Most-cited articles · 2021
The 100 most-cited articles in Molecules, 2021
Ranked by OpenAlex citation count on 29 October 2026, out of 7,718 eligible articles Molecules published in 2021. Ranks are frozen; this page will not change. Number one, with 1,745 citations: Controlled Drug Delivery Systems: Current Status and Future Directions.
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The most-cited articles from Molecules in 2021 cluster around natural products and their biological activities, drug delivery, and antimicrobial research. Plant flavonoids, phenolic compounds, resveratrol, essential oils, and plant alkaloids feature prominently, alongside reviews of controlled drug delivery systems and antibiotic resistance. The top paper, "Controlled Drug Delivery Systems: Current Status and Future Directions" by Adepu and Ramakrishna, leads with 1,745 citations, followed by "Plant Flavonoids: Chemical Characteristics and Biological Activity" with 1,522 citations.
Readers can use this list to identify the topics and review articles that attracted the most attention in 2021, spanning natural product chemistry, pharmaceutical science, and related health research. Citation counts reflect the extent to which later publications drew on these works, offering one indication of influence within the scholarly literature.
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Controlled Drug Delivery Systems: Current Status and Future Directions
Shivakalyani Adepu, Seeram Ramakrishna
1,745 citationsOpen access (CC-BY)doi:10.3390/molecules26195905OpenAlex
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The drug delivery system enables the release of the active pharmaceutical ingredient to achieve a desired therapeutic response. Conventional drug delivery systems (tablets, capsules, syrups, ointments, etc.) suffer from poor bioavailability and fluctuations in plasma drug level and are unable to achieve sustained release. Without an efficient delivery mechanism, the whole therapeutic process can be rendered useless. Moreover, the drug has to be delivered at a specified controlled rate and at the target site as precisely as possible to achieve maximum efficacy and safety. Controlled drug delivery systems are developed to combat the problems associated with conventional drug delivery. There has been a tremendous evolution in controlled drug delivery systems from the past two decades ranging from macro scale and nano scale to intelligent targeted delivery. The initial part of this review provides a basic understanding of drug delivery systems with an emphasis on the pharmacokinetics of the drug. It also discusses the conventional drug delivery systems and their limitations. Further,…
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Plant Flavonoids: Chemical Characteristics and Biological Activity
Maria Celeste Dias, Diana C. G. A. Pinto, Artur M. S. Silva
1,522 citationsOpen access (CC-BY)doi:10.3390/molecules26175377OpenAlex
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In recent years, more attention has been paid to natural sources of antioxidants. Flavonoids are natural substances synthesized in several parts of plants that exhibit a high antioxidant capacity. They are a large family, presenting several classes based on their basic structure. Flavonoids have the ability to control the accumulation of reactive oxygen species (ROS) via scavenger ROS when they are formed. Therefore, these antioxidant compounds have an important role in plant stress tolerance and a high relevance in human health, mainly due to their anti-inflammatory and antimicrobial properties. In addition, flavonoids have several applications in the food industry as preservatives, pigments, and antioxidants, as well as in other industries such as cosmetics and pharmaceuticals. However, flavonoids application for industrial purposes implies extraction processes with high purity and quality. Several methodologies have been developed aimed at increasing flavonoid extraction yield and being environmentally friendly. This review presents the most abundant natural flavonoids, their…
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Role of Phenolic Compounds in Human Disease: Current Knowledge and Future Prospects
Md. Mominur Rahman, Md. Saidur Rahaman, Md. Rezaul Islam, Firoza Rahman, Faria Mannan Mithi and 9 more
860 citationsOpen access (CC-BY)doi:10.3390/molecules27010233OpenAlex
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Inflammation is a natural protective mechanism that occurs when the body's tissue homeostatic mechanisms are disrupted by biotic, physical, or chemical agents. The immune response generates pro-inflammatory mediators, but excessive output, such as chronic inflammation, contributes to many persistent diseases. Some phenolic compounds work in tandem with nonsteroidal anti-inflammatory drugs (NSAIDs) to inhibit pro-inflammatory mediators' activity or gene expression, including cyclooxygenase (COX). Various phenolic compounds can also act on transcription factors, such as nuclear factor-κB (NF-κB) or nuclear factor-erythroid factor 2-related factor 2 (Nrf-2), to up-or downregulate elements within the antioxidant response pathways. Phenolic compounds can inhibit enzymes associated with the development of human diseases and have been used to treat various common human ailments, including hypertension, metabolic problems, incendiary infections, and neurodegenerative diseases. The inhibition of the angiotensin-converting enzyme (ACE) by phenolic compounds has been used to treat…
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Anti-Inflammatory Action and Mechanisms of Resveratrol
Tiantian Meng, Dingfu Xiao, Arowolo Muhammed, Juying Deng, Liang Chen and 1 more
706 citationsOpen access (CC-BY)doi:10.3390/molecules26010229OpenAlex
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Resveratrol (3,4',5-trihy- droxystilbene), a natural phytoalexin polyphenol, exhibits anti-oxidant, anti-inflammatory, and anti-carcinogenic properties. This phytoalexin is well-absorbed and rapidly and extensively metabolized in the body. Inflammation is an adaptive response, which could be triggered by various danger signals, such as invasion by microorganisms or tissue injury. In this review, the anti-inflammatory activity and the mechanism of resveratrol modulates the inflammatory response are examined. Multiple experimental studies that illustrate regulatory mechanisms and the immunomodulatory function of resveratrol both in vivo and in vitro. The data acquired from those studies are discussed.
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Essential Oils as Natural Sources of Fragrance Compounds for Cosmetics and Cosmeceuticals
Sharmeen Jugreet, Mohamad Fawzi Mahomoodally, Gökhan Zengin, Filippo Maggi
663 citationsOpen access (CC-BY)doi:10.3390/molecules26030666OpenAlex
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Fragrance is an integral part of cosmetic products and is often regarded as an overriding factor in the selection of cosmetics among consumers. Fragrances also play a considerable role in masking undesirable smells arising from fatty acids, oils and surfactants that are commonly used in cosmetic formulations. Essential oils are vital assets in the cosmetic industry, as along with imparting pleasant aromas in different products, they are able to act as preservatives and active agents and, simultaneously, offer various benefits to the skin. Moreover, the stimulating demand for natural ingredients has contributed massively to a renewed interest in cosmetic and wellness industries in plant derivatives, especially essential oils. This has led popular cosmetic companies to endorse natural fragrances and opt for minimally processed natural ingredients, given the potentially adverse health risks associated with artificial fragrance chemicals, which are major elements of cosmetics. Among the high-valued essential oils used as fragrances are citrus, lavender, eucalyptus, tea tree and other…
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Bone Grafts and Substitutes in Dentistry: A Review of Current Trends and Developments
Rusin Zhao, Ruijia Yang, Paul R. Cooper, Zohaib Khurshid, Amin Shavandi and 1 more
645 citationsOpen access (CC-BY)doi:10.3390/molecules26103007OpenAlex
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After tooth loss, bone resorption is irreversible, leaving the area without adequate bone volume for successful implant treatment. Bone grafting is the only solution to reverse dental bone loss and is a well-accepted procedure required in one in every four dental implants. Research and development in materials, design and fabrication technologies have expanded over the years to achieve successful and long-lasting dental implants for tooth substitution. This review will critically present the various dental bone graft and substitute materials that have been used to achieve a successful dental implant. The article also reviews the properties of dental bone grafts and various dental bone substitutes that have been studied or are currently available commercially. The various classifications of bone grafts and substitutes, including natural and synthetic materials, are critically presented, and available commercial products in each category are discussed. Different bone substitute materials, including metals, ceramics, polymers, or their combinations, and their chemical, physical, and…
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Antimicrobial Properties of Chitosan and Chitosan Derivatives in the Treatment of Enteric Infections
Dazhong Yan, Yanzhen Li, Yinling Liu, Na Li, Xue Zhang and 1 more
618 citationsOpen access (CC-BY)doi:10.3390/molecules26237136OpenAlex
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Antibiotics played an important role in controlling the development of enteric infection. However, the emergence of antibiotic resistance and gut dysbiosis led to a growing interest in the use of natural antimicrobial agents as alternatives for therapy and disinfection. Chitosan is a nontoxic natural antimicrobial polymer and is approved by GRAS (Generally Recognized as Safe by the United States Food and Drug Administration). Chitosan and chitosan derivatives can kill microbes by neutralizing negative charges on the microbial surface. Besides, chemical modifications give chitosan derivatives better water solubility and antimicrobial property. This review gives an overview of the preparation of chitosan, its derivatives, and the conjugates with other polymers and nanoparticles with better antimicrobial properties, explains the direct and indirect mechanisms of action of chitosan, and summarizes current treatment for enteric infections as well as the role of chitosan and chitosan derivatives in the antimicrobial agents in enteric infections. Finally, we suggested future directions for…
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New Antibiotics for Multidrug-Resistant Bacterial Strains: Latest Research Developments and Future Perspectives
Marco Terreni, Marina Taccani, Massimo Pregnolato
604 citationsOpen access (CC-BY)doi:10.3390/molecules26092671OpenAlex
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The present work aims to examine the worrying problem of antibiotic resistance and the emergence of multidrug-resistant bacterial strains, which have now become really common in hospitals and risk hindering the global control of infectious diseases. After a careful examination of these phenomena and multiple mechanisms that make certain bacteria resistant to specific antibiotics that were originally effective in the treatment of infections caused by the same pathogens, possible strategies to stem antibiotic resistance are analyzed. This paper, therefore, focuses on the most promising new chemical compounds in the current pipeline active against multidrug-resistant organisms that are innovative compared to traditional antibiotics: Firstly, the main antibacterial agents in clinical development (Phase III) from 2017 to 2020 are listed (with special attention on the treatment of infections caused by the pathogens Neisseria gonorrhoeae, including multidrug-resistant isolates, and Clostridium difficile), and then the paper moves on to the new agents of pharmacological interest that have…
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Heavy Metals and Human Health: Possible Exposure Pathways and the Competition for Protein Binding Sites
Danuta Witkowska, Joanna Słowik, Karolina Chilicka
603 citationsOpen access (CC-BY)doi:10.3390/molecules26196060OpenAlex
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Heavy metals enter the human body through the gastrointestinal tract, skin, or via inhalation. Toxic metals have proven to be a major threat to human health, mostly because of their ability to cause membrane and DNA damage, and to perturb protein function and enzyme activity. These metals disturb native proteins' functions by binding to free thiols or other functional groups, catalyzing the oxidation of amino acid side chains, perturbing protein folding, and/or displacing essential metal ions in enzymes. The review shows the physiological and biochemical effects of selected toxic metals interactions with proteins and enzymes. As environmental contamination by heavy metals is one of the most significant global problems, some detoxification strategies are also mentioned.
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Nanoencapsulation of Promising Bioactive Compounds to Improve Their Absorption, Stability, Functionality and the Appearance of the Final Food Products
Mirian Pateiro, Belén Gómez, Paulo E. S. Munekata, Francisco J. Barba, Predrag Putnik and 2 more
603 citationsOpen access (CC-BY)doi:10.3390/molecules26061547OpenAlex
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The design of functional foods has grown recently as an answer to rising consumers' concerns and demands for natural, nutritional and healthy food products. Nanoencapsulation is a technique based on enclosing a bioactive compound (BAC) in liquid, solid or gaseous states within a matrix or inert material for preserving the coated substance (food or flavor molecules/ingredients). Nanoencapsulation can improve stability of BACs, improving the regulation of their release at physiologically active sites. Regarding materials for food and nutraceutical applications, the most used are carbohydrate-, protein- or lipid-based alternatives such as chitosan, peptide-chitosan and β-lactoglobulin nanoparticles (NPs) or emulsion biopolymer complexes. On the other hand, the main BACs used in foods for health promoting, including antioxidants, antimicrobials, vitamins, probiotics and prebiotics and others (minerals, enzymes and flavoring compounds). Nanotechnology can also play notable role in the development of programmable food, an original futuristic concept promising the consumers to obtain high…
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A Brief History of Colour, the Environmental Impact of Synthetic Dyes and Removal by Using Laccases
Leidy D. Ardila-Leal, Raúl A. Poutou‐Piñales, Aura M. Pedroza-Rodríguez, Balkys E. Quevedo-Hidalgo
543 citationsOpen access (CC-BY)doi:10.3390/molecules26133813OpenAlex
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The history of colour is fascinating from a social and artistic viewpoint because it shows the way; use; and importance acquired. The use of colours date back to the Stone Age (the first news of cave paintings); colour has contributed to the social and symbolic development of civilizations. Colour has been associated with hierarchy; power and leadership in some of them. The advent of synthetic dyes has revolutionized the colour industry; and due to their low cost; their use has spread to different industrial sectors. Although the percentage of coloured wastewater discharged by the textile; food; pharmaceutical; cosmetic; and paper industries; among other productive areas; are unknown; the toxic effect and ecological implications of this discharged into water bodies are harmful. This review briefly shows the social and artistic history surrounding the discovery and use of natural and synthetic dyes. We summarise the environmental impact caused by the discharge of untreated or poorly treated coloured wastewater to water bodies; which has led to physical; chemical and biological…
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Probiotics Regulate Gut Microbiota: An Effective Method to Improve Immunity
Wang Xinzhou, Peng Zhang, Xin Zhang
527 citationsOpen access (CC-BY)doi:10.3390/molecules26196076OpenAlex
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Probiotics are beneficial active microorganisms that colonize the human intestines and change the composition of the flora in particular parts of the host. Recently, the use of probiotics to regulate intestinal flora to improve host immunity has received widespread attention. Recent evidence has shown that probiotics play significant roles in gut microbiota composition, which can inhibit the colonization of pathogenic bacteria in the intestine, help the host build a healthy intestinal mucosa protective layer, and enhance the host immune system. Based on the close relationship between the gut microbiota and human immunity, it has become an extremely effective way to improve human immunity by regulating the gut microbiome with probiotics. In this review, we discussed the influence of probiotics on the gut microbiota and human immunity, and the relationship between immunity, probiotics, gut microbiota, and life quality. We further emphasized the regulation of gut microflora through probiotics, thereby enhancing human immunity and improving people's lives.
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Plant-Derived Anticancer Compounds as New Perspectives in Drug Discovery and Alternative Therapy
Cristina Adriana Dehelean, Iasmina Marcovici, Codruţa Şoica, Marius Mioc, Dorina Elena Coricovac and 3 more
508 citationsOpen access (CC-BY)doi:10.3390/molecules26041109OpenAlex
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Despite the recent advances in the field of chemically synthetized pharmaceutical agents, nature remains the main supplier of bioactive molecules. The research of natural products is a valuable approach for the discovery and development of novel biologically active compounds possessing unique structures and mechanisms of action. Although their use belongs to the traditional treatment regimes, plant-derived compounds still cover a large portion of the current-day pharmaceutical agents. Their medical importance is well recognized in the field of oncology, especially as an alternative to the limitations of conventional chemotherapy (severe side effects and inefficacy due to the occurrence of multi-drug resistance). This review offers a comprehensive perspective of the first blockbuster chemotherapeutic agents of natural origin's (e.g. taxol, vincristine, doxorubicin) mechanism of action using 3D representation. In addition is portrayed the step-by-step evolution from preclinical to clinical evaluation of the most recently studied natural compounds with potent antitumor activity (e.g.…
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Diversity in Chemical Structures and Biological Properties of Plant Alkaloids
Sweta Bhambhani, Kirtikumar Ramesh Kondhare, Ashok Prabhakar Giri
503 citationsOpen access (CC-BY)doi:10.3390/molecules26113374OpenAlex
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Phytochemicals belonging to the group of alkaloids are signature specialized metabolites endowed with countless biological activities. Plants are armored with these naturally produced nitrogenous compounds to combat numerous challenging environmental stress conditions. Traditional and modern healthcare systems have harnessed the potential of these organic compounds for the treatment of many ailments. Various chemical entities (functional groups) attached to the central moiety are responsible for their diverse range of biological properties. The development of the characterization of these plant metabolites and the enzymes involved in their biosynthesis is of an utmost priority to deliver enhanced advantages in terms of biological properties and productivity. Further, the incorporation of whole/partial metabolic pathways in the heterologous system and/or the overexpression of biosynthetic steps in homologous systems have both become alternative and lucrative methods over chemical synthesis in recent times. Moreover, in-depth research on alkaloid biosynthetic pathways has revealed…
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Factors Affecting Synthetic Dye Adsorption; Desorption Studies: A Review of Results from the Last Five Years (2017–2021)
Eszter Rápó, Szende Tonk
493 citationsOpen access (CC-BY)doi:10.3390/molecules26175419OpenAlex
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The primary, most obvious parameter indicating water quality is the color of the water. Not only can it be aesthetically disturbing, but it can also be an indicator of contamination. Clean, high-quality water is a valuable, essential asset. Of the available technologies for removing dyes, adsorption is the most used method due to its ease of use, cost-effectiveness, and high efficiency. The adsorption process is influenced by several parameters, which are the basis of all laboratories researching the optimum conditions. The main objective of this review is to provide up-to-date information on the most studied influencing factors. The effects of initial dye concentration, pH, adsorbent dosage, particle size and temperature are illustrated through examples from the last five years (2017-2021) of research. Moreover, general trends are drawn based on these findings. The removal time ranged from 5 min to 36 h (E = 100% was achieved within 5-60 min). In addition, nearly 80% efficiency can be achieved with just 0.05 g of adsorbent. It is important to reduce adsorbent particle size (with Φ…
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Plant-Derived Pesticides as an Alternative to Pest Management and Sustainable Agricultural Production: Prospects, Applications and Challenges
Augusto Lopes Souto, Muriel Sylvestre, Elisabeth Dantas Tölke, Josean Fechine Tavares, José Maria Barbosa‐Filho and 1 more
463 citationsOpen access (CC-BY)doi:10.3390/molecules26164835OpenAlex
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Pests and diseases are responsible for most of the losses related to agricultural crops, either in the field or in storage. Moreover, due to indiscriminate use of synthetic pesticides over the years, several issues have come along, such as pest resistance and contamination of important planet sources, such as water, air and soil. Therefore, in order to improve efficiency of crop production and reduce food crisis in a sustainable manner, while preserving consumer's health, plant-derived pesticides may be a green alternative to synthetic ones. They are cheap, biodegradable, ecofriendly and act by several mechanisms of action in a more specific way, suggesting that they are less of a hazard to humans and the environment. Natural plant products with bioactivity toward insects include several classes of molecules, for example: terpenes, flavonoids, alkaloids, polyphenols, cyanogenic glucosides, quinones, amides, aldehydes, thiophenes, amino acids, saccharides and polyketides (which is not an exhaustive list of insecticidal substances). In general, those compounds have important…
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Clove Essential Oil (Syzygium aromaticum L. Myrtaceae): Extraction, Chemical Composition, Food Applications, and Essential Bioactivity for Human Health
José Nabor Haro-González, Gustavo Adolfo Castillo-Herrera, Moisés Martínez‐Velázquez, Hugo Espinosa‐Andrews
462 citationsOpen access (CC-BY)doi:10.3390/molecules26216387OpenAlex
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L. Myrtaceae) is an aromatic plant widely cultivated in tropical and subtropical countries, rich in volatile compounds and antioxidants such as eugenol, β-caryophyllene, and α-humulene. Clove essential oil has received considerable interest due to its wide application in the perfume, cosmetic, health, medical, flavoring, and food industries. Clove essential oil has biological activity relevant to human health, including antimicrobial, antioxidant, and insecticidal activity. The impacts of the extraction method (hydrodistillation, steam distillation, ultrasound-assisted extraction, microwave-assisted extraction, cold pressing, and supercritical fluid extraction) on the concentration of the main volatile compounds in clove essential oil and organic clove extracts are shown. Eugenol is the major compound, accounting for at least 50%. The remaining 10-40% consists of eugenyl acetate, β-caryophyllene, and α-humulene. The main biological activities reported are summarized. Furthermore, the main applications in clove essential oil in the food industry are presented. This review presents…
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Skin Wound Healing: Normal Macrophage Function and Macrophage Dysfunction in Diabetic Wounds
Savannah Margaret Aitcheson, Francesca D. Frentiu, Sheree E. Hurn, Katie P. Edwards, Rachael Zoe Murray
445 citationsOpen access (CC-BY)doi:10.3390/molecules26164917OpenAlex
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Macrophages play a prominent role in wound healing. In the early stages, they promote inflammation and remove pathogens, wound debris, and cells that have apoptosed. Later in the repair process, they dampen inflammation and secrete factors that regulate the proliferation, differentiation, and migration of keratinocytes, fibroblasts, and endothelial cells, leading to neovascularisation and wound closure. The macrophages that coordinate this repair process are complex: they originate from different sources and have distinct phenotypes with diverse functions that act at various times in the repair process. Macrophages in individuals with diabetes are altered, displaying hyperresponsiveness to inflammatory stimulants and increased secretion of pro-inflammatory cytokines. They also have a reduced ability to phagocytose pathogens and efferocytose cells that have undergone apoptosis. This leads to a reduced capacity to remove pathogens and, as efferocytosis is a trigger for their phenotypic switch, it reduces the number of M2 reparative macrophages in the wound. This can lead to diabetic…
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A Global Review on Short Peptides: Frontiers and Perspectives
Vasso Apostolopoulos, Joanna Bojarska, Tsun‐Thai Chai, Sherif M. Elnagdy, Krzysztof Kaczmarek and 20 more
431 citationsOpen access (CC-BY)doi:10.3390/molecules26020430OpenAlex
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Peptides are fragments of proteins that carry out biological functions. They act as signaling entities via all domains of life and interfere with protein-protein interactions, which are indispensable in bio-processes. Short peptides include fundamental molecular information for a prelude to the symphony of life. They have aroused considerable interest due to their unique features and great promise in innovative bio-therapies. This work focusing on the current state-of-the-art short peptide-based therapeutical developments is the first global review written by researchers from all continents, as a celebration of 100 years of peptide therapeutics since the commencement of insulin therapy in the 1920s. Peptide "drugs" initially played only the role of hormone analogs to balance disorders. Nowadays, they achieve numerous biomedical tasks, can cross membranes, or reach intracellular targets. The role of peptides in bio-processes can hardly be mimicked by other chemical substances. The article is divided into independent sections, which are related to either the progress in short…
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Characteristics of the Proteolytic Enzymes Produced by Lactic Acid Bacteria
Marek Kieliszek, Katarzyna Pobiega, Kamil Piwowarek, Anna Maria Kot
429 citationsOpen access (CC-BY)doi:10.3390/molecules26071858OpenAlex
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Over the past several decades, we have observed a very rapid development in the biotechnological use of lactic acid bacteria (LAB) in various branches of the food industry. All such areas of activity of these bacteria are very important and promise enormous economic and industrial successes. LAB are a numerous group of microorganisms that have the ability to ferment sugars into lactic acid and to produce proteolytic enzymes. LAB proteolytic enzymes play an important role in supplying cells with the nitrogen compounds necessary for their growth. Their nutritional requirements in this regard are very high. Lactic acid bacteria require many free amino acids to grow. The available amount of such compounds in the natural environment is usually small, hence the main function of these enzymes is the hydrolysis of proteins to components absorbed by bacterial cells. Enzymes are synthesized inside bacterial cells and are mostly secreted outside the cell. This type of proteinase remains linked to the cell wall structure by covalent bonds. Thanks to advances in enzymology, it is possible to…
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Nanotechnology in Wastewater Management: A New Paradigm Towards Wastewater Treatment
Keerti Jain, Anand Singh Patel, Vishwas P. Pardhi, Swaran J.S. Flora
429 citationsOpen access (CC-BY)doi:10.3390/molecules26061797OpenAlex
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Clean and safe water is a fundamental human need for multi-faceted development of society and a thriving economy. Brisk rises in populations, expanding industrialization, urbanization and extensive agriculture practices have resulted in the generation of wastewater which have not only made the water dirty or polluted, but also deadly. Millions of people die every year due to diseases communicated through consumption of water contaminated by deleterious pathogens. Although various methods for wastewater treatment have been explored in the last few decades but their use is restrained by many limitations including use of chemicals, formation of disinfection by-products (DBPs), time consumption and expensiveness. Nanotechnology, manipulation of matter at a molecular or an atomic level to craft new structures, devices and systems having superior electronic, optical, magnetic, conductive and mechanical properties, is emerging as a promising technology, which has demonstrated remarkable feats in various fields including wastewater treatment. Nanomaterials encompass a high surface to volume…
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Quercetin Prevents LPS-Induced Oxidative Stress and Inflammation by Modulating NOX2/ROS/NF-kB in Lung Epithelial Cells
Ok‐Joo Sul, Seung Hwan Won
421 citationsOpen access (CC-BY)doi:10.3390/molecules26226949OpenAlex
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Oxidative stress caused by the production of reactive oxygen species (ROS) plays a major role in inflammatory processes. We hypothesized that modulation of ROS via quercetin may protect against oxidative stress and inflammation. Thus, this study aimed to investigate the effects of quercetin on oxidative stress and inflammation in lung epithelial A549 cells. The lipopolysaccharide (LPS)-induced elevation of intracellular ROS levels was reduced after quercetin treatment, which also almost completely abolished the mRNA and protein expression of nicotinamide adenine dinucleotide phosphate oxidase 2 (NOX2) induced by LPS stimulation. In addition, quercetin suppressed the nuclear translocation of nuclear factor kappa B (NF-κB) and reduced levels of inflammatory cytokine tumor necrosis factor (TNF)-α, interleukin (IL)-1, and IL-6, which had increased significantly after LPS exposure. Our data demonstrated that quercetin decreased ROS-induced oxidative stress and inflammation by suppressing NOX2 production.
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Coriandrum sativum L.: A Review on Ethnopharmacology, Phytochemistry, and Cardiovascular Benefits
Nisa Najibah Mahleyuddin, Said Moshawih, Long Chiau Ming, Hanis Hanum Zulkifly, Nurolaini Kifli and 6 more
405 citationsOpen access (CC-BY)doi:10.3390/molecules27010209OpenAlex
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Coriandrum sativum (C. sativum), belonging to the Apiaceae (Umbelliferae) family, is widely recognized for its uses in culinary and traditional medicine. C. sativum contains various phytochemicals such as polyphenols, vitamins, and many phytosterols, which account for its properties including anticancer, anti-inflammatory, antidiabetic, and analgesic effects. The cardiovascular benefits of C. sativum have not been summarized before, hence this review aims to further evaluate and discuss its effectiveness in cardiovascular diseases, according to the recent literature. An electronic search for literature was carried out using the following databases: PubMed, Scopus, Google Scholar, preprint platforms, and the Cochrane Database of Systematic Reviews. Articles were gathered from the inception of the database until August 2021. Moreover, the traditional uses and phytochemistry of coriander were surveyed in the original resources and summarized. As a result, most of the studies that cover cardiovascular benefits and fulfilled the eligibility criteria were in vivo, while only a few were in…
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Biological Properties and Applications of Betalains
Izabela Sadowska‐Bartosz, Grzegorz Bartosz
403 citationsOpen access (CC-BY)doi:10.3390/molecules26092520OpenAlex
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Betalains are water-soluble pigments present in vacuoles of plants of the order Caryophyllales and in mushrooms of the genera Amanita, Hygrocybe and Hygrophorus. Betalamic acid is a constituent of all betalains. The type of betalamic acid substituent determines the class of betalains. The betacyanins (reddish to violet) contain a cyclo-3,4-dihydroxyphenylalanine (cyclo-DOPA) residue while the betaxanthins (yellow to orange) contain different amino acid or amine residues. The most common betacyanin is betanin (Beetroot Red), present in red beets Beta vulgaris, which is a glucoside of betanidin. The structure of this comprehensive review is as follows: Occurrence of Betalains; Structure of Betalains; Spectroscopic and Fluorescent Properties; Stability; Antioxidant Activity; Bioavailability, Health Benefits; Betalains as Food Colorants; Food Safety of Betalains; Other Applications of Betalains; and Environmental Role and Fate of Betalains.
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Cannabinoids, Phenolics, Terpenes and Alkaloids of Cannabis
Mohamed M. Radwan, Suman Chandra, Shahbaz W. Gul, Mahmoud A. ElSohly
397 citationsOpen access (CC-BY)doi:10.3390/molecules26092774OpenAlex
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Cannabis sativa is one of the oldest medicinal plants in the world. It was introduced into western medicine during the early 19th century. It contains a complex mixture of secondary metabolites, including cannabinoids and non-cannabinoid-type constituents. More than 500 compounds have been reported from C. sativa, of which 125 cannabinoids have been isolated and/or identified as cannabinoids. Cannabinoids are C21 terpeno-phenolic compounds specific to Cannabis. The non-cannabinoid constituents include: non-cannabinoid phenols, flavonoids, terpenes, alkaloids and others. This review discusses the chemistry of the cannabinoids and major non-cannabinoid constituents (terpenes, non-cannabinoid phenolics, and alkaloids) with special emphasis on their chemical structures, methods of isolation, and identification.
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Chemical Structure and Biological Activity of Humic Substances Define Their Role as Plant Growth Promoters
Serenella Nardi, Michela Schiavon, Ornella Francioso
396 citationsOpen access (CC-BY)doi:10.3390/molecules26082256OpenAlex
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Humic substances (HS) are dominant components of soil organic matter and are recognized as natural, effective growth promoters to be used in sustainable agriculture. In recent years, many efforts have been made to get insights on the relationship between HS chemical structure and their biological activity in plants using combinatory approaches. Relevant results highlight the existence of key functional groups in HS that might trigger positive local and systemic physiological responses via a complex network of hormone-like signaling pathways. The biological activity of HS finely relies on their dosage, origin, molecular size, degree of hydrophobicity and aromaticity, and spatial distribution of hydrophilic and hydrophobic domains. The molecular size of HS also impacts their mode of action in plants, as low molecular size HS can enter the root cells and directly elicit intracellular signals, while high molecular size HS bind to external cell receptors to induce molecular responses. Main targets of HS in plants are nutrient transporters, plasma membrane H+-ATPases, hormone routes,…
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Alkaloids Used as Medicines: Structural Phytochemistry Meets Biodiversity—An Update and Forward Look
Michael Heinrich, Jeffrey Mah, Vafa David Amirkia
396 citationsOpen access (CC-BY)doi:10.3390/molecules26071836OpenAlex
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Selecting candidates for drug developments using computational design and empirical rules has resulted in a broad discussion about their success. In a previous study, we had shown that a species' abundance [as expressed by the GBIF (Global Biodiversity Information Facility)] dataset is a core determinant for the development of a natural product into a medicine. Our overarching aim is to understand the unique requirements for natural product-based drug development. Web of Science was queried for research on alkaloids in combination with plant systematics/taxonomy. All alkaloids containing species demonstrated an average increase of 8.66 in GBIF occurrences between 2014 and 2020. Medicinal Species with alkaloids show higher abundance compared to non-medicinal alkaloids, often linked also to cultivation. Alkaloids with high biodiversity are often simple alkaloids found in multiple species with the presence of 'driver species' and are more likely to be included in early-stage drug development compared to 'rare' alkaloids. Similarly, the success of an alkaloid containing species as a…
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Wine Polyphenol Content and Its Influence on Wine Quality and Properties: A Review
Rocío Gutiérrez‐Escobar, María José Aliaño–González, Emma Cantos‐Villar
394 citationsOpen access (CC-BY)doi:10.3390/molecules26030718OpenAlex
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Wine is one of the most consumed beverages around the world. It is composed of alcohols, sugars, acids, minerals, proteins and other compounds, such as organic acids and volatile and phenolic compounds (also called polyphenols). Polyphenols have been shown to be highly related to both (i) wine quality (color, flavor, and taste) and (ii) health-promoting properties (antioxidant and cardioprotective among others). Polyphenols can be grouped into two big families: (i) Flavonoids, including anthocyanidins, flavonols, flavanols, hydrolysable and condensed tannins, flavanones, flavones and chalcones; and (ii) Non-flavonoids, including hydroxycinnamic acids, hydroxybenzoic acids, stilbenes, tyrosol and hydroxytyrosol. Each group affects in some way the different properties of wine to a greater or a lesser extent. For that reason, the phenolic composition can be managed to obtain singular wines with specific, desirable characteristics. The current review presents a summary of the ways in which the phenolic composition of wine can be modulated, including (a) invariable factors such as…
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Recent Developments in Chitosan-Based Adsorbents for the Removal of Pollutants from Aqueous Environments
Daniele Costa da Silva Alves, Bronach Healy, Luiz Antônio de Almeida Pinto, Tito Roberto Sant’Anna Cadaval, Carmel B. Breslin
384 citationsOpen access (CC-BY)doi:10.3390/molecules26030594OpenAlex
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The quality of water is continuously under threat as increasing concentrations of pollutants escape into the aquatic environment. However, these issues can be alleviated by adsorbing pollutants onto adsorbents. Chitosan and its composites are attracting considerable interest as environmentally acceptable adsorbents and have the potential to remove many of these contaminants. In this review the development of chitosan-based adsorbents is described and discussed. Following a short introduction to the extraction of chitin from seafood wastes, followed by its conversion to chitosan, the properties of chitosan are described. Then, the emerging chitosan/carbon-based materials, including magnetic chitosan and chitosan combined with graphene oxide, carbon nanotubes, biochar, and activated carbon and also chitosan-silica composites are introduced. The applications of these materials in the removal of various heavy metal ions, including Cr(VI), Pb(II), Cd(II), Cu(II), and different cationic and anionic dyes, phenol and other organic molecules, such as antibiotics, are reviewed, compared and…
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Astaxanthin for the Food Industry
Barbara Stachowiak, Piotr Mirosław Szulc
369 citationsOpen access (CC-BY)doi:10.3390/molecules26092666OpenAlex
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Xanthophyll astaxanthin, which is commonly used in aquaculture, is one of the most expensive and important industrial pigments. It is responsible for the pink and red color of salmonid meat and shrimp. Due to having the strongest anti-oxidative properties among carotenoids and other health benefits, natural astaxanthin is used in nutraceuticals and cosmetics, and in some countries, occasionally, to fortify foods and beverages. Its use in food technology is limited due to the unknown effects of long-term consumption of synthetic astaxanthin on human health as well as few sources and the high cost of natural astaxanthin. The article characterizes the structure, health-promoting properties, commercial sources and industrial use of astaxanthin. It presents the possibilities and limitations of the use of astaxanthin in food technology, considering its costs and food safety. It also presents the possibilities of stabilizing astaxanthin and improving its bioavailability by means of micro- and nanoencapsulation.
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The Potential of Selected Agri-Food Loss and Waste to Contribute to a Circular Economy: Applications in the Food, Cosmetic and Pharmaceutical Industries
Lady Laura Del Rio Osorio, Edwin Flórez‐López, Carlos David Grande‐Tovar
366 citationsOpen access (CC-BY)doi:10.3390/molecules26020515OpenAlex
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The food sector includes several large industries such as canned food, pasta, flour, frozen products, and beverages. Those industries transform agricultural raw materials into added-value products. The fruit and vegetable industry is the largest and fastest-growing segment of the world agricultural production market, which commercialize various products such as juices, jams, and dehydrated products, followed by the cereal industry products such as chocolate, beer, and vegetable oils are produced. Similarly, the root and tuber industry produces flours and starches essential for the daily diet due to their high carbohydrate content. However, the processing of these foods generates a large amount of waste several times improperly disposed of in landfills. Due to the increase in the world's population, the indiscriminate use of natural resources generates waste and food supply limitations due to the scarcity of resources, increasing hunger worldwide. The circular economy offers various tools for raising awareness for the recovery of waste, one of the best alternatives to mitigate the…
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Wearable Biosensors: An Alternative and Practical Approach in Healthcare and Disease Monitoring
Atul Sharma, Mihaela Badea, Swapnil Tiwari, Jean‐Louis Marty
362 citationsOpen access (CC-BY)doi:10.3390/molecules26030748OpenAlex
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With the increasing prevalence of growing population, aging and chronic diseases continuously rising healthcare costs, the healthcare system is undergoing a vital transformation from the traditional hospital-centered system to an individual-centered system. Since the 20th century, wearable sensors are becoming widespread in healthcare and biomedical monitoring systems, empowering continuous measurement of critical biomarkers for monitoring of the diseased condition and health, medical diagnostics and evaluation in biological fluids like saliva, blood, and sweat. Over the past few decades, the developments have been focused on electrochemical and optical biosensors, along with advances with the non-invasive monitoring of biomarkers, bacteria and hormones, etc. Wearable devices have evolved gradually with a mix of multiplexed biosensing, microfluidic sampling and transport systems integrated with flexible materials and body attachments for improved wearability and simplicity. These wearables hold promise and are capable of a higher understanding of the correlations between analyte…
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Green Silver and Gold Nanoparticles: Biological Synthesis Approaches and Potentials for Biomedical Applications
Andrea Rónavári, Nóra Igaz, Dóra Izabella Adamecz, Bettina Szerencsés, Csaba Molnár and 3 more
361 citationsOpen access (CC-BY)doi:10.3390/molecules26040844OpenAlex
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The nanomaterial industry generates gigantic quantities of metal-based nanomaterials for various technological and biomedical applications; however, concomitantly, it places a massive burden on the environment by utilizing toxic chemicals for the production process and leaving hazardous waste materials behind. Moreover, the employed, often unpleasant chemicals can affect the biocompatibility of the generated particles and severely restrict their application possibilities. On these grounds, green synthetic approaches have emerged, offering eco-friendly, sustainable, nature-derived alternative production methods, thus attenuating the ecological footprint of the nanomaterial industry. In the last decade, a plethora of biological materials has been tested to probe their suitability for nanomaterial synthesis. Although most of these approaches were successful, a large body of evidence indicates that the green material or entity used for the production would substantially define the physical and chemical properties and as a consequence, the biological activities of the obtained…
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Subcritical Water Extraction of Natural Products
Yan Cheng, Fumin Xue, Shuai Yu, Shichao Du, Yu Yang
358 citationsOpen access (CC-BY)doi:10.3390/molecules26134004OpenAlex
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Subcritical water refers to high-temperature and high-pressure water. A unique and useful characteristic of subcritical water is that its polarity can be dramatically decreased with increasing temperature. Therefore, subcritical water can behave similar to methanol or ethanol. This makes subcritical water a green extraction fluid used for a variety of organic species. This review focuses on the subcritical water extraction (SBWE) of natural products. The extracted materials include medicinal and seasoning herbs, vegetables, fruits, food by-products, algae, shrubs, tea leaves, grains, and seeds. A wide range of natural products such as alkaloids, carbohydrates, essential oil, flavonoids, glycosides, lignans, organic acids, polyphenolics, quinones, steroids, and terpenes have been extracted using subcritical water. Various SBWE systems and their advantages and drawbacks have also been discussed in this review. In addition, we have reviewed co-solvents including ethanol, methanol, salts, and ionic liquids used to assist SBWE. Other extraction techniques such as microwave and sonication…
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Adsorption of Crystal Violet Dye Using Activated Carbon of Lemon Wood and Activated Carbon/Fe3O4 Magnetic Nanocomposite from Aqueous Solutions: A Kinetic, Equilibrium and Thermodynamic Study
Rauf Foroutan, Seyed Jamaleddin Peighambardoust, Seyed Hadi Peighambardoust, Mirian Pateiro, José Manuel Lorenzo
357 citationsOpen access (CC-BY)doi:10.3390/molecules26082241OpenAlex
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Activated carbon prepared from lemon (Citrus limon) wood (ACL) and ACL/Fe3O4 magnetic nanocomposite were effectively used to remove the cationic dye of crystal violet (CV) from aqueous solutions. The results showed that Fe3O4 nanoparticles were successfully placed in the structure of ACL and the produced nanocomposites showed superior magnetic properties. It was found that pH was the most effective parameter in the CV dye adsorption and pH of 9 gave the maximum adsorption efficiency of 93.5% and 98.3% for ACL and ACL/Fe3O4, respectively. The Dubinin–Radushkevich (D-R) and Langmuir models were selected to investigate the CV dye adsorption equilibrium behavior for ACL and ACL/Fe3O4, respectively. A maximum adsorption capacity of 23.6 and 35.3 mg/g was obtained for ACL and ACL/Fe3O4, respectively indicating superior adsorption capacity of Fe3O4 nanoparticles. The kinetic data of the adsorption process followed the pseudo-second order (PSO) kinetic model, indicating that chemical mechanisms may have an effect on the CV dye adsorption. The negative values obtained for Gibb’s free energy…
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Advantages of Hyaluronic Acid and Its Combination with Other Bioactive Ingredients in Cosmeceuticals
Anca Maria Juncan, Dana Georgiana Moisă, Antonello Santini, Claudiu Morgovan, Luca Liviu Rus and 2 more
353 citationsOpen access (CC-BY)doi:10.3390/molecules26154429OpenAlex
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This study proposes a review on hyaluronic acid (HA) known as hyaluronan or hyaluronate and its derivates and their application in cosmetic formulations. HA is a glycosaminoglycan constituted from two disaccharides (N-acetylglucosamine and D-glucuronic acid), isolated initially from the vitreous humour of the eye, and subsequently discovered in different tissues or fluids (especially in the articular cartilage and the synovial fluid). It is ubiquitous in vertebrates, including humans, and it is involved in diverse biological processes, such as cell differentiation, embryological development, inflammation, wound healing, etc. HA has many qualities that recommend it over other substances used in skin regeneration, with moisturizing and anti-ageing effects. HA molecular weight influences its penetration into the skin and its biological activity. Considering that, nowadays, hyaluronic acid has a wide use and a multitude of applications (in ophthalmology, arthrology, pneumology, rhinology, aesthetic medicine, oncology, nutrition, and cosmetics), the present study describes the main…
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Thiazole Ring—A Biologically Active Scaffold
Anthi Petrou, Maria Fesatidou, Athina A. Geronikaki
351 citationsOpen access (CC-BY)doi:10.3390/molecules26113166OpenAlex
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BACKGROUND: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. OBJECTIVE: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. RESULTS: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.
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A Review on Natural Fiber Bio-Composites, Surface Modifications and Applications
Mohammed Zwawi
350 citationsOpen access (CC-BY)doi:10.3390/molecules26020404OpenAlex
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Increased environmental concerns and global warming have diverted focus from eco-friendly bio-composites. Naturals fibers are abundant and have low harvesting costs with adequate mechanical properties. Hazards of synthetic fibers, recycling issues, and toxic byproducts are the main driving factors in the research and development of bio-composites. Bio-composites are degradable, renewable, non-abrasive, and non-toxic, with comparable properties to those of synthetic fiber composites and used in many applications in various fields. A detailed analysis is carried out in this review paper to discuss developments in bio-composites. The review covers structure, morphology, and modifications of fiber, mechanical properties, degradable matrix materials, applications, and limitations of bio-composites. Some of the key sectors employing bio-composites are the construction, automobile, and packaging industries. Furthermore, bio-composites are used in the field of medicine and cosmetics.
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Soluble Dietary Fiber, One of the Most Important Nutrients for the Gut Microbiota
Zhi-Wei Guan, En-Ze Yu, Qiang Feng
340 citationsOpen access (CC-BY)doi:10.3390/molecules26226802OpenAlex
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Dietary fiber is a widely recognized nutrient for human health. Previous studies proved that dietary fiber has significant implications for gastrointestinal health by regulating the gut microbiota. Moreover, mechanistic research showed that the physiological functions of different dietary fibers depend to a great extent on their physicochemical characteristics, one of which is solubility. Compared with insoluble dietary fiber, soluble dietary fiber can be easily accessed and metabolized by fiber-degrading microorganisms in the intestine and produce a series of beneficial and functional metabolites. In this review, we outlined the structures, characteristics, and physiological functions of soluble dietary fibers as important nutrients. We particularly focused on the effects of soluble dietary fiber on human health via regulating the gut microbiota and reviewed their effects on dietary and clinical interventions.
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Dietary Flavonoids: Cardioprotective Potential with Antioxidant Effects and Their Pharmacokinetic, Toxicological and Therapeutic Concerns
Johra Khan, Prashanta Kumar Deb, Somi Priya, Karla Damian-Medina, Rajlakshmi Devi and 2 more
337 citationsOpen access (CC-BY)doi:10.3390/molecules26134021OpenAlex
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Flavonoids comprise a large group of structurally diverse polyphenolic compounds of plant origin and are abundantly found in human diet such as fruits, vegetables, grains, tea, dairy products, red wine, etc. Major classes of flavonoids include flavonols, flavones, flavanones, flavanols, anthocyanidins, isoflavones, and chalcones. Owing to their potential health benefits and medicinal significance, flavonoids are now considered as an indispensable component in a variety of medicinal, pharmaceutical, nutraceutical, and cosmetic preparations. Moreover, flavonoids play a significant role in preventing cardiovascular diseases (CVDs), which could be mainly due to their antioxidant, antiatherogenic, and antithrombotic effects. Epidemiological and in vitro/in vivo evidence of antioxidant effects supports the cardioprotective function of dietary flavonoids. Further, the inhibition of LDL oxidation and platelet aggregation following regular consumption of food containing flavonoids and moderate consumption of red wine might protect against atherosclerosis and thrombosis. One study suggests…
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Progresses in Food Packaging, Food Quality, and Safety—Controlled-Release Antioxidant and/or Antimicrobial Packaging
Cornelia Vasile, Mihaela Cristina Baican
333 citationsOpen access (CC-BY)doi:10.3390/molecules26051263OpenAlex
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Food packaging is designed to protect foods, to provide required information about the food, and to make food handling convenient for distribution to consumers. Packaging has a crucial role in the process of food quality, safety, and shelf-life extension. Possible interactions between food and packaging are important in what is concerning food quality and safety. This review tries to offer a picture of the most important types of active packaging emphasizing the controlled/target release antimicrobial and/or antioxidant packaging including system design, different methods of polymer matrix modification, and processing. The testing methods for the appreciation of the performance of active food packaging, as well as mechanisms and kinetics implied in active compounds release, are summarized. During the last years, many fast advancements in packaging technology appeared, including intelligent or smart packaging (IOSP), (i.e., time-temperature indicators (TTIs), gas indicators, radiofrequency identification (RFID), and others). Legislation is also discussed.
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Role of Monoamine Oxidase Activity in Alzheimer’s Disease: An Insight into the Therapeutic Potential of Inhibitors
Tapan Behl, Dapinder Kaur, Aayush Sehgal, Sukhbir Singh, Neelam Sharma and 5 more
329 citationsOpen access (CC-BY)doi:10.3390/molecules26123724OpenAlex
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Despite not being utilized as considerably as other antidepressants in the therapy of depression, the monoamine oxidase inhibitors (MAOIs) proceed to hold a place in neurodegeneration and to have a somewhat broad spectrum in respect of the treatment of neurological and psychiatric conditions. Preclinical and clinical studies on MAOIs have been developing in recent times, especially on account of rousing discoveries manifesting that these drugs possess neuroprotective activities. The altered brain levels of monoamine neurotransmitters due to monoamine oxidase (MAO) are directly associated with various neuropsychiatric conditions like Alzheimer's disease (AD). Activated MAO induces the amyloid-beta (Aβ) deposition via abnormal cleavage of the amyloid precursor protein (APP). Additionally, activated MAO contributes to the generation of neurofibrillary tangles and cognitive impairment due to neuronal loss. No matter the attention of researchers on the participation of MAOIs in neuroprotection has been on monoamine oxidase-B (MAO-B) inhibitors, there is a developing frame of proof…
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Bioethanol Production by Enzymatic Hydrolysis from Different Lignocellulosic Sources
Katja Vasić, Željko Knez, Maja Leitgeb
326 citationsOpen access (CC-BY)doi:10.3390/molecules26030753OpenAlex
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As the need for non-renewable sources such as fossil fuels has increased during the last few decades, the search for sustainable and renewable alternative sources has gained growing interest. Enzymatic hydrolysis in bioethanol production presents an important step, where sugars that are fermented are obtained in the final fermentation process. In the process of enzymatic hydrolysis, more and more new effective enzymes are being researched to ensure a more cost-effective process. There are many different enzyme strategies implemented in hydrolysis protocols, where different lignocellulosic biomass, such as wood feedstocks, different agricultural wastes, and marine algae are being used as substrates for an efficient bioethanol production. This review investigates the very recent enzymatic hydrolysis pathways in bioethanol production from lignocellulosic biomass.
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Recent Achievements in Dyes Removal Focused on Advanced Oxidation Processes Integrated with Biological Methods
S. Ledakowicz, Katarzyna Paździor
322 citationsOpen access (CC-BY)doi:10.3390/molecules26040870OpenAlex
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In the last 3 years alone, over 10,000 publications have appeared on the topic of dye removal, including over 300 reviews. Thus, the topic is very relevant, although there are few articles on the practical applications on an industrial scale of the results obtained in research laboratories. Therefore, in this review, we focus on advanced oxidation methods integrated with biological methods, widely recognized as highly efficient treatments for recalcitrant wastewater, that have the best chance of industrial application. It is extremely important to know all the phenomena and mechanisms that occur during the process of removing dyestuffs and the products of their degradation from wastewater to prevent their penetration into drinking water sources. Therefore, particular attention is paid to understanding the mechanisms of both chemical and biological degradation of dyes, and the kinetics of these processes, which are important from a design point of view, as well as the performance and implementation of these operations on a larger scale.
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A Critical Review on Pulsed Electric Field: A Novel Technology for the Extraction of Phytoconstituents
Muhammad Modassar Ali Nawaz Ranjha, Rabia Kanwal, Bakhtawar Shafique, Rai Naveed Arshad, Shafeeqa Irfan and 6 more
316 citationsOpen access (CC-BY)doi:10.3390/molecules26164893OpenAlex
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Different parts of a plant (seeds, fruits, flower, leaves, stem, and roots) contain numerous biologically active compounds called "phytoconstituents" that consist of phenolics, minerals, amino acids, and vitamins. The conventional techniques applied to extract these phytoconstituents have several drawbacks including poor performance, low yields, more solvent use, long processing time, and thermally degrading by-products. In contrast, modern and advanced extraction nonthermal technologies such as pulsed electric field (PEF) assist in easier and efficient identification, characterization, and analysis of bioactive ingredients. Other advantages of PEF include cost-efficacy, less time, and solvent consumption with improved yields. This review covers the applications of PEF to obtain bioactive components, essential oils, proteins, pectin, and other important materials from various parts of the plant. Numerous studies compiled in the current evaluation concluded PEF as the best solution to extract phytoconstituents used in the food and pharmaceutical industries. PEF-assisted extraction…
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Effect of Dataset Size and Train/Test Split Ratios in QSAR/QSPR Multiclass Classification
Anita Rácz, Dávid Bajusz, Károly Héberger
309 citationsOpen access (CC-BY)doi:10.3390/molecules26041111OpenAlex
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Applied datasets can vary from a few hundred to thousands of samples in typical quantitative structure-activity/property (QSAR/QSPR) relationships and classification. However, the size of the datasets and the train/test split ratios can greatly affect the outcome of the models, and thus the classification performance itself. We compared several combinations of dataset sizes and split ratios with five different machine learning algorithms to find the differences or similarities and to select the best parameter settings in nonbinary (multiclass) classification. It is also known that the models are ranked differently according to the performance merit(s) used. Here, 25 performance parameters were calculated for each model, then factorial ANOVA was applied to compare the results. The results clearly show the differences not just between the applied machine learning algorithms but also between the dataset sizes and to a lesser extent the train/test split ratios. The XGBoost algorithm could outperform the others, even in multiclass modeling. The performance parameters reacted differently…
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Neuroprotective Effect of SGLT2 Inhibitors
Agnieszka Pawlos, Marlena Broncel, Ewelina Woźniak, Paulina Gorzelak‐Pabiś
303 citationsOpen access (CC-BY)doi:10.3390/molecules26237213OpenAlex
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Patients with diabetes are at higher risk of cardiovascular diseases and cognitive impairment. SGLT2 inhibitors (Empagliflozin, Canagliflozin, Dapagliflozin, Ertugliflozin, Sotagliflozin) are newer hypoglycemic agents with many pleiotropic effects. In this review, we discuss their neuroprotective potential. SGLT2 inhibitors (SGLT2i) are lipid-soluble and reach the brain/serum ratio from 0.3 to 0.5. SGLT receptors are present in the central nervous system (CNS). Flozins are not fully SGLT2-selective and have an affinity for the SGLT1 receptor, which is associated with protection against ischemia/reperfusion brain damage. SGLT2i show an anti-inflammatory and anti-atherosclerotic effect, including reduction of proinflammatory cytokines, M2 macrophage polarization, JAK2/STAT1 and NLRP3 inflammasome inhibition, as well as cIMT regression. They also mitigate oxidative stress. SGLT2i improve endothelial function, prevent remodeling and exert a protective effect on the neurovascular unit, blood-brain barrier, pericytes, astrocytes, microglia, and oligodendrocytes. Flozins are also able to…
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The Concept of Folic Acid in Health and Disease
Yu. O. Shulpekova, V. M. Nechaev, Svetlana S. Kardasheva, Alla Sedova, А. А. Курбатова and 5 more
302 citationsOpen access (CC-BY)doi:10.3390/molecules26123731OpenAlex
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Folates have a pterine core structure and high metabolic activity due to their ability to accept electrons and react with O-, S-, N-, C-bounds. Folates play a role as cofactors in essential one-carbon pathways donating methyl-groups to choline phospholipids, creatine, epinephrine, DNA. Compounds similar to folates are ubiquitous and have been found in different animals, plants, and microorganisms. Folates enter the body from the diet and are also synthesized by intestinal bacteria with consequent adsorption from the colon. Three types of folate and antifolate cellular transporters have been found, differing in tissue localization, substrate affinity, type of transferring, and optimal pH for function. Laboratory criteria of folate deficiency are accepted by WHO. Severe folate deficiencies, manifesting in early life, are seen in hereditary folate malabsorption and cerebral folate deficiency. Acquired folate deficiency is quite common and is associated with poor diet and malabsorption, alcohol consumption, obesity, and kidney failure. Given the observational data that folates have a…
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TiO2 as a Photocatalyst for Water Splitting—An Experimental and Theoretical Review
Håkon Eidsvåg, Saïd Bentouba, Ponniah Vajeeston, Yohi Shivatharsiny, Dhayalan Velauthapillai
297 citationsOpen access (CC-BY)doi:10.3390/molecules26061687OpenAlex
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Hydrogen produced from water using photocatalysts driven by sunlight is a sustainable way to overcome the intermittency issues of solar power and provide a green alternative to fossil fuels. TiO2 has been used as a photocatalyst since the 1970s due to its low cost, earth abundance, and stability. There has been a wide range of research activities in order to enhance the use of TiO2 as a photocatalyst using dopants, modifying the surface, or depositing noble metals. However, the issues such as wide bandgap, high electron-hole recombination time, and a large overpotential for the hydrogen evolution reaction (HER) persist as a challenge. Here, we review state-of-the-art experimental and theoretical research on TiO2 based photocatalysts and identify challenges that have to be focused on to drive the field further. We conclude with a discussion of four challenges for TiO2 photocatalysts—non-standardized presentation of results, bandgap in the ultraviolet (UV) region, lack of collaboration between experimental and theoretical work, and lack of large/small scale production facilities. We…
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Common Trends and Differences in Antioxidant Activity Analysis of Phenolic Substances Using Single Electron Transfer Based Assays
Melanie Platzer, Sandra Kiese, Thomas Herfellner, Ute Schweiggert‐Weisz, Oliver Miesbauer and 1 more
295 citationsOpen access (CC-BY)doi:10.3390/molecules26051244OpenAlex
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Numerous assays were developed to measure the antioxidant activity, but each has limitations and the results obtained by different methods are not always comparable. Popular examples are the DPPH and ABTS assay. Our aim was to study similarities and differences of these two assay regarding the measured antioxidant potentials of 24 phenolic compounds using the same measurement and evaluation methods. This should allow conclusions to be drawn as to whether one of the assays is more suitable for measuring specific subgroups like phenolic acids, flavonols, flavanones, dihydrochalcones or flavanols. The assays showed common trends for the mean values of most of the subgroups. Some dihydrochalcones and flavanones did not react with the DPPH radical in contrast to the ABTS radical, leading to significant differences. Therefore, to determine the antioxidant potential of dihydrochalcone or flavanone-rich extracts, the ABTS assay should be preferred. We found that the results of the flavonoids in the DPPH assay were dependent on the Bors criteria, whereas the structure-activity relationship…
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Berberine as a Potential Anticancer Agent: A Comprehensive Review
Abdur Rauf, Tareq Abu‐Izneid, Anees Ahmed Khalil, Muhammad Imran, Zafar Ali Shah and 9 more
294 citationsOpen access (CC-BY)doi:10.3390/molecules26237368OpenAlex
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Berberine (BBR), a potential bioactive agent, has remarkable health benefits. A substantial amount of research has been conducted to date to establish the anticancer potential of BBR. The present review consolidates salient information concerning the promising anticancer activity of this compound. The therapeutic efficacy of BBR has been reported in several studies regarding colon, breast, pancreatic, liver, oral, bone, cutaneous, prostate, intestine, and thyroid cancers. BBR prevents cancer cell proliferation by inducing apoptosis and controlling the cell cycle as well as autophagy. BBR also hinders tumor cell invasion and metastasis by down-regulating metastasis-related proteins. Moreover, BBR is also beneficial in the early stages of cancer development by lowering epithelial-mesenchymal transition protein expression. Despite its significance as a potentially promising drug candidate, there are currently no pure berberine preparations approved to treat specific ailments. Hence, this review highlights our current comprehensive knowledge of sources, extraction methods,…
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Chitosan Nanoparticles-Insight into Properties, Functionalization and Applications in Drug Delivery and Theranostics
Jhanvi Jhaveri, Zarna Raichura, Tabassum Asif Khan, Munira M. Momin, Abdelwahab Omri
293 citationsOpen access (CC-BY)doi:10.3390/molecules26020272OpenAlex
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Nanotechnology-based development of drug delivery systems is an attractive area of research in formulation driven R&D laboratories that makes administration of new and complex drugs feasible. It plays a significant role in the design of novel dosage forms by attributing target specific drug delivery, controlled drug release, improved, patient friendly drug regimen and lower side effects. Polysaccharides, especially chitosan, occupy an important place and are widely used in nano drug delivery systems owing to their biocompatibility and biodegradability. This review focuses on chitosan nanoparticles and envisages to provide an insight into the chemistry, properties, drug release mechanisms, preparation techniques and the vast evolving landscape of diverse applications across disease categories leading to development of better therapeutics and superior clinical outcomes. It summarizes recent advancement in the development and utility of functionalized chitosan in anticancer therapeutics, cancer immunotherapy, theranostics and multistage delivery systems.
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An Insight into FDA Approved Antibody-Drug Conjugates for Cancer Therapy
Juliana T. W. Tong, Paul W. R. Harris, Margaret Anne Brimble, Iman Kavianinia
290 citationsOpen access (CC-BY)doi:10.3390/molecules26195847OpenAlex
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The large number of emerging antibody-drug conjugates (ADCs) for cancer therapy has resulted in a significant market 'boom', garnering worldwide attention. Despite ADCs presenting huge challenges to researchers, particularly regarding the identification of a suitable combination of antibody, linker, and payload, as of September 2021, 11 ADCs have been granted FDA approval, with eight of these approved since 2017 alone. Optimism for this therapeutic approach is clear, despite the COVID-19 pandemic, 2020 was a landmark year for deals and partnerships in the ADC arena, suggesting that there remains significant interest from Big Pharma. Herein we review the enthusiasm for ADCs by focusing on the features of those approved by the FDA, and offer some thoughts as to where the field is headed.
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Green Synthesis of Gold Nanoparticles Using Plant Extracts as Beneficial Prospect for Cancer Theranostics
Kaushik Kumar Bharadwaj, Bijuli Rabha, Siddhartha Pati, Tanmay Sarkar, Bhabesh Kumar Choudhury and 7 more
289 citationsOpen access (CC-BY)doi:10.3390/molecules26216389OpenAlex
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Gold nanoparticles (AuNPs) have been widely explored and are well-known for their medical applications. Chemical and physical synthesis methods are a way to make AuNPs. In any case, the hunt for other more ecologically friendly and cost-effective large-scale technologies, such as environmentally friendly biological processes known as green synthesis, has been gaining interest by worldwide researchers. The international focus on green nanotechnology research has resulted in various nanomaterials being used in environmentally and physiologically acceptable applications. Several advantages over conventional physical and chemical synthesis (simple, one-step approach to synthesize, cost-effectiveness, energy efficiency, and biocompatibility) have drawn scientists' attention to exploring the green synthesis of AuNPs by exploiting plants' secondary metabolites. Biogenic approaches, mainly the plant-based synthesis of metal nanoparticles, have been chosen as the ideal strategy due to their environmental and in vivo safety, as well as their ease of synthesis. In this review, we reviewed the…
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Dietary Plant Polyphenols: Effects of Food Processing on Their Content and Bioavailability
Leila Arfaoui
287 citationsOpen access (CC-BY)doi:10.3390/molecules26102959OpenAlex
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Dietary plant polyphenols are natural bioactive compounds that are increasingly attracting the attention of food scientists and nutritionists because of their nutraceutical properties. In fact, many studies have shown that polyphenol-rich diets have protective effects against most chronic diseases. However, these health benefits are strongly related to both polyphenol content and bioavailability, which in turn depend on their origin, food matrix, processing, digestion, and cellular metabolism. Although most fruits and vegetables are valuable sources of polyphenols, they are not usually consumed raw. Instead, they go through some processing steps, either industrially or domestically (e.g., cooling, heating, drying, fermentation, etc.), that affect their content, bioaccessibility, and bioavailability. This review summarizes the status of knowledge on the possible (positive or negative) effects of commonly used food-processing techniques on phenolic compound content and bioavailability in fruits and vegetables. These effects depend on the plant type and applied processing parameters…
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Role of Gut Microbiota, Probiotics and Prebiotics in the Cardiovascular Diseases
Anna Oniszczuk, Tomasz Oniszczuk, Marek Gancarz, Jolanta Szymańska
278 citationsOpen access (CC-BY)doi:10.3390/molecules26041172OpenAlex
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In recent years, there has been a growing interest in identifying and applying new, naturally occurring molecules that promote health. Probiotics are defined as "live microorganisms which, when administered in adequate amounts, confer health benefits on the host". Quite a few fermented products serve as the source of probiotic strains, with many factors influencing the effectiveness of probiotics, including interactions of probiotic bacteria with the host's microbiome. Prebiotics contain no microorganisms, only substances which stimulate their growth. Prebiotics can be obtained from various sources, including breast milk, soybeans, and raw oats, however, the most popular prebiotics are the oligosaccharides contained in plants. Recent research increasingly claims that probiotics and prebiotics alleviate many disorders related to the immune system, cancer metastasis, type 2 diabetes, and obesity. However, little is known about the role of these supplements as important dietary components in preventing or treating cardiovascular disease. Still, some reports and clinical studies were…
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Recovery of Banana Waste-Loss from Production and Processing: A Contribution to a Circular Economy
Sasha Alzate Acevedo, Álvaro José Díaz Carrillo, Edwin Flórez‐López, Carlos David Grande‐Tovar
277 citationsOpen access (CC-BY)doi:10.3390/molecules26175282OpenAlex
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Banana is a fruit grown mainly in tropical countries of the world. After harvest, almost 60% of banana biomass is left as waste. Worldwide, about 114.08 million metric tons of banana waste-loss are produced, leading to environmental problems such as the excessive emission of greenhouse gases. These wastes contain a high content of paramount industrial importance, such as cellulose, hemicellulose and natural fibers that various processes can modify, such as bacterial fermentation and anaerobic degradation, to obtain bioplastics, organic fertilizers and biofuels such as ethanol, biogas, hydrogen and biodiesel. In addition, they can be used in wastewater treatment methods by producing low-cost biofilters and obtaining activated carbon from rachis and banana peel. Furthermore, nanometric fibers commonly used in nanotechnology applications and silver nanoparticles useful in therapeutic cancer treatments, can be produced from banana pseudostems. The review aims to demonstrate the contribution of the recovery of banana production waste-loss towards a circular economy that would boost the…
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Verification of the Conditions for Determination of Antioxidant Activity by ABTS and DPPH Assays—A Practical Approach
Rafał Wołosiak, Beata Drużyńska, Dorota Derewiaka, Małgorzata Piecyk, Ewa Majewska and 3 more
274 citationsOpen access (CC-BY)doi:10.3390/molecules27010050OpenAlex
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The ABTS and DPPH methods are among the most popular assays of antioxidant activity determination. Attempts to adapt them to different analytes and the search for the highest values of antioxidant activity has resulted in a large variety of assay conditions to be presented in the literature, including the way the measurement is made. This makes it difficult to relate the results to real oxidation systems, and often makes it impossible to compare them. Such a comparison is limited in advance by the use of stable radicals that do not exist in nature and that react differently from those generated in food or in vivo. Therefore, it is important to introduce measures aimed at standardizing the conditions of the activity assay, including reaction time and several reaction environments suitable for testing different groups of compounds. In this study, we used natural antioxidants of various structures: phenolic acids, flavonoids, peptides and corresponding amino acids, ascorbic acid and α-tocopherol, and also synthetic analogues of selected compounds. The curves of dependence of the…
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Electrostatic Potential Topology for Probing Molecular Structure, Bonding and Reactivity
Shridhar Ramachandra Gadre, Cherumuttathu Hariharan Suresh, Neetha Mohan
266 citationsOpen access (CC-BY)doi:10.3390/molecules26113289OpenAlex
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Following the pioneering investigations of Bader on the topology of molecular electron density, the topology analysis of its sister field viz. molecular electrostatic potential (MESP) was taken up by the authors' groups. Through these studies, MESP topology emerged as a powerful tool for exploring molecular bonding and reactivity patterns. The MESP topology features are mapped in terms of its critical points (CPs), such as bond critical points (BCPs), while the minima identify electron-rich locations, such as lone pairs and π-bonds. The gradient paths of MESP vividly bring out the atoms-in-molecule picture of neutral molecules and anions. The MESP-based characterization of a molecule in terms of electron-rich and -deficient regions provides a robust prediction about its interaction with other molecules. This leads to a clear picture of molecular aggregation, hydrogen bonding, lone pair-π interactions, π-conjugation, aromaticity and reaction mechanisms. This review summarizes the contributions of the authors' groups over the last three decades and those of the other active groups…
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Overview of the Antioxidant and Anti-Inflammatory Activities of Selected Plant Compounds and Their Metal Ions Complexes
Paulina Mucha, Anna Skoczyńska, Magdalena Małecka, Paweł Hikisz, Elżbieta Budzisz
265 citationsOpen access (CC-BY)doi:10.3390/molecules26164886OpenAlex
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Numerous plant compounds and their metal-ion complexes exert antioxidative, anti-inflammatory, anticancer, and other beneficial effects. This review highlights the different bioactivities of flavonoids, chromones, and coumarins and their metal-ions complexes due to different structural characteristics. In addition to insight into the most studied antioxidative properties of these compounds, the first part of the review provides a comprehensive overview of exogenous and endogenous sources of reactive oxygen and nitrogen species, oxidative stress-mediated damages of lipids and proteins, and on protective roles of antioxidant defense systems, including plant-derived antioxidants. Additionally, the review covers the anti-inflammatory and antimicrobial activities of flavonoids, chromones, coumarins and their metal-ion complexes which support its application in medicine, pharmacy, and cosmetology.
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Selenium Biofortification: Roles, Mechanisms, Responses and Prospects
Akbar Hossain, Milan Skalický, Marián Brestič, Sagar Maitra, Sukamal Sarkar and 10 more
264 citationsOpen access (CC-BY)doi:10.3390/molecules26040881OpenAlex
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The trace element selenium (Se) is a crucial element for many living organisms, including soil microorganisms, plants and animals, including humans. Generally, in Nature Se is taken up in the living cells of microorganisms, plants, animals and humans in several inorganic forms such as selenate, selenite, elemental Se and selenide. These forms are converted to organic forms by biological process, mostly as the two selenoamino acids selenocysteine (SeCys) and selenomethionine (SeMet). The biological systems of plants, animals and humans can fix these amino acids into Se-containing proteins by a modest replacement of methionine with SeMet. While the form SeCys is usually present in the active site of enzymes, which is essential for catalytic activity. Within human cells, organic forms of Se are significant for the accurate functioning of the immune and reproductive systems, the thyroid and the brain, and to enzyme activity within cells. Humans ingest Se through plant and animal foods rich in the element. The concentration of Se in foodstuffs depends on the presence of available forms…
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Okra (Abelmoschus Esculentus) as a Potential Dietary Medicine with Nutraceutical Importance for Sustainable Health Applications
Abd Elmoneim O. Elkhalifa, Eyad Al-Shammari, Mohd Adnan, Jerold Casem Alcantara, Amir Mahgoub Awadelkareem and 4 more
263 citationsOpen access (CC-BY)doi:10.3390/molecules26030696OpenAlex
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L.) is a popular vegetable crop with good nutritional significance, along with certain therapeutic values, which makes it a potential candidate in the use of a variety of nutraceuticals. Different parts of the okra fruit (mucilage, seed, and pods) contain certain important bioactive components, which confer its medicinal properties. The phytochemicals of okra have been studied for their potential therapeutic activities on various chronic diseases, such as type-2 diabetes, cardiovascular, and digestive diseases, as well as the antifatigue effect, liver detoxification, antibacterial, and chemo-preventive activities. Moreover, okra mucilage has been widely used in medicinal applications such as a plasma replacement or blood volume expanders. Overall, okra is considered to be an easily available, low-cost vegetable crop with various nutritional values and potential health benefits. Despite several reports about its therapeutic benefits and potential nutraceutical significance, there is a dearth of research on the pharmacokinetics and bioavailability of okra, which has hampered its…
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The Protective Role of Butyrate against Obesity and Obesity-Related Diseases
Serena Coppola, Carmen Avagliano, Antonio Calignano, Roberto Berni Canani
262 citationsOpen access (CC-BY)doi:10.3390/molecules26030682OpenAlex
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Worldwide obesity is a public health concern that has reached pandemic levels. Obesity is the major predisposing factor to comorbidities, including type 2 diabetes, cardiovascular diseases, dyslipidemia, and non-alcoholic fatty liver disease. The common forms of obesity are multifactorial and derive from a complex interplay of environmental changes and the individual genetic predisposition. Increasing evidence suggest a pivotal role played by alterations of gut microbiota (GM) that could represent the causative link between environmental factors and onset of obesity. The beneficial effects of GM are mainly mediated by the secretion of various metabolites. Short-chain fatty acids (SCFAs) acetate, propionate and butyrate are small organic metabolites produced by fermentation of dietary fibers and resistant starch with vast beneficial effects in energy metabolism, intestinal homeostasis and immune responses regulation. An aberrant production of SCFAs has emerged in obesity and metabolic diseases. Among SCFAs, butyrate emerged because it might have a potential in alleviating obesity and…
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Superoxide Dismutase Administration: A Review of Proposed Human Uses
Arianna Carolina Rosa, Daniele Corsi, Niccolò Cavi, Natascia Bruni, Franco Dosio
259 citationsOpen access (CC-BY)doi:10.3390/molecules26071844OpenAlex
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Superoxide dismutases (SODs) are metalloenzymes that play a major role in antioxidant defense against oxidative stress in the body. SOD supplementation may therefore trigger the endogenous antioxidant machinery for the neutralization of free-radical excess and be used in a variety of pathological settings. This paper aimed to provide an extensive review of the possible uses of SODs in a range of pathological settings, as well as describe the current pitfalls and the delivery strategies that are in development to solve bioavailability issues. We carried out a PubMed query, using the keywords "SOD", "SOD mimetics", "SOD supplementation", which included papers published in the English language, between 2012 and 2020, on the potential therapeutic applications of SODs, including detoxification strategies. As highlighted in this paper, it can be argued that the generic antioxidant effects of SODs are beneficial under all tested conditions, from ocular and cardiovascular diseases to neurodegenerative disorders and metabolic diseases, including diabetes and its complications and obesity.…
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Nutraceuticals: Transformation of Conventional Foods into Health Promoters/Disease Preventers and Safety Considerations
Mudhi AlAli, Maream Alqubaisy, Mariam Nasser Aljaafari, Asma Obaid AlAli, Laila Baqais and 4 more
256 citationsOpen access (CC-BY)doi:10.3390/molecules26092540OpenAlex
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Nutraceuticals are essential food constituents that provide nutritional benefits as well as medicinal effects. The benefits of these foods are due to the presence of active compounds such as carotenoids, collagen hydrolysate, and dietary fibers. Nutraceuticals have been found to positively affect cardiovascular and immune system health and have a role in infection and cancer prevention. Nutraceuticals can be categorized into different classes based on their nature and mode of action. In this review, different classifications of nutraceuticals and their potential therapeutic activity, such as anti-cancer, antioxidant, anti-inflammatory and anti-lipid activity in disease will be reviewed. Moreover, the different mechanisms of action of these products, applications, and safety upon consumers including current trends and future prospect of nutraceuticals will be included.
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Nanomaterials for Biomedical Applications: Production, Characterisations, Recent Trends and Difficulties
Mostafa Mabrouk, Diganta Bhusan Das, Zeinab Amin Salem, Hanan H. Beherei
253 citationsOpen access (CC-BY)doi:10.3390/molecules26041077OpenAlex
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Designing of nanomaterials has now become a top-priority research goal with a view to developing specific applications in the biomedical fields. In fact, the recent trends in the literature show that there is a lack of in-depth reviews that specifically highlight the current knowledge based on the design and production of nanomaterials. Considerations of size, shape, surface charge and microstructures are important factors in this regard as they affect the performance of nanoparticles (NPs). These parameters are also found to be dependent on their synthesis methods. The characterisation techniques that have been used for the investigation of these nanomaterials are relatively different in their concepts, sample preparation methods and obtained results. Consequently, this review article aims to carry out an in-depth discussion on the recent trends on nanomaterials for biomedical engineering, with a particular emphasis on the choices of the nanomaterials, preparation methods/instruments and characterisations techniques used for designing of nanomaterials. Key applications of these…
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Preparation and Antimicrobial Activity of Chitosan and Its Derivatives: A Concise Review
Luminita Georgeta Confederat, Cristina Tuchiluş, Maria Drăgan, Mousa Sha’at, Oana Maria Dragostin
252 citationsOpen access (CC-BY)doi:10.3390/molecules26123694OpenAlex
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Despite the advantages presented by synthetic polymers such as strength and durability, the lack of biodegradability associated with the persistence in the environment for a long time turned the attention of researchers to natural polymers. Being biodegradable, biopolymers proved to be extremely beneficial to the environment. At present, they represent an important class of materials with applications in all economic sectors, but also in medicine. They find applications as absorbers, cosmetics, controlled drug delivery, tissue engineering, etc. Chitosan is one of the natural polymers which raised a strong interest for researchers due to some exceptional properties such as biodegradability, biocompatibility, nontoxicity, non-antigenicity, low-cost and numerous pharmacological properties as antimicrobial, antitumor, antioxidant, antidiabetic, immunoenhancing. In addition to this, the free amino and hydroxyl groups make it susceptible to a series of structural modulations, obtaining some derivatives with different biomedical applications. This review approaches the physico-chemical and…
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Chalcone Scaffolds, Bioprecursors of Flavonoids: Chemistry, Bioactivities, and Pharmacokinetics
Mithun Rudrapal, Johra Khan, Abdul Aziz Bin Dukhyil, Randa Mohamed Ismail, Emmanuel Ifeanyi Attah and 3 more
247 citationsOpen access (CC-BY)doi:10.3390/molecules26237177OpenAlex
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system) family that are ubiquitous in edible and medicinal plants, and they are bioprecursors of plant flavonoids. Chalcones and their natural derivatives are important intermediates of the flavonoid biosynthetic pathway. Plants containing chalcones have been used in traditional medicines since antiquity. Chalcones are basically α,β-unsaturated ketones that exert great diversity in pharmacological activities such as antioxidant, anticancer, antimicrobial, antiviral, antitubercular, antiplasmodial, antileishmanial, immunosuppressive, anti-inflammatory, and so on. This review provides an insight into the chemistry, biosynthesis, and occurrence of chalcones from natural sources, particularly dietary and medicinal plants. Furthermore, the pharmacological, pharmacokinetics, and toxicological aspects of naturally occurring chalcone derivatives are also discussed herein. In view of having tremendous pharmacological potential, chalcone scaffolds/chalcone derivatives and bioflavonoids after subtle chemical modification could serve as a reliable platform for natural products-based drug…
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The Therapeutic Potential of Psilocybin
Henry I. C. Lowe, Ngeh J. Toyang, Blair Steele, Henkel Valentine, Justin Grant and 3 more
243 citationsOpen access (CC-BY)doi:10.3390/molecules26102948OpenAlex
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The psychedelic effects of some plants and fungi have been known and deliberately exploited by humans for thousands of years. Fungi, particularly mushrooms, are the principal source of naturally occurring psychedelics. The mushroom extract, psilocybin has historically been used as a psychedelic agent for religious and spiritual ceremonies, as well as a therapeutic option for neuropsychiatric conditions. Psychedelic use was largely associated with the "hippie" counterculture movement, which, in turn, resulted in a growing, and still lingering, negative stigmatization for psychedelics. As a result, in 1970, the U.S. government rescheduled psychedelics as Schedule 1 drugs, ultimately ending scientific research on psychedelics. This prohibition on psychedelic drug research significantly delayed advances in medical knowledge on the therapeutic uses of agents such as psilocybin. A 2004 pilot study from the University of California, Los Angeles, exploring the potential of psilocybin treatment in patients with advanced-stage cancer managed to reignite interest and significantly renewed…
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Liposomes as Antibiotic Delivery Systems: A Promising Nanotechnological Strategy against Antimicrobial Resistance
Magda Ferreira, Maria Ogren, Joana Dias, Marta Silva, Solange Gil and 4 more
241 citationsOpen access (CC-BY)doi:10.3390/molecules26072047OpenAlex
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Antimicrobial drugs are key tools to prevent and treat bacterial infections. Despite the early success of antibiotics, the current treatment of bacterial infections faces serious challenges due to the emergence and spread of resistant bacteria. Moreover, the decline of research and private investment in new antibiotics further aggravates this antibiotic crisis era. Overcoming the complexity of antimicrobial resistance must go beyond the search of new classes of antibiotics and include the development of alternative solutions. The evolution of nanomedicine has allowed the design of new drug delivery systems with improved therapeutic index for the incorporated compounds. One of the most promising strategies is their association to lipid-based delivery (nano)systems. A drug’s encapsulation in liposomes has been demonstrated to increase its accumulation at the infection site, minimizing drug toxicity and protecting the antibiotic from peripheral degradation. In addition, liposomes may be designed to fuse with bacterial cells, holding the potential to overcome antimicrobial resistance…
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Excited-State Intramolecular Proton Transfer: A Short Introductory Review
Hem Chandra Joshi, Liudmil Antonov
241 citationsOpen access (CC-BY)doi:10.3390/molecules26051475OpenAlex
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In this short review, we attempt to unfold various aspects of excited-state intramolecular proton transfer (ESIPT) from the studies that are available up to date. Since Weller's discovery of ESIPT in salicylic acid (SA) and its derivative methyl salicylate (MS), numerous studies have emerged on the topic and it has become an attractive field of research because of its manifold applications. Here, we discuss some critical aspects of ESIPT and tautomerization from the mechanistic viewpoint. We address excitation wavelength dependence, anti-Kasha ESIPT, fast and slow ESIPT, reversibility and irreversibility of ESIPT, hydrogen bonding and geometrical factors, excited-state double proton transfer (ESDPT), concerted and stepwise ESDPT.
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Curcumin Nanoparticles as Promising Therapeutic Agents for Drug Targets
Hitesh Chopra, Protity Shuvra Dey, Debashrita Das, Tanima Bhattacharya, Muddaser Shah and 13 more
239 citationsOpen access (CC-BY)doi:10.3390/molecules26164998OpenAlex
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is curcumin and has gained importance in various treatments of various disorders such as antibacterial, antiprotozoal, cancer, obesity, diabetics and wound healing applications. Several techniques had been exploited as reported by researchers for increasing the therapeutic potential and its pharmacological activity. Here, the dictum is the new room for the development of physicochemical, as well as biological, studies for the efficacy in target specificity. Here, we discussed nanoformulation techniques, which lend support to upgrade the characters to the curcumin such as enhancing bioavailability, increasing solubility, modifying metabolisms, and target specificity, prolonged circulation, enhanced permeation. Our manuscript tried to seek the attention of the researcher by framing some solutions of some existing troubleshoots of this bioactive component for enhanced applications and making the formulations feasible at an industrial production scale. This manuscript focuses on recent inventions as well, which can further be implemented at the community level.
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Factors Affecting Preparation of Molecularly Imprinted Polymer and Methods on Finding Template-Monomer Interaction as the Key of Selective Properties of the Materials
Aliya Nur Hasanah, Nisa Safitri, Aulia Zulfa, Neli Neli, Driyanti Rahayu
238 citationsOpen access (CC-BY)doi:10.3390/molecules26185612OpenAlex
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Molecular imprinting is a technique for creating artificial recognition sites on polymer matrices that complement the template in terms of size, shape, and spatial arrangement of functional groups. The main advantage of Molecularly Imprinted Polymers (MIP) as the polymer for use with a molecular imprinting technique is that they have high selectivity and affinity for the target molecules used in the molding process. The components of a Molecularly Imprinted Polymer are template, functional monomer, cross-linker, solvent, and initiator. Many things determine the success of a Molecularly Imprinted Polymer, but the Molecularly Imprinted Polymer component and the interaction between template-monomers are the most critical factors. This review will discuss how to find the interaction between template and monomer in Molecularly Imprinted Polymer before polymerization and after polymerization and choose the suitable component for MIP development. Computer simulation, UV-Vis spectroscopy, Fourier Transform Infrared Spectroscopy (FTIR), Proton-Nuclear Magnetic Resonance (1H-NMR) are…
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Antibody–Drug Conjugates—A Tutorial Review
Stephanie Baah, Mark Laws, Khondaker Miraz Rahman
238 citationsOpen access (CC-BY)doi:10.3390/molecules26102943OpenAlex
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Antibody-drug conjugates (ADCs) are a family of targeted therapeutic agents for the treatment of cancer. ADC development is a rapidly expanding field of research, with over 80 ADCs currently in clinical development and eleven ADCs (nine containing small-molecule payloads and two with biological toxins) approved for use by the FDA. Compared to traditional small-molecule approaches, ADCs offer enhanced targeting of cancer cells along with reduced toxic side effects, making them an attractive prospect in the field of oncology. To this end, this tutorial review aims to serve as a reference material for ADCs and give readers a comprehensive understanding of ADCs; it explores and explains each ADC component (monoclonal antibody, linker moiety and cytotoxic payload) individually, highlights several EMA- and FDA-approved ADCs by way of case studies and offers a brief future perspective on the field of ADC research.
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The Role of Taurine in Mitochondria Health: More Than Just an Antioxidant
Chian Ju Jong, Priyanka Sandal, Stephen W. Schaffer
228 citationsOpen access (CC-BY)doi:10.3390/molecules26164913OpenAlex
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Taurine is a naturally occurring sulfur-containing amino acid that is found abundantly in excitatory tissues, such as the heart, brain, retina and skeletal muscles. Taurine was first isolated in the 1800s, but not much was known about this molecule until the 1990s. In 1985, taurine was first approved as the treatment among heart failure patients in Japan. Accumulating studies have shown that taurine supplementation also protects against pathologies associated with mitochondrial defects, such as aging, mitochondrial diseases, metabolic syndrome, cancer, cardiovascular diseases and neurological disorders. In this review, we will provide a general overview on the mitochondria biology and the consequence of mitochondrial defects in pathologies. Then, we will discuss the antioxidant action of taurine, particularly in relation to the maintenance of mitochondria function. We will also describe several reported studies on the current use of taurine supplementation in several mitochondria-associated pathologies in humans.
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Targeting the PI3K/AKT/mTOR Signaling Pathway in Lung Cancer: An Update Regarding Potential Drugs and Natural Products
Iksen Iksen, Sutthaorn Pothongsrisit, Varisa Pongrakhananon
228 citationsOpen access (CC-BY)doi:10.3390/molecules26134100OpenAlex
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Lung cancer is one of the most common cancers and has a high mortality rate. Due to its high incidence, the clinical management of the disease remains a major challenge. Several reports have documented a relationship between the phosphatidylinositol-3-kinase (PI3K)/ protein kinase B (AKT)/ mammalian target of rapamycin (mTOR) pathway and lung cancer. The recognition of this pathway as a notable therapeutic target in lung cancer is mainly due to its central involvement in the initiation and progression of the disease. Interest in using natural and synthetic medications to target these signaling pathways has increased in recent years, with promising results in vitro, in vivo, and in clinical trials. In this review, we focus on the current understanding of PI3K/AKT/mTOR signaling in tumor development. In addition to the signaling pathway, we highlighted the therapeutic potential of recently developed PI3K/AKT/mTOR inhibitors based on preclinical and clinical trials.
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l-Aspartate: An Essential Metabolite for Plant Growth and Stress Acclimation
Mei Han, Can Zhang, Peter Suglo, Shuyue Sun, Mingyao Wang and 1 more
225 citationsOpen access (CC-BY)doi:10.3390/molecules26071887OpenAlex
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L-aspartate (Asp) serves as a central building block, in addition to being a constituent of proteins, for many metabolic processes in most organisms, such as biosynthesis of other amino acids, nucleotides, nicotinamide adenine dinucleotide (NAD), the tricarboxylic acid (TCA) cycle and glycolysis pathway intermediates, and hormones, which are vital for growth and defense. In animals and humans, lines of data have proved that Asp is indispensable for cell proliferation. However, in plants, despite the extensive study of the Asp family amino acid pathway, little attention has been paid to the function of Asp through the other numerous pathways. This review aims to elucidate the most important aspects of Asp in plants, from biosynthesis to catabolism and the role of Asp and its metabolic derivatives in response to changing environmental conditions. It considers the distribution of Asp in various cell compartments and the change of Asp level, and its significance in the whole plant under various stresses. Moreover, it provides evidence of the interconnection between Asp and…
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Plant-Based Gums and Mucilages Applications in Pharmacology and Nanomedicine: A Review
Mohammad Sadegh Amiri, Vahideh Mohammadzadeh, Mohammad Ehsan Taghavizadeh Yazdi, Mahmood Barani, Abbas Rahdar and 1 more
224 citationsOpen access (CC-BY)doi:10.3390/molecules26061770OpenAlex
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Gums are carbohydrate biomolecules that have the potential to bind water and form gels. Gums are regularly linked with proteins and minerals in their construction. Gums have several forms, such as mucilage gums, seed gums, exudate gums, etc. Plant gums are one of the most important gums because of their bioavailability. Plant-derived gums have been used by humans since ancient times for numerous applications. The main features that make them appropriate for use in different applications are high stabilization, viscosity, adhesive property, emulsification action, and surface-active activity. In many pharmaceutical formulations, plant-based gums and mucilages are the key ingredients due to their bioavailability, widespread accessibility, non-toxicity, and reasonable prices. These compete with many polymeric materials for use as different pharmaceuticals in today's time and have created a significant achievement from being an excipient to innovative drug carriers. In particular, scientists and pharmacy industries around the world have been drawn to uncover the secret potential of…
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Lignans of Sesame (Sesamum indicum L.): A Comprehensive Review
Mebeaselassie Andargie, María Viñas, Anna Rathgeb, Evelyn Möller, Petr Karlovský
221 citationsOpen access (CC-BY)doi:10.3390/molecules26040883OpenAlex
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Major lignans of sesame sesamin and sesamolin are benzodioxol--substituted furofurans. Sesamol, sesaminol, its epimers, and episesamin are transformation products found in processed products. Synthetic routes to all lignans are known but only sesamol is synthesized industrially. Biosynthesis of furofuran lignans begins with the dimerization of coniferyl alcohol, followed by the formation of dioxoles, oxidation, and glycosylation. Most genes of the lignan pathway in sesame have been identified but the inheritance of lignan content is poorly understood. Health-promoting properties make lignans attractive components of functional food. Lignans enhance the efficiency of insecticides and possess antifeedant activity, but their biological function in plants remains hypothetical. In this work, extensive literature including historical texts is reviewed, controversial issues are critically examined, and errors perpetuated in literature are corrected. The following aspects are covered: chemical properties and transformations of lignans; analysis, purification, and total synthesis; occurrence…
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Review of Functional and Pharmacological Activities of Berries
Оксана Головинская, Chin‐Kun Wang
220 citationsOpen access (CC-BY)doi:10.3390/molecules26133904OpenAlex
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Functional plant-based foods (such as fruits, vegetables, and berries) can improve health, have a preventive effect, and diminish the risk of different chronic diseases during in vivo and in vitro studies. Berries contain many phytochemicals, fibers, vitamins, and minerals. The primary phytochemicals in berry fruits are phenolic compounds including flavonoids (anthocyanins, flavonols, flavones, flavanols, flavanones, and isoflavonoids), tannins, and phenolic acids. Since berries have a high concentration of polyphenols, it is possible to use them for treating various diseases pharmacologically by acting on oxidative stress and inflammation, which are often the leading causes of diabetes, neurological, cardiovascular diseases, and cancer. This review examines commonly consumed berries: blackberries, blackcurrants, blueberries, cranberries, raspberries, black raspberries, and strawberries and their polyphenols as potential medicinal foods (due to the presence of pharmacologically active compounds) in the treatment of diabetes, cardiovascular problems, and other diseases. Moreover,…
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Biological Effects of Quinolones: A Family of Broad-Spectrum Antimicrobial Agents
Ana R. Millanao, Aracely Y. Mora, Nicolás A. Villagra, Sergio A. Bucarey, Alejandro A. Hidalgo
219 citationsOpen access (CC-BY)doi:10.3390/molecules26237153OpenAlex
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Broad antibacterial spectrum, high oral bioavailability and excellent tissue penetration combined with safety and few, yet rare, unwanted effects, have made the quinolones class of antimicrobials one of the most used in inpatients and outpatients. Initially discovered during the search for improved chloroquine-derivative molecules with increased anti-malarial activity, today the quinolones, intended as antimicrobials, comprehend four generations that progressively have been extending antimicrobial spectrum and clinical use. The quinolone class of antimicrobials exerts its antimicrobial actions through inhibiting DNA gyrase and Topoisomerase IV that in turn inhibits synthesis of DNA and RNA. Good distribution through different tissues and organs to treat Gram-positive and Gram-negative bacteria have made quinolones a good choice to treat disease in both humans and animals. The extensive use of quinolones, in both human health and in the veterinary field, has induced a rise of resistance and menace with leaving the quinolones family ineffective to treat infections. This review revises…
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The New Challenge of Green Cosmetics: Natural Food Ingredients for Cosmetic Formulations
Irene Dini, Sonia Laneri
217 citationsOpen access (CC-BY)doi:10.3390/molecules26133921OpenAlex
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Nowadays, much attention is paid to issues such as ecology and sustainability. Many consumers choose "green cosmetics", which are environmentally friendly creams, makeup, and beauty products, hoping that they are not harmful to health and reduce pollution. Moreover, the repeated mini-lock downs during the COVID-19 pandemic have fueled the awareness that body beauty is linked to well-being, both external and internal. As a result, consumer preferences for makeup have declined, while those for skincare products have increased. Nutricosmetics, which combines the benefits derived from food supplementation with the advantages of cosmetic treatments to improve the beauty of our body, respond to the new market demands. Food chemistry and cosmetic chemistry come together to promote both inside and outside well-being. A nutricosmetic optimizes the intake of nutritional microelements to meet the needs of the skin and skin appendages, improving their conditions and delaying aging, thus helping to protect the skin from the aging action of environmental factors. Numerous studies in the…
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Imidazoles as Potential Anticancer Agents: An Update on Recent Studies
Pankaj Sharma, Chris LaRosa, Janet Antwi, Rajgopal Govindarajan, Karl A. Werbovetz
212 citationsOpen access (CC-BY)doi:10.3390/molecules26144213OpenAlex
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Nitrogen-containing heterocyclic rings are common structural components of marketed drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide range of bioactive compounds. The unique properties of such structures, including high polarity and the ability to participate in hydrogen bonding and coordination chemistry, allow them to interact with a wide range of biomolecules, and imidazole-/fused imidazole-containing compounds are reported to have a broad spectrum of biological activities. This review summarizes recent reports of imidazole/fused imidazole derivatives as anticancer agents appearing in the peer-reviewed literature from 2018 through 2020. Such molecules have been shown to modulate various targets, including microtubules, tyrosine and serine-threonine kinases, histone deacetylases, p53-Murine Double Minute 2 (MDM2) protein, poly (ADP-ribose) polymerase (PARP), G-quadraplexes, and other targets. Imidazole-containing compounds that display anticancer activity by unknown/undefined mechanisms are also described, as well as key features of…
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Melatonin in Cancer Treatment: Current Knowledge and Future Opportunities
Wamidh H. Talib, Ahmad Riyad Alsayed, Alaa Abuawad, Safa Daoud, Asma Ismail Mahmod
211 citationsOpen access (CC-BY)doi:10.3390/molecules26092506OpenAlex
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Melatonin is a pleotropic molecule with numerous biological activities. Epidemiological and experimental studies have documented that melatonin could inhibit different types of cancer in vitro and in vivo. Results showed the involvement of melatonin in different anticancer mechanisms including apoptosis induction, cell proliferation inhibition, reduction in tumor growth and metastases, reduction in the side effects associated with chemotherapy and radiotherapy, decreasing drug resistance in cancer therapy, and augmentation of the therapeutic effects of conventional anticancer therapies. Clinical trials revealed that melatonin is an effective adjuvant drug to all conventional therapies. This review summarized melatonin biosynthesis, availability from natural sources, metabolism, bioavailability, anticancer mechanisms of melatonin, its use in clinical trials, and pharmaceutical formulation. Studies discussed in this review will provide a solid foundation for researchers and physicians to design and develop new therapies to treat and prevent cancer using melatonin.
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Plant Secondary Metabolites: An Opportunity for Circular Economy
Ilaria Chiocchio, Manuela Mandrone, Paola Tomasi, Lorenzo Marincich, Ferruccio Poli
209 citationsOpen access (CC-BY)doi:10.3390/molecules26020495OpenAlex
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Moving toward a more sustainable development, a pivotal role is played by circular economy and a smarter waste management. Industrial wastes from plants offer a wide spectrum of possibilities for their valorization, still being enriched in high added-value molecules, such as secondary metabolites (SMs). The current review provides an overview of the most common SM classes (chemical structures, classification, biological activities) present in different plant waste/by-products and their potential use in various fields. A bibliographic survey was carried out, taking into account 99 research articles (from 2006 to 2020), summarizing all the information about waste type, its plant source, industrial sector of provenience, contained SMs, reported bioactivities, and proposals for its valorization. This survey highlighted that a great deal of the current publications are focused on the exploitation of plant wastes in human healthcare and food (including cosmetic, pharmaceutical, nutraceutical and food additives). However, as summarized in this review, plant SMs also possess an enormous…
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Anticancer Properties of Eugenol: A Review
Ali T. Zari, Talal A. Zari, Khalid Rehman Hakeem
208 citationsOpen access (CC-BY)doi:10.3390/molecules26237407OpenAlex
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Conventional cancer treatments have shown several unfavourable adverse effects, as well as an increase in anticancer drug resistance, which worsens the impending cancer therapy. Thus, the emphasis is currently en route for natural products. There is currently great interest in the natural bioactive components from medicinal plants possessing anticancer characteristics. For example, clove (Syzygium aromaticum L.) (Family Myrtaceae) is a highly prized spice that has been historically utilized as a food preservative and for diverse medical uses. It is reckoned amongst the valued sources of phenolics. It is indigenous to Indonesia but currently is cultivated in various places of the world. Among diverse active components, eugenol, the principal active component of S. aromaticum, has optimistic properties comprising antioxidant, anti-inflammatory, and anticancer actions. Eugenol (4-allyl-2-methoxyphenol) is a musky oil that is mainly obtained from clove. It has long been utilized all over the world as a result of its broad properties like antioxidant, anticancer, anti-inflammatory, and…
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T-2 Toxin—The Most Toxic Trichothecene Mycotoxin: Metabolism, Toxicity, and Decontamination Strategies
Edyta Janik, Marcin Niemcewicz, Marcin Podogrocki, Michał Ceremuga, Maksymilian Stela and 1 more
207 citationsOpen access (CC-BY)doi:10.3390/molecules26226868OpenAlex
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species. Moreover, T-2 is the most common cause of poisoning that results from the consumption of contaminated cereal-based food and feed reported among humans and animals. The food and feed most contaminated with T-2 toxin is made from wheat, barley, rye, oats, and maize. After exposition or ingestion, T-2 is immediately absorbed from the alimentary tract or through the respiratory mucosal membranes and transported to the liver as a primary organ responsible for toxin's metabolism. Depending on the age, way of exposure, and dosage, intoxication manifests by vomiting, feed refusal, stomach necrosis, and skin irritation, which is rarely observed in case of mycotoxins intoxication. In order to eliminate T-2 toxin, various decontamination techniques have been found to mitigate the concentration of T-2 toxin in agricultural commodities. However, it is believed that 100% degradation of this toxin could be not possible. In this review, T-2 toxin toxicity, metabolism, and decontamination strategies are presented and discussed.
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Hybrid Drugs—A Strategy for Overcoming Anticancer Drug Resistance?
Marta Szumilak, Anna Wiktorowska‐Owczarek, Andrzej Stańczak
205 citationsOpen access (CC-BY)doi:10.3390/molecules26092601OpenAlex
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Despite enormous progress in the treatment of many malignancies, the development of cancer resistance is still an important reason for cancer chemotherapy failure. Increasing knowledge of cancers' molecular complexity and mechanisms of their resistance to anticancer drugs, as well as extensive clinical experience, indicate that an effective fight against cancer requires a multidimensional approach. Multi-target chemotherapy may be achieved using drugs combination, co-delivery of medicines, or designing hybrid drugs. Hybrid drugs simultaneously targeting many points of signaling networks and various structures within a cancer cell have been extensively explored in recent years. The single hybrid agent can modulate multiple targets involved in cancer cell proliferation, possesses a simpler pharmacokinetic profile to reduce the possibility of drug interactions occurrence, and facilitates the process of drug development. Moreover, a single medication is expected to enhance patient compliance due to a less complicated treatment regimen, as well as a diminished number of adverse reactions…
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Propolis Extract and Its Bioactive Compounds—From Traditional to Modern Extraction Technologies
Jelena Šuran, Ivica Cepanec, Tomislav Mašek, Božo Radić, Saša Radić and 2 more
204 citationsOpen access (CC-BY)doi:10.3390/molecules26102930OpenAlex
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Propolis is a honeybee product known for its antioxidant, anti-inflammatory, anticancer, and antimicrobial effects. It is rich in bioactive molecules whose content varies depending on the botanical and geographical origin of propolis. These bioactive molecules have been studied individually and as a part of propolis extracts, as they can be used as representative markers for propolis standardization. Here, we compare the pharmacological effects of representative polyphenols and whole propolis extracts. Based on the literature data, polyphenols and extracts act by suppressing similar targets, from pro-inflammatory TNF/NF-κB to the pro-proliferative MAPK/ERK pathway. In addition, they activate similar antioxidant mechanisms of action, like Nrf2-ARE intracellular antioxidant pathway, and they all have antimicrobial activity. These similarities do not imply that we should attribute the action of propolis solely to the most representative compounds. Moreover, its pharmacological effects will depend on the efficacy of these compounds' extraction. Thus, we also give an overview of…
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Neuroprotective Potential of Limonene and Limonene Containing Natural Products
Lujain Bader Eddin, Niraj Kumar Jha, Mohamed Fizur Nagoor Meeran, Kavindra Kumar Kesari, Rami Beiram and 1 more
203 citationsOpen access (CC-BY)doi:10.3390/molecules26154535OpenAlex
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, showing several biological properties such as antioxidant, anti-inflammatory, anticancer, antinociceptive and gastroprotective characteristics. Recently, there is notable interest in investigating the pharmacological effects of limonene in various chronic diseases due to its mitigating effect on oxidative stress and inflammation and regulating apoptotic cell death. There are several available studies demonstrating the neuroprotective role of limonene in neurodegenerative diseases, including Alzheimer's disease, multiple sclerosis, epilepsy, anxiety, and stroke. The high abundance of limonene in nature, its safety profile, and various mechanisms of action make this monoterpene a favorable molecule to be developed as a nutraceutical for preventive purposes and as an alternative agent or adjuvant to modern therapeutic drugs in curbing the onset and progression of neurodegenerative diseases. This manuscript presents a comprehensive review of the available scientific literature discussing the pharmacological activities of limonene or plant products containing limonene which attribute…
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Electrochemical Biosensors in Food Safety: Challenges and Perspectives
Antonella Curulli
201 citationsOpen access (CC-BY)doi:10.3390/molecules26102940OpenAlex
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Safety and quality are key issues for the food industry. Consequently, there is growing demand to preserve the food chain and products against substances toxic, harmful to human health, such as contaminants, allergens, toxins, or pathogens. For this reason, it is mandatory to develop highly sensitive, reliable, rapid, and cost-effective sensing systems/devices, such as electrochemical sensors/biosensors. Generally, conventional techniques are limited by long analyses, expensive and complex procedures, and skilled personnel. Therefore, developing performant electrochemical biosensors can significantly support the screening of food chains and products. Here, we report some of the recent developments in this area and analyze the contributions produced by electrochemical biosensors in food screening and their challenges.
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Edible Mushrooms as Functional Ingredients for Development of Healthier and More Sustainable Muscle Foods: A Flexitarian Approach
Arun Kumar Das, Pramod Kumar Nanda, Premanshu Dandapat, Samiran Bandyopadhyay, Patricia Gullón and 4 more
201 citationsOpen access (CC-BY)doi:10.3390/molecules26092463OpenAlex
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Consumers are increasingly interested in nutritious, safe and healthy muscle food products with reduced salt and fat that benefit their well-being. Hence, food processors are constantly in search of natural bioactive ingredients that offer health benefits beyond their nutritive values without affecting the quality of the products. Mushrooms are considered as next-generation healthy food components. Owing to their low content of fat, high-quality proteins, dietary fibre and the presence of nutraceuticals, they are ideally preferred in formulation of low-caloric functional foods. There is a growing trend to fortify muscle food with edible mushrooms to harness their goodness in terms of nutritive, bioactive and therapeutic values. The incorporation of mushrooms in muscle foods assumes significance, as it is favourably accepted by consumers because of its fibrous structure that mimics the texture with meat analogues offering unique taste and umami flavour. This review outlines the current knowledge in the literature about the nutritional richness, functional bioactive compounds and…
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Structural Diversity of Ubiquitin E3 Ligase
Sachiko Toma-Fukai, Toshiyuki Shimizu
200 citationsOpen access (CC-BY)doi:10.3390/molecules26216682OpenAlex
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The post-translational modification of proteins regulates many biological processes. Their dysfunction relates to diseases. Ubiquitination is one of the post-translational modifications that target lysine residue and regulate many cellular processes. Three enzymes are required for achieving the ubiquitination reaction: ubiquitin-activating enzyme (E1), ubiquitin-conjugating enzyme (E2), and ubiquitin ligase (E3). E3s play a pivotal role in selecting substrates. Many structural studies have been conducted to reveal the molecular mechanism of the ubiquitination reaction. Recently, the structure of PCAF_N, a newly categorized E3 ligase, was reported. We present a review of the recent progress toward the structural understanding of E3 ligases.
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Modern Carbon–Based Materials for Adsorptive Removal of Organic and Inorganic Pollutants from Water and Wastewater
Vera I. Isaeva, M. D. Vedenyapina, Alexandra Yu. Kurmysheva, Dirk Weichgrebe, Rahul Ramesh Nair and 2 more
200 citationsOpen access (CC-BY)doi:10.3390/molecules26216628OpenAlex
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Currently, a serious threat for living organisms and human life in particular, is water contamination with persistent organic and inorganic pollutants. To date, several techniques have been adopted to remove/treat organics and toxic contaminants. Adsorption is one of the most effective and economical methods for this purpose. Generally, porous materials are considered as appropriate adsorbents for water purification. Conventional adsorbents such as activated carbons have a limited possibility of surface modification (texture and functionality), and their adsorption capacity is difficult to control. Therefore, despite the significant progress achieved in the development of the systems for water remediation, there is still a need for novel adsorptive materials with tunable functional characteristics. This review addresses the new trends in the development of new adsorbent materials. Herein, modern carbon-based materials, such as graphene, oxidized carbon, carbon nanotubes, biomass-derived carbonaceous matrices-biochars as well as their composites with metal-organic frameworks (MOFs)…
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Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism
Mohammed A. S. Abourehab, Alaa Mohammad Alqahtani, Bahaa G. M. Youssif, Ahmed M. Gouda
198 citationsOpen access (CC-BY)doi:10.3390/molecules26216677OpenAlex
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Targeting the EGFR with small-molecule inhibitors is a confirmed valid strategy in cancer therapy. Since the FDA approval of the first EGFR-TKI, erlotinib, great efforts have been devoted to the discovery of new potent inhibitors. Until now, fourteen EGFR small-molecule inhibitors have been globally approved for the treatment of different types of cancers. Although these drugs showed high efficacy in cancer therapy, EGFR mutations have emerged as a big challenge for these drugs. In this review, we focus on the EGFR small-molecule inhibitors that have been approved for clinical uses in cancer therapy. These drugs are classified based on their chemical structures, target kinases, and pharmacological uses. The synthetic routes of these drugs are also discussed. The crystal structures of these drugs with their target kinases are also summarized and their bonding modes and interactions are visualized. Based on their binding interactions with the EGFR, these drugs are also classified into reversible and irreversible inhibitors. The cytotoxicity of these drugs against different types of…
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A Review on Current Status of Biochar Uses in Agriculture
Tara Allohverdi, Amar Kumar Mohanty, Poritosh Roy, Manjusri Misra
197 citationsOpen access (CC-BY)doi:10.3390/molecules26185584OpenAlex
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In a time when climate change increases desertification and drought globally, novel and effective solutions are required in order to continue food production for the world's increasing population. Synthetic fertilizers have been long used to improve the productivity of agricultural soils, part of which leaches into the environment and emits greenhouse gasses (GHG). Some fundamental challenges within agricultural practices include the improvement of water retention and microbiota in soils, as well as boosting the efficiency of fertilizers. Biochar is a nutrient rich material produced from biomass, gaining attention for soil amendment purposes, improving crop yields as well as for carbon sequestration. This study summarizes the potential benefits of biochar applications, placing emphasis on its application in the agricultural sector. It seems biochar used for soil amendment improves nutrient density of soils, water holding capacity, reduces fertilizer requirements, enhances soil microbiota, and increases crop yields. Additionally, biochar usage has many environmental benefits,…
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Gingival Crevicular Fluid (GCF): A Diagnostic Tool for the Detection of Periodontal Health and Diseases
Tauqeer Bibi, Zohaib Khurshid, Ambreen Rehman, Eisha Imran, Kumar Chandan Srivastava and 1 more
197 citationsOpen access (CC-BY)doi:10.3390/molecules26051208OpenAlex
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The methodologies applicable for the evaluation of periodontal associated diseases are constantly evolving to provide quick, realistic, and scientifically proven results. Trends in the past followed a clinical evaluation of periodontal tissues and radiographic-based reports that formed the foundation for detection of diseases involving the structures supporting the teeth. As the confines and limitations of conventional strategies became obvious over the passage of time, hand in hand variety of techniques have evolved and experimentally justified. These improvisations are based on an improved understanding of the periodontal-pathogenic cascade. Periodontal pathogenesis and a paradigm shift from disease understanding to disease prevention and treatment entail few prerequisites that demand the objectivity of diagnostics procedure that includes sensitivity and specificity along with an explanation of the intensity of the disease, Gingival crevicular fluid an oral bio-fluid resides in the close proximity with gingival tissues have been widely used to understand and differentiate the…
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Biocide Use in the Antimicrobial Era: A Review
Imogen Anne Jones, Lovleen Tina Joshi
192 citationsOpen access (CC-BY)doi:10.3390/molecules26082276OpenAlex
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Biocides are widely used in healthcare and industry to control infections and microbial contamination. Ineffectual disinfection of surfaces and inappropriate use of biocides can result in the survival of microorganisms such as bacteria and viruses on inanimate surfaces, often contributing to the transmission of infectious agents. Biocidal disinfectants employ varying modes of action to kill microorganisms, ranging from oxidization to solubilizing lipids. This review considers the main biocides used within healthcare and industry environments and highlights their modes of action, efficacy and relevance to disinfection of pathogenic bacteria. This information is vital for rational use and development of biocides in an era where microorganisms are becoming resistant to chemical antimicrobial agents.
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Microorganisms: A Potential Source of Bioactive Molecules for Antioxidant Applications
Alka Rani, Khem Chand Saini, Felix Bast, Sanjeet Mehariya, Shashi Kant Bhatia and 2 more
192 citationsOpen access (CC-BY)doi:10.3390/molecules26041142OpenAlex
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Oxidative stress is an elevated intracellular level of free oxygen radicals that cause lipid peroxidation, protein denaturation, DNA hydroxylation, and apoptosis, ultimately negotiating cells viability. Antioxidants can scavenge such free radicals, thus reducing the oxidative stress and eventually prevent cellular damage. Medicinal plants, fruits, and spices remain the prioritized sources of antioxidants and antimicrobial properties since the time immemorial, but in contrast to plants, microorganisms can be grown at a faster rate under controlled conditions. They are non-toxic, non-carcinogenic, and biodegradable as compared to synthetic antioxidants. Microorganisms including actinomycetes, archaea, bacteria, protozoa, yeast, and fungi are auspicious source of vital bioactive compounds. The list comprises ample of bioactive components from microorganisms. One of them is bacteriocins, which are ribosomally synthesized antimicrobial peptides product of Eurotium sp., Streptomyces parvulus, S. thermophiles, Lactococcus lactis, etc. It has a great potential as next-generation antibiotics…
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The Second Life of Citrus Fruit Waste: A Valuable Source of Bioactive Compounds
Caterina Russo, Alessandro Maugeri, Giovanni Enrico Lombardo, Laura Musumeci, Davide Barreca and 3 more
190 citationsOpen access (CC-BY)doi:10.3390/molecules26195991OpenAlex
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fruits (CF) are among the most widely cultivated fruit crops throughout the world and their production is constantly increasing along with consumers' demand. Therefore, huge amounts of waste are annually generated through CF processing, causing high costs for their disposal, as well as environmental and human health damage, if inappropriately performed. According to the most recent indications of an economic, environmental and pharmaceutical nature, CF processing residues must be transformed from a waste to be disposed to a valuable resource to be reused. Based on a circular economy model, CF residues (i.e., seeds, exhausted peel, pressed pulp, secondary juice and leaves) have increasingly been re-evaluated to also obtain, but not limited to, valuable compounds to be employed in the food, packaging, cosmetic and pharmaceutical industries. However, the use of CF by-products is still limited because of their underestimated nutritional and economic value, hence more awareness and knowledge are needed to overcome traditional approaches for their disposal. This review summarizes recent…
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The cohort is every article, review and book chapter OpenAlex attributes to Molecules with publication year 2021, 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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