit the secretion of arachidonic acid, which reduces inflammatory reactions. Flavonoids such as quercetin, genistein, apigenin, kaempferol, and epigallocatechin 3-gallate modulate the expression and activation of a cytokine such as interleukin-1beta (IL-1β), Tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), and interleukin-8 (IL-8); regulate the gene expression of many pro-inflammatory molecules such s nuclear factor kappa-light chain enhancer of activated B cells (NF-κB), activator protein-1 (AP-1), intercellular adhesion molecule-1 (ICAM), vascular cell adhesion molecule-1 (VCAM), and E-selectins; and…

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    Role of Cholinergic Signaling in Alzheimer’s Disease

    Zhi-ru Chen, Jiabao Huang, Shu‐Long Yang, Fen‐Fang Hong

    917 citationsOpen access (CC-BY)doi:10.3390/molecules27061816OpenAlex

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    Acetylcholine, a neurotransmitter secreted by cholinergic neurons, is involved in signal transduction related to memory and learning ability. Alzheimer's disease (AD), a progressive and commonly diagnosed neurodegenerative disease, is characterized by memory and cognitive decline and behavioral disorders. The pathogenesis of AD is complex and remains unclear, being affected by various factors. The cholinergic hypothesis is the earliest theory about the pathogenesis of AD. Cholinergic atrophy and cognitive decline are accelerated in age-related neurodegenerative diseases such as AD. In addition, abnormal central cholinergic changes can also induce abnormal phosphorylation of ttau protein, nerve cell inflammation, cell apoptosis, and other pathological phenomena, but the exact mechanism of action is still unclear. Due to the complex and unclear pathogenesis, effective methods to prevent and treat AD are unavailable, and research to explore novel therapeutic drugs is various and active in the world. This review summaries the role of cholinergic signaling and the correlation between the…

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    Prostate Cancer Review: Genetics, Diagnosis, Treatment Options, and Alternative Approaches

    Mamello Patience Sekhoacha, Keamogetswe Riet, Paballo Motloung, Lemohang Gumenku, Ayodeji Mathias Adegoke and 1 more

    914 citationsOpen access (CC-BY)doi:10.3390/molecules27175730OpenAlex

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    Prostate cancer is one of the malignancies that affects men and significantly contributes to increased mortality rates in men globally. Patients affected with prostate cancer present with either a localized or advanced disease. In this review, we aim to provide a holistic overview of prostate cancer, including the diagnosis of the disease, mutations leading to the onset and progression of the disease, and treatment options. Prostate cancer diagnoses include a digital rectal examination, prostate-specific antigen analysis, and prostate biopsies. Mutations in certain genes are linked to the onset, progression, and metastasis of the cancer. Treatment for localized prostate cancer encompasses active surveillance, ablative radiotherapy, and radical prostatectomy. Men who relapse or present metastatic prostate cancer receive androgen deprivation therapy (ADT), salvage radiotherapy, and chemotherapy. Currently, available treatment options are more effective when used as combination therapy; however, despite available treatment options, prostate cancer remains to be incurable. There has…

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    Role of Lipids in Food Flavor Generation

    Fereidoon Shahidi, Abul Hossain

    685 citationsOpen access (CC-BY)doi:10.3390/molecules27155014OpenAlex

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    Lipids in food are a source of essential fatty acids and also play a crucial role in flavor and off-flavor development. Lipids contribute to food flavor generation due to their degradation to volatile compounds during food processing, heating/cooking, and storage and/or interactions with other constituents developed from the Maillard reaction and Strecker degradation, among others. The degradation of lipids mainly occurs via autoxidation, photooxidation, and enzymatic oxidation, which produce a myriad of volatile compounds. The oxidation of unsaturated fatty acids generates hydroperoxides that then further break down to odor-active volatile secondary lipid oxidation products including aldehydes, alcohols, and ketones. In this contribution, a summary of the most relevant and recent findings on the production of volatile compounds from lipid degradation and Maillard reactions and their interaction has been compiled and discussed. In particular, the effects of processing such as cooking, drying, and fermentation as well as the storage of lipid-based foods on flavor generation are…

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    Natural Products as Anticancer Agents: Current Status and Future Perspectives

    Abid Naeem, Pengyi Hu, Ming Yu Yang, Jing Zhang, Yali Liu and 2 more

    616 citationsOpen access (CC-BY)doi:10.3390/molecules27238367OpenAlex

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    Natural products have been an invaluable and useful source of anticancer agents over the years. Several compounds have been synthesized from natural products by modifying their structures or by using naturally occurring compounds as building blocks in the synthesis of these compounds for various purposes in different fields, such as biology, medicine, and engineering. Multiple modern and costly treatments have been applied to combat cancer and limit its lethality, but the results are not significantly refreshing. Natural products, which are a significant source of new therapeutic drugs, are currently being investigated as potential cytotoxic agents and have shown a positive trend in preclinical research and have prompted numerous innovative strategies in order to combat cancer and expedite the clinical research. Natural products are becoming increasingly important for drug discovery due to their high molecular diversity and novel biofunctionality. Furthermore, natural products can provide superior efficacy and safety due to their unique molecular properties. The objective of the…

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    Modern Approaches in the Discovery and Development of Plant-Based Natural Products and Their Analogues as Potential Therapeutic Agents

    Asim Najmi, Sadique Akhtar Javed, Mohammed Al Bratty, Hassan A. Alhazmi

    603 citationsOpen access (CC-BY)doi:10.3390/molecules27020349OpenAlex

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    Natural products represents an important source of new lead compounds in drug discovery research. Several drugs currently used as therapeutic agents have been developed from natural sources; plant sources are specifically important. In the past few decades, pharmaceutical companies demonstrated insignificant attention towards natural product drug discovery, mainly due to its intrinsic complexity. Recently, technological advancements greatly helped to address the challenges and resulted in the revived scientific interest in drug discovery from natural sources. This review provides a comprehensive overview of various approaches used in the selection, authentication, extraction/isolation, biological screening, and analogue development through the application of modern drug-development principles of plant-based natural products. Main focus is given to the bioactivity-guided fractionation approach along with associated challenges and major advancements. A brief outline of historical development in natural product drug discovery and a snapshot of the prominent natural drugs developed in…

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    Antimicrobial Activity of Quercetin: An Approach to Its Mechanistic Principle

    Thi Lan Anh Nguyen, Debanjana Bhattacharya

    553 citationsOpen access (CC-BY)doi:10.3390/molecules27082494OpenAlex

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    Quercetin, an essential plant flavonoid, possesses a variety of pharmacological activities. Extensive literature investigates its antimicrobial activity and possible mechanism of action. Quercetin has been shown to inhibit the growth of different Gram-positive and Gram-negative bacteria as well as fungi and viruses. The mechanism of its antimicrobial action includes cell membrane damage, change of membrane permeability, inhibition of synthesis of nucleic acids and proteins, reduction of expression of virulence factors, mitochondrial dysfunction, and preventing biofilm formation. Quercetin has also been shown to inhibit the growth of various drug-resistant microorganisms, thereby suggesting its use as a potent antimicrobial agent against drug-resistant strains. Furthermore, certain structural modifications of quercetin have sometimes been shown to enhance its antimicrobial activity compared to that of the parent molecule. In this review, we have summarized the antimicrobial activity of quercetin with a special focus on its mechanistic principle. Therefore, this review will provide…

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    Antibacterial Effects of Flavonoids and Their Structure-Activity Relationship Study: A Comparative Interpretation

    Nur Farisya Shamsudin, Qamar Uddin Ahmed, Syed Mahmood, Syed Adnan Alı Shah, Alfi Khatib and 4 more

    516 citationsOpen access (CC-BY)doi:10.3390/molecules27041149OpenAlex

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    According to the latest report released by the World Health Organization, bacterial resistance to well-known and widely available antibacterial drugs has become a significant and severe global health concern and a grim challenge to tackle in order to cure infections associated with multidrug-resistant pathogenic microorganisms efficiently. Consequently, various strategies have been orchestrated to cure the severe complications related to multidrug-resistant bacteria effectively. Some approaches involved the retardation of biofilm formation and multidrug-resistance pumps in bacteria as well as the discovery of new antimicrobial agents demonstrating different mechanisms of action. In this regard, natural products namely alkaloids, terpenoids, steroids, anthraquinone, flavonoids, saponins, tannins, etc., have been suggested to tackle the multidrug-resistant bacterial strains owing to their versatile pharmacological effects. Amongst these, flavonoids, also known as polyphenolic compounds, have been widely evaluated for their antibacterial property due to their tendency to retard the…

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    Plant Secondary Metabolites Produced in Response to Abiotic Stresses Has Potential Application in Pharmaceutical Product Development

    Karma Yeshi, Darren M. Crayn, Edita Ritmejerytė, Phurpa Wangchuk

    488 citationsOpen access (CC-BY)doi:10.3390/molecules27010313OpenAlex

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    Plant secondary metabolites (PSMs) are vital for human health and constitute the skeletal framework of many pharmaceutical drugs. Indeed, more than 25% of the existing drugs belong to PSMs. One of the continuing challenges for drug discovery and pharmaceutical industries is gaining access to natural products, including medicinal plants. This bottleneck is heightened for endangered species prohibited for large sample collection, even if they show biological hits. While cultivating the pharmaceutically interesting plant species may be a solution, it is not always possible to grow the organism outside its natural habitat. Plants affected by abiotic stress present a potential alternative source for drug discovery. In order to overcome abiotic environmental stressors, plants may mount a defense response by producing a diversity of PSMs to avoid cells and tissue damage. Plants either synthesize new chemicals or increase the concentration (in most instances) of existing chemicals, including the prominent bioactive lead compounds morphine, camptothecin, catharanthine, epicatechin-3-gallate…

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    Multidrug Resistance (MDR): A Widespread Phenomenon in Pharmacological Therapies

    Alessia Anna Catalano, Domenico Iacopetta, Jessica Ceramella, Domenica Scumaci, Federica Giuzio and 4 more

    475 citationsOpen access (CC-BY)doi:10.3390/molecules27030616OpenAlex

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    Multidrug resistance is a leading concern in public health. It describes a complex phenotype whose predominant feature is resistance to a wide range of structurally unrelated cytotoxic compounds, many of which are anticancer agents. Multidrug resistance may be also related to antimicrobial drugs, and is known to be one of the most serious global public health threats of this century. Indeed, this phenomenon has increased both mortality and morbidity as a consequence of treatment failures and its incidence in healthcare costs. The large amounts of antibiotics used in human therapies, as well as for farm animals and even for fishes in aquaculture, resulted in the selection of pathogenic bacteria resistant to multiple drugs. It is not negligible that the ongoing COVID-19 pandemic may further contribute to antimicrobial resistance. In this paper, multidrug resistance and antimicrobial resistance are underlined, focusing on the therapeutic options to overcome these obstacles in drug treatments. Lastly, some recent studies on nanodrug delivery systems have been reviewed since they may…

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    Health Benefits of Quercetin in Age-Related Diseases

    Deepika, Pawan Kumar Maurya

    449 citationsOpen access (CC-BY)doi:10.3390/molecules27082498OpenAlex

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    Polyphenols are the known group of phytochemicals that essentially consists of phenolic rings. These are the plant product present in varied fruits and vegetables. These secondary metabolites perform a protective function in plants from environmental and biological stress. When consumed as a human diet these are also known to prevent various age-associated diseases. Polyphenols are known to possess antioxidant properties and protect against oxidative stress. The literature survey was carried out using databases such as PubMed, Science direct and Springer. The research articles from last 10-12 years were selected for this review based on its relevancy with the topic. The articles selected was mainly focused on quercetin and its health benefits. The present review highlights the main functions of a flavonoid, quercetin. Quercetin is among the widely occurring polyphenol, found abundantly in nature. It is commonly present in different plant products. Onion is known to have the highest quantity of quercetin. This plant compound is possessed antioxidant properties and is considered to…

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    Lipopolysaccharide-Induced Model of Neuroinflammation: Mechanisms of Action, Research Application and Future Directions for Its Use

    Anna Skrzypczak-Wiercioch, Kinga Sałat

    400 citationsOpen access (CC-BY)doi:10.3390/molecules27175481OpenAlex

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    Despite advances in antimicrobial and anti-inflammatory therapies, inflammation and its consequences still remain a significant problem in medicine. Acute inflammatory responses are responsible for directly life-threating conditions such as septic shock; on the other hand, chronic inflammation can cause degeneration of body tissues leading to severe impairment of their function. Neuroinflammation is defined as an inflammatory response in the central nervous system involving microglia, astrocytes, and cytokines including chemokines. It is considered an important cause of neurodegerative diseases, such as Alzheimer's disease, Parkinson's disease and amyotrophic lateral sclerosis. Lipopolysaccharide (LPS) is a strong immunogenic particle present in the outer membrane of Gram-negative bacteria. It is a major triggering factor for the inflammatory cascade in response to a Gram-negative bacteria infection. The use of LPS as a strong pro-inflammatory agent is a well-known model of inflammation applied in both in vivo and in vitro studies. This review offers a summary of the pathogenesis…

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    Different Schiff Bases—Structure, Importance and Classification

    Edyta Raczuk, Barbara Dmochowska, Justyna Samaszko-Fiertek, Janusz Madaj

    399 citationsOpen access (CC-BY)doi:10.3390/molecules27030787OpenAlex

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    Schiff bases are a vast group of compounds characterized by the presence of a double bond linking carbon and nitrogen atoms, the versatility of which is generated in the many ways to combine a variety of alkyl or aryl substituents. Compounds of this type are both found in nature and synthesized in the laboratory. For years, Schiff bases have been greatly inspiring to many chemists and biochemists. In this article, we attempt to present a new take on this group of compounds, underlining of the importance of various types of Schiff bases. Among the different types of compounds that can be classified as Schiff bases, we chose hydrazides, dihydrazides, hydrazones and mixed derivatives such as hydrazide-hydrazones. For these compounds, we presented the elements of their structure that allow them to be classified as Schiff bases. While hydrazones are typical examples of Schiff bases, including hydrazides among them may be surprising for some. In their case, this is possible due to the amide-iminol tautomerism. The carbon-nitrogen double bond present in the iminol tautomer is a typical…

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    The Current Situation of Pea Protein and Its Application in the Food Industry

    Parvathy Shanthakumar, Joanna Klepacka, Aarti Bains, Prince Chawla, Sanju Bala Dhull and 1 more

    386 citationsOpen access (CC-BY)doi:10.3390/molecules27165354OpenAlex

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    ) is an important source of nutritional components and is rich in protein, starch, and fiber. Pea protein is considered a high-quality protein and a functional ingredient in the global industry due to its low allergenicity, high protein content, availability, affordability, and deriving from a sustainable crop. Moreover, pea protein has excellent functional properties such as solubility, water, and oil holding capacity, emulsion ability, gelation, and viscosity. Therefore, these functional properties make pea protein a promising ingredient in the food industry. Furthermore, several extraction techniques are used to obtain pea protein isolate and concentrate, including dry fractionation, wet fractionation, salt extraction, and mild fractionation methods. Dry fractionation is chemical-free, has no loss of native functionality, no water use, and is cost-effective, but the protein purity is comparatively low compared to wet extraction. Pea protein can be used as a food emulsifier, encapsulating material, a biodegradable natural polymer, and also in cereals, bakery, dairy, and meat…

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    Quercetin: Its Antioxidant Mechanism, Antibacterial Properties and Potential Application in Prevention and Control of Toxipathy

    Weidong Qi, Wanxiang Qi, Dongwei Xiong, Miao Long

    373 citationsOpen access (CC-BY)doi:10.3390/molecules27196545OpenAlex

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    Quercetin, as a flavonol compound found in plants, has a variety of biological activities. It is widely present in nature and the human diet, with powerful oxidative properties and biological activities. In this review, the antioxidant mechanism and broad-spectrum antibacterial properties of quercetin are revealed; the intervention effects of quercetin on pesticide poisoning and the pathway of action are investigated; the toxic effects of main mycotoxins on the collection and the detoxification process of quercetin are summarized; whether it is able to reduce the toxicity of mycotoxins is proved; and the harmful effects of heavy metal poisoning on the collection, the prevention, and control of quercetin are evaluated. This review is expected to enrich the understanding of the properties of quercetin and promote its better application in clinical practice.

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    Revisiting the Physicochemical Properties and Applications of Deep Eutectic Solvents

    Sushma P. Ijardar, Vickramjeet Singh, Ramesh L. Gardas

    373 citationsOpen access (CC-BY)doi:10.3390/molecules27041368OpenAlex

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    Recently, deep eutectic solvent (DES) or ionic liquid (IL) analogues have been considered as the newest green solvent, demonstrating the potential to replace harsh volatile organic solvents. DESs are mainly a combination of two compounds: hydrogen bond acceptor (HBA) and hydrogen bond donor (HBD), which have the ability to interact through extensive hydrogen bonds. A thorough understanding of their physicochemical properties is essential, given their successful applications on an industrial scale. The appropriate blend of HBA to HBD can easily fine-tune DES properties for desired applications. In this context, we have reviewed the basic information related to DESs, the two most studied physicochemical properties (density and viscosity), and their performance as a solvent in (i) drug delivery and (ii) extraction of biomolecules. A broader approach of various factors affecting their performance has been considered, giving a detailed picture of the current status of DESs in research and development.

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    Role of Phenylpropanoids and Flavonoids in Plant Resistance to Pests and Diseases

    Marie‐Louisa Ramaroson, Claude Emmanuel Koutouan, Jean‐Jacques Hélesbeux, V. Le Clerc, Latifa Hamama and 2 more

    361 citationsOpen access (CC-BY)doi:10.3390/molecules27238371OpenAlex

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    Phenylpropanoids and flavonoids are specialized metabolites frequently reported as involved in plant defense to biotic or abiotic stresses. Their biosynthetic accumulation may be constitutive and/or induced in response to external stimuli. They may participate in plant signaling driving plant defense responses, act as a physical or chemical barrier to prevent invasion, or as a direct toxic weapon against microbial or insect targets. Their protective action is described as the combinatory effect of their localization during the host's interaction with aggressors, their sustained availability, and the predominance of specific compounds or synergy with others. Their biosynthesis and regulation are partly deciphered; however, a lot of gaps in knowledge remain to be filled. Their mode of action on microorganisms and insects probably arises from an interference with important cellular machineries and structures, yet this is not fully understood for all type of pests and pathogens. We present here an overview of advances in the state of the art for both phenylpropanoids and flavonoids with…

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    Bioethanol Production from Lignocellulosic Biomass—Challenges and Solutions

    Magdalena Broda, Daniel J. Yelle, Katarzyna Serwańska

    359 citationsOpen access (CC-BY)doi:10.3390/molecules27248717OpenAlex

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    Regarding the limited resources for fossil fuels and increasing global energy demands, greenhouse gas emissions, and climate change, there is a need to find alternative energy sources that are sustainable, environmentally friendly, renewable, and economically viable. In the last several decades, interest in second-generation bioethanol production from non-food lignocellulosic biomass in the form of organic residues rapidly increased because of its abundance, renewability, and low cost. Bioethanol production fits into the strategy of a circular economy and zero waste plans, and using ethanol as an alternative fuel gives the world economy a chance to become independent of the petrochemical industry, providing energy security and environmental safety. However, the conversion of biomass into ethanol is a challenging and multi-stage process because of the variation in the biochemical composition of biomass and the recalcitrance of lignin, the aromatic component of lignocellulose. Therefore, the commercial production of cellulosic ethanol has not yet become well-received commercially,…

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    Green Tea (Camellia sinensis): A Review of Its Phytochemistry, Pharmacology, and Toxicology

    Tiantian Zhao, Chao Li, Shuai Wang, Xinqiang Song

    350 citationsOpen access (CC-BY)doi:10.3390/molecules27123909OpenAlex

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    ) is a kind of unfermented tea that retains the natural substance in fresh leaves to a great extent. It is regarded as the second most popular drink in the world besides water. In this paper, the phytochemistry, pharmacology, and toxicology of green tea are reviewed systematically and comprehensively. Key findings Green tea has been demonstrated to be good for human health. Nowadays, multiple pharmacologically active components have been isolated and identified from green tea, including tea polyphenols, alkaloids, amino acids, polysaccharides, and volatile components. Recent studies have demonstrated that green tea shows versatile pharmacological activities, such as antioxidant, anticancer, hypoglycemic, antibacterial, antiviral, and neuroprotective. Studies on the toxic effects of green tea extract and its main ingredients have also raised concerns including hepatotoxicity and DNA damage. Summary Green tea can be used to assist the treatment of diabetes, Alzheimer's disease, oral cancer, and dermatitis. Consequently, green tea has shown promising practical prospects in health care…

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    General Health Benefits and Pharmacological Activities of Triticum aestivum L.

    Said Moshawih, Rabi’atul Nur Amalia Abdullah Juperi, Ganesh Sritheran Paneerselvam, Long Chiau Ming, Kai Bin Liew and 6 more

    345 citationsOpen access (CC-BY)doi:10.3390/molecules27061948OpenAlex

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    Common wheat (Triticum aestivum), one of the world’s most consumed cereal grains, is known for its uses in baking and cooking in addition to its medicinal uses. As this plant’s medical benefits are enormous and scattered, this narrative review was aimed at describing the pharmacological activities, phytochemistry, and the nutritional values of Triticum aestivum. It is a good source of dietary fiber, resistant starch, phenolic acids, alkylresorcinols, lignans, and diverse antioxidant compounds such as carotenoids, tocopherols and tocotrienols. These constituents provide Triticum aestivum with a wide range of pharmacological properties, including anticancer, antimicrobial, antidiabetic, hypolipemic, antioxidant, laxative, and moisturizing effects. This review summarized the established benefits of wheat in human health, the mode of action, and different clinical, in vitro and in vivo studies for different varieties and cultivars. This review also gives an insight for future research into the better use of this plant as a functional food. More clinical trials, in vivo and in vitro…

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    Mechanistic Insight into Oxidative Stress-Triggered Signaling Pathways and Type 2 Diabetes

    Anju Singh, Ritushree Kukreti, Luciano Saso, Shrikant Kukreti

    330 citationsOpen access (CC-BY)doi:10.3390/molecules27030950OpenAlex

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    Oxidative stress (OS) is a metabolic dysfunction mediated by the imbalance between the biochemical processes leading to elevated production of reactive oxygen species (ROS) and the antioxidant defense system of the body. It has a ubiquitous role in the development of numerous noncommunicable maladies including cardiovascular diseases, cancers, neurodegenerative diseases, aging and respiratory diseases. Diseases associated with metabolic dysfunction may be influenced by changes in the redox balance. Lately, there has been increasing awareness and evidence that diabetes mellitus (DM), particularly type 2 diabetes, is significantly modulated by oxidative stress. DM is a state of impaired metabolism characterized by hyperglycemia, resulting from defects in insulin secretion or action, or both. ROS such as hydrogen peroxide and the superoxide anion introduce chemical changes virtually in all cellular components, causing deleterious effects on the islets of β-cells, in turn affecting insulin production. Under hyperglycemic conditions, various signaling pathways such as nuclear factor-κβ…

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    Applications of Essential Oils and Plant Extracts in Different Industries

    Parisa Bolouri, Robab Salami, Shaghayegh Kouhi, Masoumeh Kordi, Behnam Asgari Lajayer and 2 more

    329 citationsOpen access (CC-BY)doi:10.3390/molecules27248999OpenAlex

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    Essential oils (EOs) and plant extracts are sources of beneficial chemical compounds that have potential applications in medicine, food, cosmetics, and the agriculture industry. Plant medicines were the only option for preventing and treating mankind's diseases for centuries. Therefore, plant products are fundamental sources for producing natural drugs. The extraction of the EOs is the first important step in preparing these compounds. Modern extraction methods are effective in the efficient development of these compounds. Moreover, the compounds extracted from plants have natural antimicrobial activity against many spoilage and disease-causing bacteria. Also, the use of plant compounds in cosmetics and hygiene products, in addition to their high marketability, has been helpful for many beauty problems. On the other hand, the agricultural industry has recently shifted more from conventional production systems to authenticated organic production systems, as consumers prefer products without any pesticide and herbicide residues, and certified organic products command higher prices.…

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    Electrochemical Impedance Spectroscopy in the Characterisation and Application of Modified Electrodes for Electrochemical Sensors and Biosensors

    Christopher M. A. Brett

    295 citationsOpen access (CC-BY)doi:10.3390/molecules27051497OpenAlex

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    Electrochemical impedance spectroscopy is finding increasing use in electrochemical sensors and biosensors, both in their characterisation, including during successive phases of sensor construction, and in application as a quantitative determination technique. Much of the published work continues to make little use of all the information that can be furnished by full physical modelling and analysis of the impedance spectra, and thus does not throw more than a superficial light on the processes occurring. Analysis is often restricted to estimating values of charge transfer resistances without interpretation and ignoring other electrical equivalent circuit components. In this article, the important basics of electrochemical impedance for electrochemical sensors and biosensors are presented, focussing on the necessary electrical circuit elements. This is followed by examples of its use in characterisation and in electroanalytical applications, at the same time demonstrating how fuller use can be made of the information obtained from complete modelling and analysis of the data in the…

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    Formation and Analysis of Volatile and Odor Compounds in Meat—A Review

    Julian Bleicher, Elmar E. Ebner, Kathrine H. Bak

    265 citationsOpen access (CC-BY)doi:10.3390/molecules27196703OpenAlex

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    The volatile composition and odor of meat and meat products is based on the precursors present in the raw meat. These are influenced by various pre-slaughter factors (species, breed, sex, age, feed, muscle type). Furthermore, post-mortem conditions (chiller aging, cooking conditions, curing, fermentation, etc.) determine the development of meat volatile organic compounds (VOCs). In this review, the main reactions leading to the development of meat VOCs such as the Maillard reaction; Strecker degradation; lipid oxidation; and thiamine, carbohydrate, and nucleotide degradation are described. The important pre-slaughter factors and post-mortem conditions influencing meat VOCs are discussed. Finally, the pros, cons, and future perspectives of the most commonly used sample preparation techniques (solid-phase microextraction, stir bar sorptive extraction, dynamic headspace extraction) and analytical methods (gas chromatography mass spectrometry and olfactometry, as well as electronic noses) for the analysis of meat VOCs are discussed, and the continued importance of sensorial analysis is…

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    A Comprehensive Review of Rosmarinic Acid: From Phytochemistry to Pharmacology and Its New Insight

    Huaquan Guan, Wenbin Luo, Beihua Bao, Yudan Cao, Fang-Fang Cheng and 5 more

    253 citationsOpen access (CC-BY)doi:10.3390/molecules27103292OpenAlex

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    ) is well-known, and is present in over 160 species belonging to many families, especially the Lamiaceae. Aside from this herbal ingredient, dozens of its natural derivatives have also been isolated and characterized from many natural plants. In recent years, with the increasing focus on the natural products as alternative treatments, a large number of pharmacological studies have been carried out to demonstrate the various biological activities of RA such as anti-inflammation, anti-oxidation, anti-diabetes, anti-virus, anti-tumor, neuroprotection, hepatoprotection, etc. In addition, investigations concerning its biosynthesis, extraction, analysis, clinical applications, and pharmacokinetics have also been performed. Although many achievements have been made in various research aspects, there still exist some problems or issues to be answered, especially its toxicity and bioavailability. Thus, we hope that in the case of natural products, the present review can not only provide a comprehensive understanding on RA covering its miscellaneous research fields, but also highlight some of…

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    A Review of Microalgae- and Cyanobacteria-Based Biodegradation of Organic Pollutants

    Hussein El-Sayed Touliabah, Mostafa Mohamed El-Sheekh, Mona Mohamed Ismail, Hala Yassin El-Kassas

    251 citationsOpen access (CC-BY)doi:10.3390/molecules27031141OpenAlex

    Show abstract

    This review proposes a new bioremediation method based on the diverse functionalities of algae. A greenway for cleansing wastewater is more ecologically friendly and environmentally sustainable than prior methods with other bacteria. New bioremediation technology employing algae and cyanobacteria for the removal of a wide range of organic contaminants is reasonable and has great potential. The prevalence of organic contaminants in aquatic habitats may endanger the health and well-being of several marine creatures. Agriculture, industry, and household trash are just a few of the human-caused sources of organic pollutants that contaminate waterways around the world. Before wastewater can be released into waterways, it must be cleaned. Algae-based wastewater treatment systems are becoming increasingly popular because of their environmental sustainability and lack of secondary pollutants. According to the kind of pollutant, the physicochemical properties of wastewater, and the algal species, algae and cyanobacteria can absorb and accumulate a wide spectrum of organic pollutants at…

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    Selenium: An Antioxidant with a Critical Role in Anti-Aging

    Geir Bjørklund, Mariia Shanaida, Roman Lysiuk, Halyna Antonyak, Ivan M. Klishch and 2 more

    247 citationsOpen access (CC-BY)doi:10.3390/molecules27196613OpenAlex

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    Aging is characterized by an imbalance between damage inflicted by reactive oxygen species (ROS) and the antioxidative defenses of the organism. As a significant nutritional factor, the trace element selenium (Se) may remodel gradual and spontaneous physiological changes caused by oxidative stress, potentially leading to disease prevention and healthy aging. Se is involved in improving antioxidant defense, immune functions, and metabolic homeostasis. An inadequate Se status may reduce human life expectancy by accelerating the aging process or increasing vulnerability to various disorders, including immunity dysfunction, and cancer risk. This review highlights the available studies on the effective role of Se in aging mechanisms and shows the potential clinical implications related to its consumption. The main sources of organic Se and the advantages of its nanoformulations were also discussed.

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    Antimicrobial Mechanisms and Clinical Application Prospects of Antimicrobial Peptides

    Xin Li, Siyao Zuo, Wang Bin, Kaiyu Zhang, Yang Wang

    246 citationsOpen access (CC-BY)doi:10.3390/molecules27092675OpenAlex

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    Antimicrobial peptides are a type of small-molecule peptide that widely exist in nature and are components of the innate immunity of almost all living things. They play an important role in resisting foreign invading microorganisms. Antimicrobial peptides have a wide range of antibacterial activities against bacteria, fungi, viruses and other microorganisms. They are active against traditional antibiotic-resistant strains and do not easily induce the development of drug resistance. Therefore, they have become a hot spot of medical research and are expected to become a new substitute for fighting microbial infection and represent a new method for treating drug-resistant bacteria. This review briefly introduces the source and structural characteristics of antimicrobial peptides and describes those that have been used against common clinical microorganisms (bacteria, fungi, viruses, and especially coronaviruses), focusing on their antimicrobial mechanism of action and clinical application prospects.

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    Amyloidosis in Alzheimer’s Disease: Pathogeny, Etiology, and Related Therapeutic Directions

    Chen Ma, Fen‐Fang Hong, Shu‐Long Yang

    242 citationsOpen access (CC-BY)doi:10.3390/molecules27041210OpenAlex

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    The amyloid hypothesis of Alzheimer's disease has long been the predominant theory, suggesting that Alzheimer's disease is caused by the accumulation of amyloid beta protein (Aβ) in the brain, leading to neuronal toxicity in the central nervous system (CNS). Because of breakthroughs in molecular medicine, the amyloid pathway is thought to be central to the pathophysiology of Alzheimer's disease (AD). Currently, it is believed that altered biochemistry of the Aβ cycle remains a central biological feature of AD and is a promising target for treatment. This review provides an overview of the process of amyloid formation, explaining the transition from amyloid precursor protein to amyloid beta protein. Moreover, we also reveal the relationship between autophagy, cerebral blood flow, ACHE, expression of LRP1, and amyloidosis. In addition, we discuss the detailed pathogenesis of amyloidosis, including oxidative damage, tau protein, NFTs, and neuronal damage. Finally, we list some ways to treat AD in terms of decreasing the accumulation of Aβ in the brain.

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    Thiazole: A Versatile Standalone Moiety Contributing to the Development of Various Drugs and Biologically Active Agents

    Mohammed Faiz Arshad, Aftab Alam, Abdullah Ayed Alshammari, Mohammed Bader Alhazza, Ibrahim Mohammed Alzimam and 11 more

    235 citationsOpen access (CC-BY)doi:10.3390/molecules27133994OpenAlex

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    For many decades, the thiazole moiety has been an important heterocycle in the world of chemistry. The thiazole ring consists of sulfur and nitrogen in such a fashion that the pi (π) electrons are free to move from one bond to other bonds rendering aromatic ring properties. On account of its aromaticity, the ring has many reactive positions where donor-acceptor, nucleophilic, oxidation reactions, etc., may take place. Molecules containing a thiazole ring, when entering physiological systems, behave unpredictably and reset the system differently. These molecules may activate/stop the biochemical pathways and enzymes or stimulate/block the receptors in the biological systems. Therefore, medicinal chemists have been focusing their efforts on thiazole-bearing compounds in order to develop novel therapeutic agents for a variety of pathological conditions. This review attempts to inform the readers on three major classes of thiazole-bearing molecules: Thiazoles as treatment drugs, thiazoles in clinical trials, and thiazoles in preclinical and developmental stages. A compilation of…

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    Lysozyme and Its Application as Antibacterial Agent in Food Industry

    Nida Nawaz, Sai Wen, Fenghuan Wang, Shiza Nawaz, Junaid Raza and 2 more

    232 citationsOpen access (CC-BY)doi:10.3390/molecules27196305OpenAlex

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    Lysozymes are hydrolytic enzymes characterized by their ability to cleave the β-(1,4)-glycosidic bonds in peptidoglycan, a major structural component of the bacterial cell wall. This hydrolysis action compromises the integrity of the cell wall, causing the lysis of bacteria. For more than 80 years, its role of antibacterial defense in animals has been renowned, and it is also used as a preservative in foods and pharmaceuticals. In order to improve the antimicrobial efficacy of lysozyme, extensive research has been intended for its modifications. This manuscript reviews the natural antibiotic compound lysozyme with reference to its catalytic and non-catalytic mode of antibacterial action, lysozyme types, susceptibility and resistance of bacteria, modification of lysozyme molecules, and its applications in the food industry.

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    Anticancer Drugs: Recent Strategies to Improve Stability Profile, Pharmacokinetic and Pharmacodynamic Properties

    Giuseppina Ioele, Martina Chieffallo, Maria Antonietta Occhiuzzi, Michele De Luca, Antonio Garofalo and 2 more

    227 citationsOpen access (CC-BY)doi:10.3390/molecules27175436OpenAlex

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    In past decades, anticancer research has led to remarkable results despite many of the approved drugs still being characterized by high systemic toxicity mainly due to the lack of tumor selectivity and present pharmacokinetic drawbacks, including low water solubility, that negatively affect the drug circulation time and bioavailability. The stability studies, performed in mild conditions during their development or under stressing exposure to high temperature, hydrolytic medium or light source, have demonstrated the sensitivity of anticancer drugs to many parameters. For this reason, the formation of degradation products is assessed both in pharmaceutical formulations and in the environment as hospital waste. To date, numerous formulations have been developed for achieving tissue-specific drug targeting and reducing toxic side effects, as well as for improving drug stability. The development of prodrugs represents a promising strategy in targeted cancer therapy for improving the selectivity, efficacy and stability of active compounds. Recent studies show that the incorporation of…

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    Trends and Technological Advancements in the Possible Food Applications of Spirulina and Their Health Benefits: A Review

    Nawal K. Z. AlFadhly, Nawfal Alhelfi, Ammar B. Altemimi, Deepak Kumar Verma, Francesco Cacciola and 1 more

    225 citationsOpen access (CC-BY)doi:10.3390/molecules27175584OpenAlex

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    Spirulina is a kind of blue-green algae (BGA) that is multicellular, filamentous, and prokaryotic. It is also known as a cyanobacterium. It is classified within the phylum known as blue-green algae. Despite the fact that it includes a high concentration of nutrients, such as proteins, vitamins, minerals, and fatty acids-in particular, the necessary omega-3 fatty acids and omega-6 fatty acids-the percentage of total fat and cholesterol that can be found in these algae is substantially lower when compared to other food sources. This is the case even if the percentage of total fat that can be found in these algae is also significantly lower. In addition to this, spirulina has a high concentration of bioactive compounds, such as phenols, phycocyanin pigment, and polysaccharides, which all take part in a number of biological activities, such as antioxidant and anti-inflammatory activity. As a result of this, spirulina has found its way into the formulation of a great number of medicinal foods, functional foods, and nutritional supplements. Therefore, this article makes an effort to shed…

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    Natural Compounds and Products from an Anti-Aging Perspective

    Geir Bjørklund, Mariia Shanaida, Roman Lysiuk, Monica Butnariu, Massimiliano Peana and 4 more

    222 citationsOpen access (CC-BY)doi:10.3390/molecules27207084OpenAlex

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    Aging is a very complex process that is accompanied by a degenerative impairment in many of the major functions of the human body over time. This inevitable process is influenced by hereditary factors, lifestyle, and environmental influences such as xenobiotic pollution, infectious agents, UV radiation, diet-borne toxins, and so on. Many external and internal signs and symptoms are related with the aging process and senescence, including skin dryness and wrinkles, atherosclerosis, diabetes, neurodegenerative disorders, cancer, etc. Oxidative stress, a consequence of the imbalance between pro- and antioxidants, is one of the main provoking factors causing aging-related damages and concerns, due to the generation of highly reactive byproducts such as reactive oxygen and nitrogen species during the metabolism, which result in cellular damage and apoptosis. Antioxidants can prevent these processes and extend healthy longevity due to the ability to inhibit the formation of free radicals or interrupt their propagation, thereby lowering the level of oxidative stress. This review focuses on…

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    MXenes as Emerging Materials: Synthesis, Properties, and Applications

    Ubaid Ur Rahman, Muhammad Humayun, Usman ul Ghani, Muhammad Usman, Habib Ullah and 3 more

    220 citationsOpen access (CC-BY)doi:10.3390/molecules27154909OpenAlex

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    Due to their unique layered microstructure, the presence of various functional groups at the surface, earth abundance, and attractive electrical, optical, and thermal properties, MXenes are considered promising candidates for the solution of energy- and environmental-related problems. It is seen that the energy conversion and storage capacity of MXenes can be enhanced by changing the material dimensions, chemical composition, structure, and surface chemistry. Hence, it is also essential to understand how one can easily improve the structure-property relationship from an applied point of view. In the current review, we reviewed the fabrication, properties, and potential applications of MXenes. In addition, various properties of MXenes such as structural, optical, electrical, thermal, chemical, and mechanical have been discussed. Furthermore, the potential applications of MXenes in the areas of photocatalysis, electrocatalysis, nitrogen fixation, gas sensing, cancer therapy, and supercapacitors have also been outlooked. Based on the reported works, it could easily be observed that the…

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    Effect of Ginger on Inflammatory Diseases

    Pura Ballester, Begoña Cerdá, Raúl Arcusa, Javier Marhuenda, Karen Yamedjeu and 1 more

    219 citationsOpen access (CC-BY)doi:10.3390/molecules27217223OpenAlex

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    Ulcerative colitis, Crohn’s disease, rheumatoid arthritis, psoriasis, and lupus erythematosus are some of common inflammatory diseases. These affections are highly disabling and share signals such as inflammatory sequences and immune dysregulation. The use of foods with anti-inflammatory properties such as ginger (Zingiber officinale Roscoe) could improve the quality of life of these patients. Ginger is a plant widely used and known by its bioactive compounds. There is enough evidence to prove that ginger possesses multiple biological activities, especially antioxidant and anti-inflammatory capacities. In this review, we summarize the current knowledge about the bioactive compounds of ginger and their role in the inflammatory process and its signaling pathways. We can conclude that the compounds 6-shoagol, zingerone, and 8-shoagol display promising results in human and animal models, reducing some of the main symptoms of some inflammatory diseases such as arthritis. For lupus, 6-gingerol demonstrated a protective attenuating neutrophil extracellular trap release in response to…

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    Glutathione in Brain Disorders and Aging

    Igor Y. Iskusnykh, Anastasia A. Zakharova, Dhruba Pathak

    213 citationsOpen access (CC-BY)doi:10.3390/molecules27010324OpenAlex

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    Glutathione is a remarkably functional molecule with diverse features, which include being an antioxidant, a regulator of DNA synthesis and repair, a protector of thiol groups in proteins, a stabilizer of cell membranes, and a detoxifier of xenobiotics. Glutathione exists in two states-oxidized and reduced. Under normal physiological conditions of cellular homeostasis, glutathione remains primarily in its reduced form. However, many metabolic pathways involve oxidization of glutathione, resulting in an imbalance in cellular homeostasis. Impairment of glutathione function in the brain is linked to loss of neurons during the aging process or as the result of neurological diseases such as Huntington's disease, Parkinson's disease, stroke, and Alzheimer's disease. The exact mechanisms through which glutathione regulates brain metabolism are not well understood. In this review, we will highlight the common signaling cascades that regulate glutathione in neurons and glia, its functions as a neuronal regulator in homeostasis and metabolism, and finally a mechanistic recapitulation of…

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    Modern Methods of Pre-Treatment of Plant Material for the Extraction of Bioactive Compounds

    Aneta Krakowska‐Sieprawska, Anna Kiełbasa, Katarzyna Rafińska, Magdalena Ligor, Bogusław Buszewski

    212 citationsOpen access (CC-BY)doi:10.3390/molecules27030730OpenAlex

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    In this review, recent advances in the methods of pre-treatment of plant material for the extraction of secondary metabolites with high biological activity are presented. The correct preparation of the material for extraction is as important as the selection of the extraction method. This step should prevent the degradation of bioactive compounds as well as the development of fungi and bacteria. Currently, the methods of preparation are expected to modify the particles of the plant material in such a way that will contribute to the release of bioactive compounds loosely bonded to cell wall polymers. This review presents a wide range of methods of preparing plant material, including drying, freeze-drying, convection drying, microwave vacuum drying, enzymatic processes, and fermentation. The influence of the particular methods on the structure of plant material particles, the level of preserved bioactive compounds, and the possibility of their release during the extraction were highlighted. The plant material pre-treatment techniques used were discussed with respect to the amount of…

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    Tannin in Ruminant Nutrition: Review

    Maghsoud Besharati, Aristide Maggiolino, Valiollah Palangı, Adem Kaya, Muhammad Jabbar and 3 more

    210 citationsOpen access (CC-BY)doi:10.3390/molecules27238273OpenAlex

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    Tannins are polyphenols characterized by different molecular weights that plants are able to synthetize during their secondary metabolism. Macromolecules (proteins, structural carbohydrates and starch) can link tannins and their digestion can decrease. Tannins can be classified into two groups: hydrolysable tannins and condensed tannins. Tannins are polyphenols, which can directly or indirectly affect intake and digestion. Their ability to bind molecules and form complexes depends on the structure of polyphenols and on the macromolecule involved. Tannins have long been known to be an "anti-nutritional agent" in monogastric and poultry animals. Using good tannins' proper application protocols helped the researchers observe positive effects on the intestinal microbial ecosystem, gut health, and animal production. Plant tannins are used as an alternative to in-feed antibiotics, and many factors have been described by researchers which contribute to the variability in their efficiencies. The objective of this study was to review the literature about tannins, their effects and use in…

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    The Utilization of Algae and Seaweed Biomass for Bioremediation of Heavy Metal-Contaminated Wastewater

    Hussein Tawfeek Znad, Md. Rabiul Awual, RA Sri Martini

    210 citationsOpen access (CC-BY)doi:10.3390/molecules27041275OpenAlex

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    The presence of heavy metals in water bodies is linked to the increasing number of industries and populations. This has serious consequences for the quality of human health and the environment. In accordance with this issue, water and wastewater treatment technologies including ion exchange, chemical extraction, and hydrolysis should be conducted as a first water purification stage. However, the sequestration of these toxic substances tends to be expensive, especially for large scale treatment methods that require tedious control and have limited efficiency. Therefore, adsorption methods using adsorbents derived from biomass represent a promising alternative due to their great efficiency and abundance. Algal and seaweed biomass has appeared as a sustainable solution for environmentally friendly adsorbent production. This review further discusses recent developments in the use of algal and seaweed biomass as potential sorbent for heavy metal bioremediation. In addition, relevant aspects like metal toxicity, adsorption mechanism, and parameters affecting the completion of adsorption…

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    Phenolic Compounds in Active Packaging and Edible Films/Coatings: Natural Bioactive Molecules and Novel Packaging Ingredients

    Ajit Kumar Singh, Jae Young Kim, Youn Suk Lee

    208 citationsOpen access (CC-BY)doi:10.3390/molecules27217513OpenAlex

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    In recent years, changing lifestyles and food consumption patterns have driven demands for high-quality, ready-to-eat food products that are fresh, clean, minimally processed, and have extended shelf lives. This demand sparked research into the creation of novel tools and ingredients for modern packaging systems. The use of phenolic-compound-based active-packaging and edible films/coatings with antimicrobial and antioxidant activities is an innovative approach that has gained widespread attention worldwide. As phenolic compounds are natural bioactive molecules that are present in a wide range of foods, such as fruits, vegetables, herbs, oils, spices, tea, chocolate, and wine, as well as agricultural waste and industrial byproducts, their utilization in the development of packaging materials can lead to improvements in the oxidative status and antimicrobial properties of food products. This paper reviews recent trends in the use of phenolic compounds as potential ingredients in food packaging, particularly for the development of phenolic compounds-based active packaging and edible…

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    Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review

    Vivek P. Chavda, Jinal Ajabiya, Divya Teli, Joanna Bojarska, Vasso Apostolopoulos

    208 citationsOpen access (CC-BY)doi:10.3390/molecules27134315OpenAlex

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    The prevalence of obesity and diabetes is an increasing global problem, especially in developed countries, and is referred to as the twin epidemics. As such, advanced treatment approaches are needed. Tirzepatide, known as a ‘twincretin’, is a ‘first-in-class’ and the only dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) receptor agonist, that can significantly reduce glycemic levels and improve insulin sensitivity, as well as reducing body weight by more than 20% and improving lipid metabolism. This novel anti-diabetic drug is a synthetic peptide analog of the human GIP hormone with a C20 fatty-diacid portion attached which, via acylation technology, can bind to albumin in order to provide a dose of the drug, by means of subcutaneous injection, once a week, which is appropriate to its a half-life of about five days. Tirzepatide, developed by Eli Lilly, was approved, under the brand name Mounjaro, by the United States Food and Drug Administration in May 2022. This started the ‘twincretin’ era of enormously important and appealing dual…

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    Phytochemistry and Biological Activity of Medicinal Plants in Wound Healing: An Overview of Current Research

    Stefania Vitale, Sara Colanero, Martina Placidi, Giovanna Di Emidio, Carla Tatone and 2 more

    207 citationsOpen access (CC-BY)doi:10.3390/molecules27113566OpenAlex

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    Wound healing is a complicated process, and the effective management of wounds is a major challenge. Natural herbal remedies have now become fundamental for the management of skin disorders and the treatment of skin infections due to the side effects of modern medicine and lower price for herbal products. The aim of the present study is to summarize the most recent in vitro, in vivo, and clinical studies on major herbal preparations, their phytochemical constituents, and new formulations for wound management. Research reveals that several herbal medicaments have marked activity in the management of wounds and that this activity is ascribed to flavonoids, alkaloids, saponins, and phenolic compounds. These phytochemicals can act at different stages of the process by means of various mechanisms, including anti-inflammatory, antimicrobial, antioxidant, collagen synthesis stimulating, cell proliferation, and angiogenic effects. The application of natural compounds using nanotechnology systems may provide significant improvement in the efficacy of wound treatments. Increasing the clinical…

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    Metallo-Drugs in Cancer Therapy: Past, Present and Future

    Roxana Liana Lucaciu, Adriana Corina Hangan, Bogdan Sevastre, Luminita Simona Oprean

    205 citationsOpen access (CC-BY)doi:10.3390/molecules27196485OpenAlex

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    Cancer treatments which include conventional chemotherapy have not proven very successful in curing human malignancies. The failures of these treatment modalities include inherent resistance, systemic toxicity and severe side effects. Out of 50% patients administrated to chemotherapy, only 5% survive. For these reasons, the identification of new drug designs and therapeutic strategies that could target cancer cells while leaving normal cells unaffected still continues to be a challenge. Despite advances that have led to the development of new therapies, treatment options are still limited for many types of cancers. This review provides an overview of platinum, copper and ruthenium metal based anticancer drugs in clinical trials and in vitro/in vivo studies. Presumably, copper and ruthenium complexes have greater potential than Pt(II) complexes, showing reduced toxicity, a new mechanism of action, a different spectrum of activity and the possibility of non-cross-resistance. We focus the discussion towards past, present and future aspects.

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    Analytical Evaluation of Carbamate and Organophosphate Pesticides in Human and Environmental Matrices: A Review

    Nonkululeko Landy Mdeni, Abiodun Olagoke Adeniji, Anthony Ifeanyi Okoh, Omobola Oluranti Okoh

    205 citationsOpen access (CC-BY)doi:10.3390/molecules27030618OpenAlex

    Show abstract

    Pesticides are synthetic compounds that may become environmental contaminants through their use and application. The high productivity achieved in the agricultural industry can be credited to the use and application of pesticides by way of pest and insect control. As much as pesticides have a positive impact on the agricultural industry, some disadvantages come with their application in the environment because they are intentionally toxic, and this is more towards non-target organisms. They are grouped into chlorophenols, organochlorines, synthetic pyrethroid, carbamates, and organophosphorus based on their structure. The symptoms of exposure to carbamate (CM) and organophosphates (OP) are similar, although poisoning from CM is of a shorter duration. The analytical evaluation of carbamate and organophosphate pesticides in human and environmental matrices are reviewed using suitable extraction and analytical methods.

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    Green Extraction Techniques as Advanced Sample Preparation Approaches in Biological, Food, and Environmental Matrices: A Review

    José S. Câmara, Rosa Perestrelo, Cristina V. Berenguer, Carolina F. P. Andrade, Telma M. Gomes and 5 more

    203 citationsOpen access (CC-BY)doi:10.3390/molecules27092953OpenAlex

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    Green extraction techniques (GreETs) emerged in the last decade as greener and sustainable alternatives to classical sample preparation procedures aiming to improve the selectivity and sensitivity of analytical methods, simultaneously reducing the deleterious side effects of classical extraction techniques (CETs) for both the operator and the environment. The implementation of improved processes that overcome the main constraints of classical methods in terms of efficiency and ability to minimize or eliminate the use and generation of harmful substances will promote more efficient use of energy and resources in close association with the principles supporting the concept of green chemistry. The current review aims to update the state of the art of some cutting-edge GreETs developed and implemented in recent years focusing on the improvement of the main analytical features, practical aspects, and relevant applications in the biological, food, and environmental fields. Approaches to improve and accelerate the extraction efficiency and to lower solvent consumption, including…

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    Biofortification—A Frontier Novel Approach to Enrich Micronutrients in Field Crops to Encounter the Nutritional Security

    Salwinder Singh Dhaliwal, Vivek Sharma, Arvind Kumar Shukla, Vibha Verma, Manmeet Kaur and 8 more

    202 citationsOpen access (CC-BY)doi:10.3390/molecules27041340OpenAlex

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    Globally, many developing countries are facing silent epidemics of nutritional deficiencies in human beings and animals. The lack of diversity in diet, i.e., cereal-based crops deficient in mineral nutrients is an additional threat to nutritional quality. The present review accounts for the significance of biofortification as a process to enhance the productivity of crops and also an agricultural solution to address the issues of nutritional security. In this endeavor, different innovative and specific biofortification approaches have been discussed for nutrient enrichment of field crops including cereals, pulses, oilseeds and fodder crops. The agronomic approach increases the micronutrient density in crops with soil and foliar application of fertilizers including amendments. The biofortification through conventional breeding approach includes the selection of efficient genotypes, practicing crossing of plants with desirable nutritional traits without sacrificing agricultural and economic productivity. However, the transgenic/biotechnological approach involves the synthesis of…

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    Anticancer Effects and Mechanisms of Berberine from Medicinal Herbs: An Update Review

    Ruo-Gu Xiong, Siyu Huang, Si-Xia Wu, Dan-Dan Zhou, Zhijun Yang and 6 more

    199 citationsOpen access (CC-BY)doi:10.3390/molecules27144523OpenAlex

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    Cancer has been a serious public health problem. Berberine is a famous natural compound from medicinal herbs and shows many bioactivities, such as antioxidant, anti-inflammatory, antidiabetic, anti-obesity, and antimicrobial activities. In addition, berberine shows anticancer effects on a variety of cancers, such as breast, lung, gastric, liver, colorectal, ovarian, cervical, and prostate cancers. The underlying mechanisms of action include inhibiting cancer cell proliferation, suppressing metastasis, inducing apoptosis, activating autophagy, regulating gut microbiota, and improving the effects of anticancer drugs. This paper summarizes effectiveness and mechanisms of berberine on different cancers and highlights the mechanisms of action. In addition, the nanotechnologies to improve bioavailability of berberine are included. Moreover, the side effects of berberine are also discussed. This paper is helpful for the prevention and treatment of cancers using berberine.

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    Pretreatment of Wheat Straw Lignocelluloses by Deep Eutectic Solvent for Lignin Extraction

    Hongzhi Ma, Penglu Fu, Jihua Zhao, Xingxing Lin, Wenyu Wu and 5 more

    198 citationsOpen access (CC-BY)doi:10.3390/molecules27227955OpenAlex

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    In order to increase the fractionation efficiency of the wheat straw, a deep eutectic solvent (DES) system consisting of chlorine/lactic acid was used in this study for wheat straw pretreatment. The outcomes exhibited that DES pretreatment significantly enhanced the capability to extract lignin, retain cellulose, and remove hemicellulose. The best condition for the pretreatment of wheat straw was 150 °C for 6 h. The process retained most cellulose in the pretreated biomass (49.94-73.60%), and the enzymatic digestibility of the pretreatment residue reached 89.98%. Further characterization of lignin showed that the high yield (81.54%) and the high purity (91.33%) resulted from the ether bond cleavage in lignin and the connection between hemicellulose and lignin. As for application, the enzymatic hydrolysis of the best condition reached 89.98%, and the lignin also had suitable stability. The investigation exhibited that DES pretreatment has the potential to realize an efficient fractionation of lignocellulosic biomass into high-applicability cellulose and lignin of high-quality.

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    Propolis: Its Role and Efficacy in Human Health and Diseases

    Nadzirah Zullkiflee, Hussein Taha, Anwar Usman

    191 citationsOpen access (CC-BY)doi:10.3390/molecules27186120OpenAlex

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    honeybees as alternative complementary medicines for the potential treatment of various acute and chronic diseases. Propolis can be found in tropical and subtropical forests throughout the world. The composition of phytochemical constituents in propolis varies depending on the bee species, geographical location, botanical source, and environmental conditions. Typically, propolis contains lipid, beeswax, essential oils, pollen, and organic components. The latter include flavonoids, phenolic compounds, polyphenols, terpenes, terpenoids, coumarins, steroids, amino acids, and aromatic acids. The biologically active constituents of propolis, which include countless organic compounds such as artepillin C, caffeic acid, caffeic acid phenethyl ester, apigenin, chrysin, galangin, kaempferol, luteolin, genistein, naringin, pinocembrin, coumaric acid, and quercetin, have a broad spectrum of biological and therapeutic properties such as antidiabetic, anti-inflammatory, antioxidant, anticancer, rheumatoid arthritis, chronic obstruct pulmonary disorders, cardiovascular diseases, respiratory…

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    Protein–Ligand Docking in the Machine-Learning Era

    Chao Yang, Eric Anthony Chen, Yingkai Zhang

    191 citationsOpen access (CC-BY)doi:10.3390/molecules27144568OpenAlex

    Show abstract

    Molecular docking plays a significant role in early-stage drug discovery, from structure-based virtual screening (VS) to hit-to-lead optimization, and its capability and predictive power is critically dependent on the protein-ligand scoring function. In this review, we give a broad overview of recent scoring function development, as well as the docking-based applications in drug discovery. We outline the strategies and resources available for structure-based VS and discuss the assessment and development of classical and machine learning protein-ligand scoring functions. In particular, we highlight the recent progress of machine learning scoring function ranging from descriptor-based models to deep learning approaches. We also discuss the general workflow and docking protocols of structure-based VS, such as structure preparation, binding site detection, docking strategies, and post-docking filter/re-scoring, as well as a case study on the large-scale docking-based VS test on the LIT-PCBA data set.

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    The Bioavailability and Biological Activities of Phytosterols as Modulators of Cholesterol Metabolism

    Xiang Li, Yan Xin, Yuqian Mo, Pavel M. Marozik, Taiping He and 1 more

    189 citationsOpen access (CC-BY)doi:10.3390/molecules27020523OpenAlex

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    Phytosterols are natural sterols widely found in plants that have a variety of physiological functions, and their role in reducing cholesterol absorption has garnered much attention. Although the bioavailability of phytosterols is only 0.5-2%, they can still promote cholesterol balance in the body. A mechanism of phytosterols for lowering cholesterol has now been proposed. They not only reduce the uptake of cholesterol in the intestinal lumen and affect its transport, but also regulate the metabolism of cholesterol in the liver. In addition, phytosterols can significantly reduce the plasma concentration of total cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C), with a dose-response relationship. Ingestion of 3 g of phytosterols per day can reach the platform period, and this dose can reduce LDL-C by about 10.7%. On the other hand, phytosterols can also activate the liver X receptor α-CPY7A1 mediated bile acids excretion pathway and accelerate the transformation and metabolism of cholesterol. This article reviews the research progress of phytosterols as a…

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    Recent Update on the Anti-Inflammatory Activities of Propolis

    Felix Zulhendri, Ronny Lesmana, Steven Tandean, Andreas Christoper, Kavita Chandrasekaran and 4 more

    185 citationsOpen access (CC-BY)doi:10.3390/molecules27238473OpenAlex

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    In recent years, research has demonstrated the efficacy propolis as a potential raw material for pharmaceuticals and nutraceuticals. There is limited report detailing the mechanisms of action of propolis and its bioactive compounds in relation to their anti-inflammatory properties. Thus, the aim of the present review is to examine the latest experimental evidence (2017-2022) regarding the anti-inflammatory properties of propolis. A systematic scoping review methodology was implemented. After applying the exclusion criteria, a total of 166 research publications were identified and retrieved from Scopus, Web of Science, and Pubmed. Several key themes related to the anti-inflammatory properties of propolis were subsequently identified, namely in relation to cancers, oral health, metabolic syndrome, organ toxicity and inflammation, immune system, wound healing, and pathogenic infections. Based on the latest experimental evidence, propolis is demonstrated to possess various mechanisms of action in modulating inflammation towards the regulatory balance and anti-inflammatory environment.…

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    8-oxoguanine and 8-oxodeoxyguanosine Biomarkers of Oxidative DNA Damage: A Review on HPLC–ECD Determination

    Ana-Maria Chiorcea Paquim

    185 citationsOpen access (CC-BY)doi:10.3390/molecules27051620OpenAlex

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    Reactive oxygen species (ROS) are continuously produced in living cells due to metabolic and biochemical reactions and due to exposure to physical, chemical and biological agents. Excessive ROS cause oxidative stress and lead to oxidative DNA damage. Within ROS-mediated DNA lesions, 8-oxoguanine (8-oxoG) and its nucleotide 8-oxo-2'-deoxyguanosine (8-oxodG)-the guanine and deoxyguanosine oxidation products, respectively, are regarded as the most significant biomarkers for oxidative DNA damage. The quantification of 8-oxoG and 8-oxodG in urine, blood, tissue and saliva is essential, being employed to determine the overall effects of oxidative stress and to assess the risk, diagnose, and evaluate the treatment of autoimmune, inflammatory, neurodegenerative and cardiovascular diseases, diabetes, cancer and other age-related diseases. High-performance liquid chromatography with electrochemical detection (HPLC-ECD) is largely employed for 8-oxoG and 8-oxodG determination in biological samples due to its high selectivity and sensitivity, down to the femtomolar range. This review seeks to…

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    The Lactoferrin Phenomenon—A Miracle Molecule

    Paweł Kowalczyk, Katarzyna Kaczyńska, Patrycja Kleczkowska, Iwona Bukowska‐Ośko, Karol Kramkowski and 1 more

    180 citationsOpen access (CC-BY)doi:10.3390/molecules27092941OpenAlex

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    Numerous harmful factors that affect the human body from birth to old age cause many disturbances, e.g., in the structure of the genome, inducing cell apoptosis and their degeneration, which leads to the development of many diseases, including cancer. Among the factors leading to pathological processes, microbes, viruses, gene dysregulation and immune system disorders have been described. The function of a protective agent may be played by lactoferrin as a "miracle molecule", an endogenous protein with a number of favorable antimicrobial, antiviral, antioxidant, immunostimulatory and binding DNA properties. The purpose of this article is to present the broad spectrum of properties and the role that lactoferrin plays in protecting human cells at all stages of life.

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    FNDC5/Irisin: Physiology and Pathophysiology

    Rashid Waseem, Anas Shamsi, Taj Mohammad, Md. Imtaiyaz Hassan, Syed Naqui Kazim and 5 more

    180 citationsOpen access (CC-BY)doi:10.3390/molecules27031118OpenAlex

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    A sedentary lifestyle or lack of physical activity increases the risk of different diseases, including obesity, diabetes, heart diseases, certain types of cancers, and some neurological diseases. Physical exercise helps improve quality of life and reduces the risk of many diseases. Irisin, a hormone induced by exercise, is a fragmented product of FNDC5 (a cell membrane protein) and acts as a linkage between muscles and other tissues. Over the past decade, it has become clear that irisin is a molecular mimic of exercise and shows various beneficial effects, such as browning of adipocytes, modulation of metabolic processes, regulation of bone metabolism, and functioning of the nervous system. Irisin has a role in carcinogenesis; numerous studies have shown its impact on migration, invasion, and proliferation of cancer cells. The receptor of irisin is not completely known; however, in some tissues it probably acts via a specific class of integrin receptors. Here, we review research from the past decade that has identified irisin as a potential therapeutic agent in the prevention or…

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    Theoretical, Equilibrium, Kinetics and Thermodynamic Investigations of Methylene Blue Adsorption onto Lignite Coal

    Naim Hasani, Teuta Selimi, Altin Mele, Veprim Thaçi, Jeton Halili and 2 more

    179 citationsOpen access (CC-BY)doi:10.3390/molecules27061856OpenAlex

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    The interaction of methylene blue (MB) dye with natural coal (collected from coal landfills of the Kosovo Energy Corporation) in aqueous solutions was studied using adsorption, kinetics, and thermodynamic data, and Monte Carlo (MC) calculations. In a batch procedure, the effects of contact duration, initial MB concentration, pH, and solution temperature on the adsorption process were examined. The Langmuir, Freundlich, Temkin, and Dubinin–Radushkevich (D–R) isotherms were used to examine the equilibrium adsorption data. The equilibrium data fit well to the Freundlich and Langmuir adsorption isotherm models; however, the Freundlich model suited the adsorption data to a slightly better extent than the Langmuir model. The kinetics experimental data was fitted using pseudo-first-order, first-order, pseudo-second-order, second-order, Elvoich equation, and diffusion models. The pseudo-second-order rate model manifested a superlative fit to the experimental data, while the adsorption of MB onto coal is regulated by both liquid film and intraparticle diffusions at the same time.…

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    Polyphenols in Metabolic Diseases

    Amin Gasmi, Pavan Kumar Mujawdiya, Sàdaf Noor, Roman Lysiuk, Roman Darmohray and 9 more

    176 citationsOpen access (CC-BY)doi:10.3390/molecules27196280OpenAlex

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    Polyphenols (PPs) are a large group of phytochemicals containing phenolic rings with two or more hydroxyl groups. They possess powerful antioxidant properties, multiple therapeutic effects, and possible health benefits in vivo and in vitro, as well as reported clinical studies. Considering their free-radical scavenging and anti-inflammatory properties, these substances can be used to treat different kinds of conditions associated with metabolic disorders. Many symptoms of metabolic syndrome (MtS), including obesity, dyslipidemia, atherosclerosis, elevated blood sugar, accelerating aging, liver intoxication, hypertension, as well as cancer and neurodegenerative disorders, are substantially relieved by dietary PPs. The present study explores the bioprotective properties and associated underlying mechanisms of PPs. A detailed understanding of these natural compounds will open up new opportunities for producing unique natural PP-rich dietary and medicinal plans, ultimately affirming their health benefits.

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    Antibacterial Mechanisms of Zinc Oxide Nanoparticle against Bacterial Food Pathogens Resistant to Beta-Lactam Antibiotics

    Rajapandiyan Krishnamoorthy, Jegan Athinarayanan, Vaiyapuri Subbarayan Periasamy, Mohammad A. Alshuniaber, Ghedeir Muslem Alshammari and 3 more

    175 citationsOpen access (CC-BY)doi:10.3390/molecules27082489OpenAlex

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    The increase in β-lactam-resistant Gram-negative bacteria is a severe recurrent problem in the food industry for both producers and consumers. The development of nanotechnology and nanomaterial applications has transformed many features in food science. The antibacterial activity of zinc oxide nanoparticles (ZnO NPs) and their mechanism of action on β-lactam-resistant Gram-negative food pathogens, such as Escherichia coli, Pseudomonas aeruginosa, Salmonella typhi, Serratia marcescens, Klebsiella pneumoniae, and Proteus mirabilis, are investigated in the present paper. The study results demonstrate that ZnO NPs possesses broad-spectrum action against these β-lactamase-producing strains. The minimal inhibitory and minimal bactericidal concentrations vary from 0.04 to 0.08 and 0.12 to 0.24 mg/mL, respectively. The ZnO NPs elevate the level of reactive oxygen species (ROS) and malondialdehyde in the bacterial cells as membrane lipid peroxidation. It has been confirmed from the transmission electron microscopy image of the treated bacterial cells that ZnO NPs diminish the permeable…

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    The Role of Serotonin Neurotransmission in Gastrointestinal Tract and Pharmacotherapy

    Tomasz Guzel, Dagmara Maria Mirowska-Guzel

    175 citationsOpen access (CC-BY)doi:10.3390/molecules27051680OpenAlex

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    5-Hydroxytryptamine (5-HT, serotonin) is a neurotransmitter in both the central nervous system and peripheral structures, acting also as a hormone in platelets. Although its concentration in the gut covers >90% of all organism resources, serotonin is mainly known as a neurotransmitter that takes part in the pathology of mental diseases. Serotonin modulates not only CNS neurons, but also pain transmission and platelet aggregation. In the periphery, 5-HT influences muscle motility in the gut, bronchi, uterus, and vessels directly and through neurons. Serotonin synthesis starts from hydroxylation of orally delivered tryptophan, followed by decarboxylation. Serotonin acts via numerous types of receptors and clinically plays a role in several neural, mental, and other chronic disorders, such as migraine, carcinoid syndrome, and some dysfunctions of the alimentary system. 5-HT acts as a paracrine hormone and growth factor. 5-HT receptors in both the brain and gut are targets for drugs modifying serotonin neurotransmission. The aim of the present article is to review the 5-HT receptors in…

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    The Potential Role of Apigenin in Cancer Prevention and Treatment

    Arshad Husain Rahmani, Mohammed A. Alsahli, Ahmad Almatroudi, Mashael Abdullah Almogbel, Amjad Ali Khan and 2 more

    174 citationsOpen access (CC-BY)doi:10.3390/molecules27186051OpenAlex

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    Cancer is the leading cause of death worldwide. In spite of advances in the treatment of cancer, currently used treatment modules including chemotherapy, hormone therapy, radiation therapy and targeted therapy causes adverse effects and kills the normal cells. Therefore, the goal of more effective and less side effects-based cancer treatment approaches is still at the primary position of present research. Medicinal plants or their bioactive ingredients act as dynamic sources of drugs due to their having less side effects and also shows the role in reduction of resistance against cancer therapy. Apigenin is an edible plant-derived flavonoid that has received significant scientific consideration for its health-promoting potential through modulation of inflammation, oxidative stress and various other biological activities. Moreover, the anti-cancer potential of apigenin is confirmed through its ability to modulate various cell signalling pathways, including tumor suppressor genes, angiogenesis, apoptosis, cell cycle, inflammation, apoptosis, PI3K/AKT, NF-κB, MAPK/ERK and STAT3…

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    The Role of Microencapsulation in Food Application

    Mariel Calderón‐Oliver, Edith Ponce‐Alquicira

    174 citationsOpen access (CC-BY)doi:10.3390/molecules27051499OpenAlex

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    Modern microencapsulation techniques are employed to protect active molecules or substances such as vitamins, pigments, antimicrobials, and flavorings, among others, from the environment. Microencapsulation offers advantages such as facilitating handling and control of the release and solubilization of active substances, thus offering a great area for food science and processing development. For instance, the development of functional food products, fat reduction, sensory improvement, preservation, and other areas may involve the use of microcapsules in various food matrices such as meat products, dairy products, cereals, and fruits, as well as in their derivatives, with good results. The versatility of applications arises from the diversity of techniques and materials used in the process of microencapsulation. The objective of this review is to report the state of the art in the application and evaluation of microcapsules in various food matrices, as a one-microcapsule-core system may offer different results according to the medium in which it is used. The inclusion of…

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    Mechanistic Insights into the Pharmacological Significance of Silymarin

    Karan Wadhwa, Rakesh Pahwa, Manish Kumar, Shobhit Kumar, Prabodh Chander Sharma and 6 more

    171 citationsOpen access (CC-BY)doi:10.3390/molecules27165327OpenAlex

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    Medicinal plants are considered the reservoir of diverse therapeutic agents and have been traditionally employed worldwide to heal various ailments for several decades. Silymarin is a plant-derived mixture of polyphenolic flavonoids originating from the fruits and akenes of Silybum marianum and contains three flavonolignans, silibinins (silybins), silychristin and silydianin, along with taxifolin. Silybins are the major constituents in silymarin with almost 70–80% abundance and are accountable for most of the observed therapeutic activity. Silymarin has also been acknowledged from the ancient period and is utilized in European and Asian systems of traditional medicine for treating various liver disorders. The contemporary literature reveals that silymarin is employed significantly as a neuroprotective, hepatoprotective, cardioprotective, antioxidant, anti-cancer, anti-diabetic, anti-viral, anti-hypertensive, immunomodulator, anti-inflammatory, photoprotective and detoxification agent by targeting various cellular and molecular pathways, including MAPK, mTOR, β-catenin and Akt,…

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    Antioxidant and Antimicrobial Peptides Derived from Food Proteins

    Guadalupe López-García, Octavio Dublán‐García, Daniel Arizmendi‐Cotero, Leobardo Manuel Gómez‐Oliván

    171 citationsOpen access (CC-BY)doi:10.3390/molecules27041343OpenAlex

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    Recently, the demand for food proteins in the market has increased due to a rise in degenerative illnesses that are associated with the excessive production of free radicals and the unwanted side effects of various drugs, for which researchers have suggested diets rich in bioactive compounds. Some of the functional compounds present in foods are antioxidant and antimicrobial peptides, which are used to produce foods that promote health and to reduce the consumption of antibiotics. These peptides have been obtained from various sources of proteins, such as foods and agri-food by-products, via enzymatic hydrolysis and microbial fermentation. Peptides with antioxidant properties exert effective metal ion (Fe2+/Cu2+) chelating activity and lipid peroxidation inhibition, which may lead to notably beneficial effects in promoting human health and food processing. Antimicrobial peptides are small oligo-peptides generally containing from 10 to 100 amino acids, with a net positive charge and an amphipathic structure; they are the most important components of the antibacterial defense of…

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    Toxicity of Selected Monoterpenes and Essential Oils Rich in These Compounds

    Karolina A. Wojtunik‐Kulesza

    169 citationsOpen access (CC-BY)doi:10.3390/molecules27051716OpenAlex

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    family. The compounds demonstrate antioxidative, antibacterial, sedative and anti-inflammatory activity, hence, they are often employed in medicine and pharmaceuticals. Additionally, their fragrant character is often made use of, notably in the food and cosmetic industries. Nevertheless, long-lasting studies have revealed their toxic properties. This fact has led to a detailed analysis of the compounds towards their side effects on the human organism. Although most are safe for human food and medical applications, there are monoterpene compounds that, in certain amounts or under particular circumstances (e.g., pregnancy), can cause serious disorders. The presented review characterises in vitro and in vivo, the toxic character of selected monoterpenes (α-terpinene, camphor, citral, limonene, pulegone, thujone), as well as that of their original plant sources and their essential oils. The selected monoterpenes reveal various toxic properties among which are embryotoxic, neurotoxic, allergenic and genotoxic. It is also known that the essential oils of popular plants can also reveal…

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    From Traditional Ethnopharmacology to Modern Natural Drug Discovery: A Methodology Discussion and Specific Examples

    Stergios Pirintsos, Athanasios A. Panagiotopoulos, Michael Bariotakis, Vangelis Daskalakis, Christos D Lionis and 4 more

    168 citationsOpen access (CC-BY)doi:10.3390/molecules27134060OpenAlex

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    Ethnopharmacology, through the description of the beneficial effects of plants, has provided an early framework for the therapeutic use of natural compounds. Natural products, either in their native form or after crude extraction of their active ingredients, have long been used by different populations and explored as invaluable sources for drug design. The transition from traditional ethnopharmacology to drug discovery has followed a straightforward path, assisted by the evolution of isolation and characterization methods, the increase in computational power, and the development of specific chemoinformatic methods. The deriving extensive exploitation of the natural product chemical space has led to the discovery of novel compounds with pharmaceutical properties, although this was not followed by an analogous increase in novel drugs. In this work, we discuss the evolution of ideas and methods, from traditional ethnopharmacology to in silico drug discovery, applied to natural products. We point out that, in the past, the starting point was the plant itself, identified by sustained…

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    Antioxidant, Anti-Obesity, Nutritional and Other Beneficial Effects of Different Chili Pepper: A Review

    Azrina Azlan, Sharmin Sultana, Chan Suk Huei, Muhammad Rizal Razman

    168 citationsOpen access (CC-BY)doi:10.3390/molecules27030898OpenAlex

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    Fruits and vegetables are important components of a healthy diet. They are rich sources of vitamins and minerals, dietary fibre and a host of beneficial non-nutrient substances including plant sterols, flavonoids and other antioxidants. It has been reported that reduced intake of fruits and vegetables may increase the risk of non-communicable diseases (NCDs). Chili pepper, is a common and important spice used to enhance taste and nutrition. Over the years, reports have shown its potential as antioxidant and an anti-obesity agent. Obesity is a serious health concern as it may initiate other common chronic diseases. Due to the side effects of synthetic antioxidants and anti-obesity drugs, scientists are now focusing on natural products which produce similar effects to synthetic chemicals. This up-to-date review addresses this research gap and presents, in an accessible format, the nutritional, antioxidant and anti-obesity properties of different chili peppers. This review article serves as a reference guide for use of chili peppers as anti-obesity agents.

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    Chamomile: A Review of Its Traditional Uses, Chemical Constituents, Pharmacological Activities and Quality Control Studies

    Yun-Lei Dai, Ying Li, Qi Wang, Feng-Jv Niu, Kunwei Li and 4 more

    166 citationsOpen access (CC-BY)doi:10.3390/molecules28010133OpenAlex

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    Matricaria chamomilla L. (MC) and Chamaemelum nobile (L.) All. (CN) are two varieties of Chamomile. These herbs have been used for thousands of years in Greece, Rome and ancient Egypt. Chamomile has been used for the treatment of stomach problems, cramps, dermatitis, and minor infections. The purpose of this study was to introduce the botanical characteristics and geographical distribution, traditional uses, chemical constituents, pharmacological activities, toxicity studies and quality control studies, and lay a theoretical foundation for the rational development and utilization of chamomile. This review powered that chemical constituents include flavonoids, coumarins, volatile oils, terpenes, organic acids, polysaccharides, and others. These compounds possess anticancer, anti-infective, anti-inflammatory, antithrombotic, antioxidant, hypolipidaemic, hypoglycaemic, antihypertensive, antidepressant, neuroprotective activities, among others. Chamomile is a widely used herb in traditional medicine. It brings great economic value due to its numerous pharmacological effects and…

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    Green Synthesis of Zinc Oxide Nanoparticles Using Pomegranate Fruit Peel and Solid Coffee Grounds vs. Chemical Method of Synthesis, with Their Biocompatibility and Antibacterial Properties Investigation

    Hala Mohamed Abdelmigid, Nahed Ahmed Hussien, Amal Ahmed Alyamani, Maissa M. Morsi, Noha Moslah Al Sufyani and 1 more

    166 citationsOpen access (CC-BY)doi:10.3390/molecules27041236OpenAlex

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    This research aims to investigate the synthesis, characterization, and evaluation of the biocompatibility and antibacterial activity of novel zinc oxide (ZnO) nanoparticles (NPs) prepared by Punica granatum peel and coffee ground extracts as the reducing and capping agents. Chemically synthesized ZnONPs were prepared using zinc acetate dihydrate and sodium hydroxide as reducing precursors. ZnONPs were characterized using an ultraviolet-visible spectrophotometer (UV-VIS), X-ray diffraction (XRD), scanning electron microscope (SEM), transmission electron microscope (TEM), and Fourier transform infrared (FTIR) spectroscopy. Peaks of UV spectra were 300 nm for ZnONPs_PPE, 320 nm (ZnONPs_CE), 290 nm, and 440 nm (ZnONP_Chem), thereby confirming ZnONPs formation. The X-ray diffractograms revealed their hexagonal structure. TEM micrographs of the biosynthesized ZnONPs revealed their hexagonal pattern and nanorod shape for ZnONPs_Chem with particle sizes of 118.6 nm, 115.7 nm, and 111.2 nm, respectively. The FTIR analysis demonstrated the presence of proteins, carboxyl, and hydroxyl groups…

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    Exosomes as New Generation Vehicles for Drug Delivery: Biomedical Applications and Future Perspectives

    Amarjitsing Rajput, Akansh Varshney, Rashi Bajaj, Varsha Pokharkar

    165 citationsOpen access (CC-BY)doi:10.3390/molecules27217289OpenAlex

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    Currently, particular interest among the scientific community is focused on exploring the use of exosomes for several pharmaceutical and biomedical applications. This is due to the identification of the role of exosomes as an excellent intercellular communicator by delivering the requisite cargo comprising of functional proteins, metabolites and nucleic acids. Exosomes are the smallest extracellular vesicles (EV) with sizes ranging from 30-100 nm and are derived from endosomes. Exosomes have similar surface morphology to cells and act as a signal transduction channel between cells. They encompass different biomolecules, such as proteins, nucleic acids and lipids, thus rendering them naturally as an attractive drug delivery vehicle. Like the other advanced drug delivery systems, such as polymeric nanoparticles and liposomes to encapsulate drug substances, exosomes also gained much attention in enhancing therapeutic activity. Exosomes present many advantages, such as compatibility with living tissues, low toxicity, extended blood circulation, capability to pass contents from one cell…

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    Recovering Microalgal Bioresources: A Review of Cell Disruption Methods and Extraction Technologies

    Md. Mijanur Rahman, Nushin Hosano, Hamid Hosano

    165 citationsOpen access (CC-BY)doi:10.3390/molecules27092786OpenAlex

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    Microalgae have evolved into a promising sustainable source of a wide range of compounds, including protein, carbohydrates, biomass, vitamins, animal feed, and cosmetic products. The process of extraction of intracellular composites in the microalgae industry is largely determined by the microalgal species, cultivation methods, cell wall disruption techniques, and extraction strategies. Various techniques have been applied to disrupt the cell wall and recover the intracellular molecules from microalgae, including non-mechanical, mechanical, and combined methods. A comprehensive understanding of the cell disruption processes in each method is essential to improve the efficiency of current technologies and further development of new methods in this field. In this review, an overview of microalgal cell disruption techniques and an analysis of their performance and challenges are provided. A number of studies on cell disruption and microalgae extraction are examined in order to highlight the key challenges facing the field of microalgae and their future prospects. In addition, the…

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    Cranberry: Chemical Composition, Antioxidant Activity and Impact on Human Health: Overview

    Boris V. Nemzer, Fadwa Al-Taher, Alexander Ya Yashin, Igor A. Revelsky, Yakov I. Yashin

    165 citationsOpen access (CC-BY)doi:10.3390/molecules27051503OpenAlex

    Show abstract

    Cranberries are a rich source of bioactive compounds that comprise a healthy diet. Cranberry is abundant in nutritional components and many bioactive compounds that have antioxidant properties. Both American (Vaccinium macrocarpon) and European (Vaccinium oxycoccus) cranberry species are rich in polyphenols such as phenolic acids, anthocyanins and flavonoids, and is one of the few fruits that is high in proanthocyanidins, which is linked to many health benefits. The review systematizes information on the chemical composition of cranberry, its antioxidant effect, and the beneficial impact on human health and disease prevention after cranberry consumption, and in particular, its effect against urinary tract inflammation with both adults and children, cardiovascular, oncology diseases, type 2 diabetes, metabolic syndrome, obesity, tooth decay and periodontitis, Helicobacter pylori bacteria in the stomach and other diseases. Additional research needs to study cranberry proteomics profiling, polyphenols interaction and synergism with other biologically active compounds from natural…

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    Natural Antioxidant Evaluation: A Review of Detection Methods

    Jenifer da Silva Mendonça, Rita de Cássia Avellaneda Guimarães, Verônica Assalin Zorgetto-Pinheiro, Carolina Di Pietro Fernandes, Gabriela Marcelino and 6 more

    164 citationsOpen access (CC-BY)doi:10.3390/molecules27113563OpenAlex

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    Antioxidants have drawn the attention of the scientific community due to being related to the prevention of various degenerative diseases. The antioxidant capacity has been extensively studied in vitro, and different methods have been used to assess its activity. However, the main issues related to studying natural antioxidants are evaluating whether these antioxidants demonstrate a key role in the biological system and assessing their bioavailability in the organism. The majority of outcomes in the literature are controversial due to a lack of method standardization and their proper application. Therefore, this study aims to compile the main issues concerning the natural antioxidant field of study, comparing the most common in vitro methods to evaluate the antioxidant activity of natural compounds, demonstrating the antioxidant activity in biological systems and the role of the main antioxidant enzymes of redox cellular signaling and explaining how the bioavailability of bioactive compounds is evaluated in animal models and human clinical trials.

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    Recent Progress in Organic Solar Cells: A Review on Materials from Acceptor to Donor

    Yang Li, Wei Huang, Dejiang Zhao, Lu Wang, Zhiqiang Jiao and 4 more

    163 citationsOpen access (CC-BY)doi:10.3390/molecules27061800OpenAlex

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    In the last few decades, organic solar cells (OSCs) have drawn broad interest owing to their advantages such as being low cost, flexible, semitransparent, non-toxic, and ideal for roll-to-roll large-scale processing. Significant advances have been made in the field of OSCs containing high-performance active layer materials, electrodes, and interlayers, as well as novel device structures. Particularly, the innovation of active layer materials, including novel acceptors and donors, has contributed significantly to the power conversion efficiency (PCE) improvement in OSCs. In this review, high-performance acceptors, containing fullerene derivatives, small molecular, and polymeric non-fullerene acceptors (NFAs), are discussed in detail. Meanwhile, highly efficient donor materials designed for fullerene- and NFA-based OSCs are also presented. Additionally, motivated by the incessant developments of donor and acceptor materials, recent advances in the field of ternary and tandem OSCs are reviewed as well.

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    Polydatin: Pharmacological Mechanisms, Therapeutic Targets, Biological Activities, and Health Benefits

    Ahmad Karami, Sajad Fakhri, Leila Kooshki, Haroon Zaman Khan

    161 citationsOpen access (CC-BY)doi:10.3390/molecules27196474OpenAlex

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    Polydatin is a natural potent stilbenoid polyphenol and a resveratrol derivative with improved bioavailability. Polydatin possesses potential biological activities predominantly through the modulation of pivotal signaling pathways involved in inflammation, oxidative stress, and apoptosis. Various imperative biological activities have been suggested for polydatin towards promising therapeutic effects, including anticancer, cardioprotective, anti-diabetic, gastroprotective, hepatoprotective, neuroprotective, anti-microbial, as well as health-promoting roles on the renal system, the respiratory system, rheumatoid diseases, the skeletal system, and women's health. In the present study, the therapeutic targets, biological activities, pharmacological mechanisms, and health benefits of polydatin are reviewed to provide new insights to researchers. The need to develop further clinical trials and novel delivery systems of polydatin is also considered to reveal new insights to researchers.

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    Insights on Chemical Crosslinking Strategies for Proteins

    Brindha Jayachandran, Thansila Parvin N, Mohammed Mujahid Alam, Kaushik Chanda, M. M. Balamurali

    160 citationsOpen access (CC-BY)doi:10.3390/molecules27238124OpenAlex

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    Crosslinking of proteins has gained immense significance in the fabrication of biomaterials for various health care applications. Various novel chemical-based strategies are being continuously developed for intra-/inter-molecular crosslinking of proteins to create a network/matrix with desired mechanical/functional properties without imparting toxicity to the host system. Many materials that are used in biomedical and food packaging industries are prepared by chemical means of crosslinking the proteins, besides the physical or enzymatic means of crosslinking. Such chemical methods utilize the chemical compounds or crosslinkers available from natural sources or synthetically generated with the ability to form covalent/non-covalent bonds with proteins. Such linkages are possible with chemicals like carbodiimides/epoxides, while photo-induced novel chemical crosslinkers are also available. In this review, we have discussed different protein crosslinking strategies under chemical methods, along with the corresponding crosslinking reactions/conditions, material properties and significant…

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    Limitations of Phage Therapy and Corresponding Optimization Strategies: A Review

    Jiaxi Lin, Fangyuan Du, Miao Long, Peng Li

    160 citationsOpen access (CC-BY)doi:10.3390/molecules27061857OpenAlex

    Show abstract

    Bacterial infectious diseases cause serious harm to human health. At present, antibiotics are the main drugs used in the treatment of bacterial infectious diseases, but the abuse of antibiotics has led to the rapid increase in drug-resistant bacteria and to the inability to effectively control infections. Bacteriophages are a kind of virus that infects bacteria and archaea, adopting bacteria as their hosts. The use of bacteriophages as antimicrobial agents in the treatment of bacterial diseases is an alternative to antibiotics. At present, phage therapy (PT) has been used in various fields and has provided a new technology for addressing diseases caused by bacterial infections in humans, animals, and plants. PT uses bacteriophages to infect pathogenic bacteria so to stop bacterial infections and treat and prevent related diseases. However, PT has several limitations, due to a narrow host range, the lysogenic phenomenon, the lack of relevant policies, and the lack of pharmacokinetic data. The development of reasonable strategies to overcome these limitations is essential for the…

  81. 81
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    New Halogen-Containing Drugs Approved by FDA in 2021: An Overview on Their Syntheses and Pharmaceutical Use

    Davide Benedetto Tiz, Luana Bagnoli, Ornelio Rosati, Francesca Marini, Luca Sancineto and 1 more

    160 citationsOpen access (CC-BY)doi:10.3390/molecules27051643OpenAlex

    Show abstract

    This review describes the recent Food and Drug Administration (FDA)-approved drugs (in the year 2021) containing at least one halogen atom (covalently bound). The structures proposed throughout this work are grouped according to their therapeutical use. Their synthesis is presented as well. The number of halogenated molecules that are reaching the market is regularly preserved, and 14 of the 50 molecules approved by the FDA in the last year contain halogens. This underlines the emergent role of halogens and, in particular, of fluorine and chlorine in the preparation of drugs for the treatment of several diseases such as viral infections, several types of cancer, cardiovascular disease, multiple sclerosis, migraine and inflammatory diseases such as vasculitis.

  82. 82
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    The Hydrophobic Effects: Our Current Understanding

    Qiang Sun

    158 citationsOpen access (CC-BY)doi:10.3390/molecules27207009OpenAlex

    Show abstract

    Hydrophobic interactions are involved in and believed to be the fundamental driving force of many chemical and biological phenomena in aqueous environments. This review focuses on our current understanding on hydrophobic effects. As a solute is embedded into water, the interface appears between solute and water, which mainly affects the structure of interfacial water (the topmost water layer at the solute/water interface). From our recent structural studies on water and air-water interface, hydration free energy is derived and utilized to investigate the origin of hydrophobic interactions. It is found that hydration free energy depends on the size of solute. With increasing the solute size, it is reasonably divided into initial and hydrophobic solvation processes, and various dissolved behaviors of the solutes are expected in different solvation processes, such as dispersed and accumulated distributions in solutions. Regarding the origin of hydrophobic effects, it is ascribed to the structural competition between the hydrogen bondings of interfacial and bulk water. This can be…

  83. 83
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    Biological Synthesis of Silver Nanoparticles and Prospects in Plant Disease Management

    Moh Tariq, Khan Nazima Mohammad, Bilal Ahmed, Mansoor A. Siddiqui, Jintae Lee

    158 citationsOpen access (CC-BY)doi:10.3390/molecules27154754OpenAlex

    Show abstract

    Exploration of nanoparticles (NPs) for various biological and environmental applications has become one of the most important attributes of nanotechnology. Due to remarkable physicochemical properties, silver nanoparticles (AgNPs) are the most explored and used NPs in wide-ranging applications. Also, they have proven to be of high commercial use since they possess great chemical stability, conductivity, catalytic activity, and antimicrobial potential. Though several methods including chemical and physical methods have been devised, biological approaches using organisms such as bacteria, fungi, and plants have emerged as economical, safe, and effective alternatives for the biosynthesis of AgNPs. Recent studies highlight the potential of AgNPs in modern agricultural practices to control the growth and spread of infectious pathogenic microorganisms since the introduction of AgNPs effectively reduces plant diseases caused by a spectrum of bacteria and fungi. In this review, we highlight the biosynthesis of AgNPs and discuss their applications in plant disease management with recent…

  84. 84
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    The Multifunctional Role of Herbal Products in the Management of Diabetes and Obesity: A Comprehensive Review

    Md. Mominur Rahman, Md. Rezaul Islam, Sheikh Shohag, Md. Emon Hossain, Md. Saidur Rahaman and 8 more

    158 citationsOpen access (CC-BY)doi:10.3390/molecules27051713OpenAlex

    Show abstract

    Obesity and diabetes are the most demanding health problems today, and their prevalence, as well as comorbidities, is on the rise all over the world. As time goes on, both are becoming big issues that have a big impact on people's lives. Diabetes is a metabolic and endocrine illness set apart by hyperglycemia and glucose narrow-mindedness because of insulin opposition. Heftiness is a typical, complex, and developing overall wellbeing worry that has for quite some time been connected to significant medical issues in individuals, all things considered. Because of the wide variety and low adverse effects, herbal products are an important hotspot for drug development. Synthetic compounds are not structurally diverse and lack drug-likeness properties. Thus, it is basic to keep on exploring herbal products as possible wellsprings of novel drugs. We conducted this review of the literature by searching Scopus, Science Direct, Elsevier, PubMed, and Web of Science databases. From 1990 until October 2021, research reports, review articles, and original research articles in English are…

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    Effect of Heavy Metal Stress on Phenolic Compounds Accumulation in Winter Wheat Plants

    Marta Jańczak-Pieniążek, Jan Cichoński, Patrycja Michalik, Grzegorz Chrzanowski

    156 citationsOpen access (CC-BY)doi:10.3390/molecules28010241OpenAlex

    Show abstract

    Heavy metal stress can lead to many adverse effects that inhibit cellular processes at various levels of metabolism, causing a decrease in plant productivity. In response to environmental stressors, phenolic compounds fulfill significant molecular and biochemical functions in plants. Increasing the biosynthesis of phenolic compounds in plants subjected to heavy metal stress helps protect plants from oxidative stress. A pot experiment was carried out to determine the effect of the accumulation of copper (Cu) and lead (Pb) salts at concentrations of 200, 500, and 1000 ppm on seed germination, the activity of enzymes in the phenylalanine ammonia-lyase pathway (PAL) and tyrosine ammonia-lyase (TAL), along with the total phenol and flavonoid contents in seedlings of hybrid Triticum aestivum L. (winter wheat) cultivars. The accumulation of heavy metals, especially Cu, had a negative impact on the seed germination process. The cultivar “Hyacinth” reacted most strongly to heavy metal stress, which was confirmed by obtaining the lowest values of the germination parameters. Heavy metal stress…

  86. 86
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    Coffee Chlorogenic Acids Incorporation for Bioactivity Enhancement of Foods: A Review

    Alexis Rojas-González, Claudia Yuritzi Figueroa-Hernández, Óscar González-Ríos, Mirna Leonor Suárez-Quiroz, Rosa María González‐Amaro and 2 more

    156 citationsOpen access (CC-BY)doi:10.3390/molecules27113400OpenAlex

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    The demand of foods with high antioxidant capacity have increased and research on these foods continues to grow. This review is focused on chlorogenic acids (CGAs) from green coffee, which is the most abundant source. The main CGA in coffee is 5-O-caffeoylquinic acid (5-CQA). Coffee extracts are currently the most widely used source to enhance the antioxidant activity of foods. Due to the solubility of CGAs, their extraction is mainly performed with organic solvents. CGAs have been associated with health benefits, such as antioxidant, antiviral, antibacterial, anticancer, and anti-inflammatory activity, and others that reduce the risk of cardiovascular diseases, type 2 diabetes, and Alzheimer's disease. However, the biological activities depend on the stability of CGAs, which are sensitive to pH, temperature, and light. The anti-inflammatory activity of 5-CQA is attributed to reducing the proinflammatory activity of cytokines. 5-CQA can negatively affect colon microbiota. An increase in anthocyanins and antioxidant activity was observed when CGAs extracts were added to different…

  87. 87
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    Indole-Containing Natural Products 2019–2022: Isolations, Reappraisals, Syntheses, and Biological Activities

    Syed Muhammad Umer, Mehwish Solangi, Khalid Mohammed Khan, Rahman Shah Zaib Saleem

    154 citationsOpen access (CC-BY)doi:10.3390/molecules27217586OpenAlex

    Show abstract

    Indole alkaloids represent a large subset of natural products, with more than 4100 known compounds. The majority of these alkaloids are biologically active, with some exhibiting excellent antitumor, antibacterial, antiviral, antifungal, and antiplasmodial activities. Consequently, the natural products of this class have attracted considerable attention as potential leads for novel therapeutics and are routinely isolated, characterized, and profiled to gauge their biological potential. However, data on indole alkaloids, their various structures, and bioactivities are complex due to their diverse sources, such as plants, fungi, bacteria, sponges, tunicates, and bryozoans; thus, isolation methods produce an incredible trove of information. The situation is exacerbated when synthetic derivatives, as well as their structures, bioactivities, and synthetic schemes, are considered. Thus, to make such data comprehensive and inform researchers about the current field's state, this review summarizes recent reports on novel indole alkaloids. It deals with the isolation and characterization of…

  88. 88
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    Anticancer, Cardio-Protective and Anti-Inflammatory Potential of Natural-Sources-Derived Phenolic Acids

    Afnan, Ammara Saleem, Muhammad Furqan Akhtar, Ali Sharif, Bushra Akhtar and 4 more

    154 citationsOpen access (CC-BY)doi:10.3390/molecules27217286OpenAlex

    Show abstract

    L. Their biosynthesis, physical and chemical characteristics and structure-activity relationship are well understood. These phytochemicals and their derivatives exert several bioactivities including but not limited to anticancer, cardioprotective, anti-inflammatory, immune-regulatory and anti-obesity properties. They are strong antioxidants because of hydroxyl groups which play pivotal role in their anticancer, anti-inflammatory and cardioprotective potential. They may play significant role in improving human health owing to anticarcinogenic, anti-arthritis, antihypertensive, anti-stroke, and anti-atherosclerosis activities, as several PAs have demonstrated biological activities against these disease during in vitro and in vivo studies. These PAs exhibited anticancer action by promoting apoptosis, targeting angiogenesis, and reducing abnormal cell growth, while anti-inflammatory activity was attributed to reducing proinflammatory cytokines. Pas exhibited anti-atherosclerotic activity via inhibition of platelets. Moreover, they also reduced cardiovascular complications such as…

  89. 89
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    Protective, Biostimulating, and Eliciting Effects of Chitosan and Its Derivatives on Crop Plants

    Maria Stasińska-Jakubas, Barbara Hawrylak-Nowak

    151 citationsOpen access (CC-BY)doi:10.3390/molecules27092801OpenAlex

    Show abstract

    Chitosan is a biodegradable and biocompatible polysaccharide obtained by partial deacetylation of chitin. This polymer has been gaining increasing popularity due to its natural origin, favorable physicochemical properties, and multidirectional bioactivity. In agriculture, the greatest hopes are raised by the possibility of using chitosan as a biostimulant, a plant protection product, an elicitor, or an agent to increase the storage stability of plant raw materials. The most important properties of chitosan include induction of plant defense mechanisms and regulation of metabolic processes. Additionally, it has antifungal, antibacterial, antiviral, and antioxidant activity. The effectiveness of chitosan interactions is determined by its origin, deacetylation degree and acetylation pattern, molecular weight, type of chemical modifications, pH, concentration, and solubility. There is a need to conduct research on alternative sources of chitosan, extraction methods, optimization of physicochemical properties, and commercial implementation of scientific progress outcomes in this field.…

  90. 90
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    Current Use of Fenton Reaction in Drugs and Food

    Chizumi Abe, Taiki Miyazawa, Teruo Miyazawa

    150 citationsOpen access (CC-BY)doi:10.3390/molecules27175451OpenAlex

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    Iron is the most abundant mineral in the human body and plays essential roles in sustaining life, such as the transport of oxygen to systemic organs. The Fenton reaction is the reaction between iron and hydrogen peroxide, generating hydroxyl radical, which is highly reactive and highly toxic to living cells. "Ferroptosis", a programmed cell death in which the Fenton reaction is closely involved, has recently received much attention. Furthermore, various applications of the Fenton reaction have been reported in the medical and nutritional fields, such as cancer treatment or sterilization. Here, this review summarizes the recent growing interest in the usefulness of iron and its biological relevance through basic and practical information of the Fenton reaction and recent reports.

  91. 91
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    Perilla frutescens: A Rich Source of Pharmacological Active Compounds

    Tianyu Hou, Vasudeva Reddy Netala, Hongjiao Zhang, Yun Xing, Huizhen Li and 1 more

    150 citationsOpen access (CC-BY)doi:10.3390/molecules27113578OpenAlex

    Show abstract

    Perilla frutescens (L.) Britton, an important pharmaceutical and nutraceutical crop, is widely cultivated in East Asian countries. In this review, we present the latest research findings on the phytochemistry and pharmacological activities of P. frutescens. Different databases, including PubMed, Scopus, CNKI, Agricola, Scifinder, Embase, ScienceDirect, DOAJ, and Web of Science, were searched to present the best review. In this review, we clearly represent the active constituents responsible for each and every pharmacological activity, plausible mechanism of action, and maximum inhibitory concentrations, as well as IC50 values. Approximately 400 different bioactive compounds, including alkaloids, terpenoids, quinines, phenylpropanoids, polyphenolic compounds, flavonoids, coumarins, anthocyanins, carotenoids, neolignans, fatty acids, polycosanols, tocopherols, and sitosterols, have been reported in the leaves, seeds, roots, and aerial parts of P. frutescens. The bioactive constituents of P. frutescens exhibited different enzyme-inhibition properties, including antihyaluronidase…

  92. 92
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    Enzymatic Oxidation of Tea Catechins and Its Mechanism

    Buhailiqiemu Abudureheman, Xiaochun Yu, Dandan Fang, Henghui Zhang

    150 citationsOpen access (CC-BY)doi:10.3390/molecules27030942OpenAlex

    Show abstract

    ) is one of the most widely consumed beverages in the world. The three major types of tea, green tea, oolong tea, and black tea, differ in terms of the manufacture and chemical composition. Catechins, theaflavins, and thearubigins have been identified as the major components in tea. Other minor oligomers have also been found in tea. Different kinds of ring fission and formation elucidate the major transformed pathways of tea catechins to their dimers and polymers. The present review summarizes the data concerning the enzymatic oxidation of catechins, their dimers, and thearubigins in tea.

  93. 93
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    The Roles and Associated Mechanisms of Adipokines in Development of Metabolic Syndrome

    Ji Eun Kim, Jin‐Sun Kim, Min-Jee Jo, Eun‐Jung Cho, Shin-Young Ahn and 2 more

    148 citationsOpen access (CC-BY)doi:10.3390/molecules27020334OpenAlex

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    Metabolic syndrome is a cluster of metabolic indicators that increase the risk of diabetes and cardiovascular diseases. Visceral obesity and factors derived from altered adipose tissue, adipokines, play critical roles in the development of metabolic syndrome. Although the adipokines leptin and adiponectin improve insulin sensitivity, others contribute to the development of glucose intolerance, including visfatin, fetuin-A, resistin, and plasminogen activator inhibitor-1 (PAI-1). Leptin and adiponectin increase fatty acid oxidation, prevent foam cell formation, and improve lipid metabolism, while visfatin, fetuin-A, PAI-1, and resistin have pro-atherogenic properties. In this review, we briefly summarize the role of various adipokines in the development of metabolic syndrome, focusing on glucose homeostasis and lipid metabolism.

  94. 94
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    Evaluation of Biological Activity of Natural Compounds: Current Trends and Methods

    Carlos Barba‐Ostria, Saskya E. Carrera-Pacheco, Rebeca González‐Pastor, Jorge Heredia‐Moya, Arianna Mayorga-Ramos and 4 more

    147 citationsOpen access (CC-BY)doi:10.3390/molecules27144490OpenAlex

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    Natural compounds have diverse structures and are present in different forms of life. Metabolites such as tannins, anthocyanins, and alkaloids, among others, serve as a defense mechanism in live organisms and are undoubtedly compounds of interest for the food, cosmetic, and pharmaceutical industries. Plants, bacteria, and insects represent sources of biomolecules with diverse activities, which are in many cases poorly studied. To use these molecules for different applications, it is essential to know their structure, concentrations, and biological activity potential. In vitro techniques that evaluate the biological activity of the molecules of interest have been developed since the 1950s. Currently, different methodologies have emerged to overcome some of the limitations of these traditional techniques, mainly via reductions in time and costs. These emerging technologies continue to appear due to the urgent need to expand the analysis capacity of a growing number of reported biomolecules. This review presents an updated summary of the conventional and relevant methods to evaluate…

  95. 95
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    Boron Chemicals in Drug Discovery and Development: Synthesis and Medicinal Perspective

    Bhaskar C. Das, Nitesh Kumar Nandwana, Sasmita Das, Varsha Nandwana, Mohd Adil Shareef and 6 more

    147 citationsOpen access (CC-BY)doi:10.3390/molecules27092615OpenAlex

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    A standard goal of medicinal chemists has been to discover efficient and potent drug candidates with specific enzyme-inhibitor abilities. In this regard, boron-based bioactive compounds have provided amphiphilic properties to facilitate interaction with protein targets. Indeed, the spectrum of boron-based entities as drug candidates against many diseases has grown tremendously since the first clinically tested boron-based drug, Velcade. In this review, we collectively represent the current boron-containing drug candidates, boron-containing retinoids, benzoxaboroles, aminoboronic acid, carboranes, and BODIPY, for the treatment of different human diseases.In addition, we also describe the synthesis, key structure-activity relationship, and associated biological activities, such as antimicrobial, antituberculosis, antitumor, antiparasitic, antiprotozoal, anti-inflammatory, antifolate, antidepressant, antiallergic, anesthetic, and anti-Alzheimer's agents, as well as proteasome and lipogenic inhibitors. This compilation could be very useful in the exploration of novel boron-derived…

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    Pharmacological Activities of Soursop (Annona muricata Lin.)

    Mutakin Mutakin, Rizky Fauziati, Fahrina Nur Fadhilah, Ade Zuhrotun, Riezki Amalia and 1 more

    147 citationsOpen access (CC-BY)doi:10.3390/molecules27041201OpenAlex

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    Soursop (Annona muricata Lin.) is a plant belonging to the Annonaceae family that has been widely used globally as a traditional medicine for many diseases. In this review, we discuss the traditional use, chemical content, and pharmacological activities of A.muricata. From 49 research articles that were obtained from 1981 to 2021, A.muricata’s activities were shown to include anticancer (25%), antiulcer (17%), antidiabetic (14%), antiprotozoal (10%), antidiarrhea (8%), antibacterial (8%), antiviral (8%), antihypertensive (6%), and wound healing (4%). Several biological activities and the general mechanisms underlying the effects of A.muricata have been tested both in vitro and in vivo. A.muricata contains chemicals such as acetogenins (annomuricins and annonacin), alkaloids (coreximine and reticuline), flavonoids (quercetin), and vitamins, which are predicted to be responsible for the biological activity of A.muricata.

  97. 97
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    Overview of Research into mTOR Inhibitors

    Beibei Mao, Qi Zhang, Li Ma, Dongsheng Zhao, Pan Zhao and 1 more

    146 citationsOpen access (CC-BY)doi:10.3390/molecules27165295OpenAlex

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    The mammalian target of rapamycin (mTOR) is a serine/threonine kinase that belongs to the phosphoinositide 3-kinase (PI3K)-related kinase (PIKK) family. The kinase exists in the forms of two complexes, mTORC1 and mTORC2, and it participates in cell growth, proliferation, metabolism, and survival. The kinase activity is closely related to the occurrence and development of multiple human diseases. Inhibitors of mTOR block critical pathways to produce antiviral, anti-inflammatory, antiproliferative and other effects, and they have been applied to research in cancer, inflammation, central nervous system diseases and viral infections. Existing mTOR inhibitors are commonly divided into mTOR allosteric inhibitors, ATP-competitive inhibitors and dual binding site inhibitors, according to their sites of action. In addition, there exist several dual-target mTOR inhibitors that target PI3K, histone deacetylases (HDAC) or ataxia telangiectasia mutated and Rad-3 related (ATR) kinases. This review focuses on the structure of mTOR protein and related signaling pathways as well as the structure and…

  98. 98
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    FTIR as a Method for Qualitative Assessment of Solid Samples in Geochemical Research: A Review

    Yana Tkachenko, Przemysław Niedzielski

    145 citationsOpen access (CC-BY)doi:10.3390/molecules27248846OpenAlex

    Show abstract

    This study aims to collect information about soil investigation by FTIR. As we know, the FTIR technique is most often used in organic and bioorganic chemistry, while in geochemistry FTIR spectroscopy is not used very often. Therefore, there is a problem with the identification and interpretation of the IR spectra of minerals contained in sediments and soils. The reason for this is a deficiency of data about characteristic wavenumbers for minerals. Therefore, this study reviews and sums up, in one place, published articles that are connected to an investigation of minerals from 2002 to 2021 (based on the Scopus database). Additionally, the present review highlights various analytical techniques (ATR-FTIR, DRIFT, 2D-IR, and SR-FTIR) and discusses some of them for geochemical study. Additionally, the study describes helpful tools in the data pre-processing of IR spectra (normalization, baseline correction, and spectral derivatives).

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    A Comprehensive Review on the Benefits and Problems of Curcumin with Respect to Human Health

    Siyu Liu, Jie Liu, Lan He, Liu Liu, Bo Hao Cheng and 3 more

    144 citationsOpen access (CC-BY)doi:10.3390/molecules27144400OpenAlex

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    Curcumin is the most important active component in turmeric extracts. Curcumin, a natural monomer from plants has received a considerable attention as a dietary supplement, exhibiting evident activity in a wide range of human pathological conditions. In general, curcumin is beneficial to human health, demonstrating pharmacological activities of anti-inflammation and antioxidation, as well as antitumor and immune regulation activities. Curcumin also presents therapeutic potential in neurodegenerative, cardiovascular and cerebrovascular diseases. In this review article, we summarize the advancements made in recent years with respect to curcumin as a biologically active agent in malignant tumors, Alzheimer's disease (AD), hematological diseases and viral infectious diseases. We also focus on problems associated with curcumin from basic research to clinical translation, such as its low solubility, leading to poor bioavailability, as well as the controversy surrounding the association between curcumin purity and effect. Through a review and summary of the clinical research on curcumin…

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    Recent Advances in Natural Polyphenol Research

    Irene Dini, Lucia Grumetto

    143 citationsOpen access (CC-BY)doi:10.3390/molecules27248777OpenAlex

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    Polyphenols are secondary metabolites produced by plants, which contribute to the plant's defense against abiotic stress conditions (e.g., UV radiation and precipitation), the aggression of herbivores, and plant pathogens. Epidemiological studies suggest that long-term consumption of plant polyphenols protects against cardiovascular disease, cancer, osteoporosis, diabetes, and neurodegenerative diseases. Their structural diversity has fascinated and confronted analytical chemists on how to carry out unambiguous identification, exhaustive recovery from plants and organic waste, and define their nutritional and biological potential. The food, cosmetic, and pharmaceutical industries employ polyphenols from fruits and vegetables to produce additives, additional foods, and supplements. In some cases, nanocarriers have been used to protect polyphenols during food processing, to solve the issues related to low water solubility, to transport them to the site of action, and improve their bioavailability. This review summarizes the structure-bioactivity relationships, processing parameters…

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The cohort is every article, review and book chapter OpenAlex attributes to Molecules with publication year 2022, excluding retracted works and paratext such as editorials and errata. The top 100 by citation count are listed; the percentile is the rank divided by the cohort size. 100 of the 100 entries have an abstract in OpenAlex. Counts were read on 29 October 2026 and will not be updated on this page, so a quoted rank stays verifiable. Full rules on the methodology page.

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