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Current Topics in Medicinal Chemistry 2024
Topics: Humans; Phytochemicals
PubMed: 38842097
DOI: 10.2174/156802662409240325005442 -
Scientific Reports Aug 2023In this study, we investigated whether zerumbone (ZBN), ellagic acid (ELA) and quercetin (QCT), the plant-derived components, can modulate the role of COX-3 or cytokines...
In this study, we investigated whether zerumbone (ZBN), ellagic acid (ELA) and quercetin (QCT), the plant-derived components, can modulate the role of COX-3 or cytokines liable in arthritic disorder. Initially, the effect of ZBN, ELA, and QCT on inflammatory process was investigated using in-vitro models. In-silico docking and molecular dynamics study of these molecules with respective targets also corroborate with in-vitro studies. Further, the in-vivo anti-arthritic potential of these molecules in Complete Freund's adjuvant (CFA)-induced arthritic rats was confirmed. CFA increases in TNF-α and IL-1β levels in the arthritic control animals were significantly (***p < 0.001) attenuated in the ZBN- and ELA-treated animals. CFA-induced attenuation in IL-10 levels recovered under treatment. Moreover, ELA attenuated CFA-induced upregulation of COX-3 and ZBN downregulated CFA-triggered NFκB expression in arthritic animals. The bonding patterns of zerumbone in the catalytic sites of targets provide a useful hint in designing and developing suitable derivatives that can be used as a potential drug. To our best knowledge, the first time we are reporting the role of COX-3 in the treatment of arthritic disorders which could provide a novel therapeutic approach for the treatment of inflammatory disorders.
Topics: Animals; Rats; NF-kappa B; Arthritis; Cytokines; Ellagic Acid; Freund's Adjuvant; Phytochemicals
PubMed: 37604838
DOI: 10.1038/s41598-023-37729-2 -
Neurochemistry International Nov 2023Parkinson's disease (PD) is one of the most prevalent neuroinflammatory illnesses, characterized by the progressive loss of neurons in the brain. Proinflammatory... (Review)
Review
Parkinson's disease (PD) is one of the most prevalent neuroinflammatory illnesses, characterized by the progressive loss of neurons in the brain. Proinflammatory cytokines play a key role in initiating and perpetuating neuroinflammation, which can lead to the activation of glial cells and the deregulation of inflammatory pathways, ultimately leading to permanent brain damage. Currently, available drugs for PD mostly alleviate symptoms but do not target underlying inflammatory processes. There is a growing interest in exploring the potential of phytochemicals to mitigate neuroinflammation. Phytochemicals such as resveratrol, apigenin, catechin, anthocyanins, amentoflavone, quercetin, berberine, and genistein have been studied for their ability to scavenge free radicals and reduce proinflammatory cytokine levels in the brain. These plant-derived compounds offer a natural and potentially safe alternative to conventional drugs for managing neuroinflammation in PD and other neurodegenerative diseases. However, further research is necessary to elucidate their underlying mechanisms of action and clinical effectiveness. So, this review delves into the pathophysiology of PD and its intricate relationship with proinflammatory cytokines, and explores how their insidious contributions fuel the disease's initiation and progression via cytokine-dependent signaling pathways. Additionally, we tried to give an account of PD management using existing drugs along with their limitations. Furthermore, our aim is to provide a thorough overview of the diverse groups of phytochemicals, their plentiful sources, and the current understanding of their anti-neuroinflammatory properties. Through this exploration, we posit the innovative idea that consuming nutrient-rich phytochemicals could be an effective approach to preventing and treating PD.
Topics: Humans; Parkinson Disease; Cytokines; Neuroinflammatory Diseases; Anthocyanins; Phytochemicals
PubMed: 37683836
DOI: 10.1016/j.neuint.2023.105604 -
Chemistry & Biodiversity May 2024Fruits and vegetables serve not only as sources of nutrition but also as medicinal agents for the treatment of diverse diseases and maladies. These dietary components... (Review)
Review
Fruits and vegetables serve not only as sources of nutrition but also as medicinal agents for the treatment of diverse diseases and maladies. These dietary components are significant resources of phytochemicals that demonstrate therapeutic properties against many illnesses. Fraxin is a naturally occurring coumarin glycoside mainly present in various species of Fraxinus genera, having a multitude of therapeutic uses against various diseases and disorders. This study focuses to investigate the pharmacological activities, botanical sources, and biopharmaceutical profile of the phytochemical fraxin based on different preclinical and non-clinical studies to show the scientific evidence and to evaluate the underlying molecular mechanisms of the therapeutic effects against various ailments. For this, data was searched and collected (as of February 15, 2024) in a variety of credible electronic databases, including PubMed/Medline, Scopus, Springer Link, ScienceDirect, Wiley Online, Web of Science, and Google Scholar. The findings demonstrated favorable outcomes in relation to a range of diseases or medical conditions, including inflammation, neurodegenerative disorders such as cerebral ischemia-reperfusion (I/R) and depression, viral infection, as well as diabetic nephropathy. The phytochemical also showed protective effects such as osteoprotective, renoprotective, pulmoprotective, hepatoprotective, and gastroprotective effects due to its antioxidant capacity. Fraxin has a great capability to diminish oxidative stress-related damage in different organs by stimulating the antioxidant enzymes, downregulating nuclear factor kappa B and NLRP3, and triggering the Nrf2/ARE signaling pathways. Fraxin exhibited poor oral bioavailability because of reduced absorption and a wide distribution into tissues of different organs. However, extensive research is required to decipher the biopharmaceutical profiles, and clinical studies are necessary to establish the efficacy of the natural compound as a reliable therapeutic agent.
Topics: Humans; Animals; Phytochemicals; Furocoumarins; Antioxidants
PubMed: 38506600
DOI: 10.1002/cbdv.202301615 -
Journal of Ethnopharmacology Jan 2024Dried root tubers of L.aggregata have been widely used in Chinese herbal medicine for thousands of years to promote qi, relieve pain, warm kidney, and disperse cold. (Review)
Review
ETHNOPHARMACOLOGICAL RELEVANCE
Dried root tubers of L.aggregata have been widely used in Chinese herbal medicine for thousands of years to promote qi, relieve pain, warm kidney, and disperse cold.
AIM OF THE STUDY
This review aims to assess the research progress of L.aggregata, to comprehensively understand its development status, to point out the shortcomings of the existing researches, and to provide reference for further research on L.aggregata.
MATERIALS AND METHODS
By searching various databases for literatures on "Lindera aggregata", "Linderae Radix" and "Lindera strychnifolia", as well as relevant textbooks and digital documents, an overall and critical review of the subject was conducted.
RESULTS
Through phytochemical studies on different parts of L.aggregata, about 260 compounds were isolated, including flavonoids, alkaloids, terpenes, volatile oils, and other compounds. A large number of in vivo and in vitro studies have shown that L.aggregata has a plethora of pharmacological effects such as anti-cancer, anti-arthritis, anti-bacterial, anti-oxidation, anti-diabetic nephropathy, hepatoprotective, lipid-lowering effect and so on.
CONCLUSION
While the pharmacological effects of L.aggregata have been confirmed, most studies only use simple in vitro cell lines or animal disease models to evaluate their pharmacological activities. Therefore, future research should be conducted in a more comprehensive clinical manner. Further pharmacological research is also necessary to fully clarify the action mechanism of L.aggregata. It is also interesting to note that L.aggregata is often used to treat frequent urination in ancient times, but its molecular basis and mechanism of action are still unclear, and systematic studies are lacking. In terms of quality control, the source of L.aggregata is single, mostly wild, and the main medicinal part of L.aggregata is the tuber, while the yield of straight root is large. Therefore, further attention should be paid to the rapid propagation technology of L.aggregata and whether straight root can be included in medicinal use. It is also worth thinking whether sulfur-fumigation is necessary for preserving L.aggregata. As vinegar-processing is a common processing method for L. aggregata, the mechanism of such processing method remains to be investigated. In addition, in-depth research on the pharmacokinetics and long-term toxicity of L.aggregata is necessary to ensure its efficacy and safety.
Topics: Animals; Ethnopharmacology; Lindera; Phytochemicals; Oils, Volatile; Quality Control; Phytotherapy
PubMed: 37499843
DOI: 10.1016/j.jep.2023.116954 -
Molecules (Basel, Switzerland) Dec 2023(Dunn) Pimenov, commonly known as Qianhu in China, is a widely used folk Chinese herbal medicine. This article reviews its botanical traits, ethnopharmacology,... (Review)
Review
(Dunn) Pimenov, commonly known as Qianhu in China, is a widely used folk Chinese herbal medicine. This article reviews its botanical traits, ethnopharmacology, cultivation techniques, identification, phytochemical compositions, and pharmacological effects. Over 70 coumarin compounds, including simple coumarins, pyranocoumarins, and furanocoumarins, have been isolated within this plant. Additionally, contains other components such as flavonoids, fatty acids, benzoic acids, and sterols. This information highlights the importance of utilizing active ingredients and excavating pharmacological effects. With its remarkable versatility, exhibits a wide range of pharmacological effects. It has been found to possess expectorant and bronchodilator properties, cardiovascular protection, antimicrobial and antioxidant activities, anti-tumor effects, and even antidiabetic properties. It is recommended to focus on the development of new drugs that leverage the active ingredients of and explore its potential for new clinical applications and holistic utilization.
Topics: Medicine, Chinese Traditional; Ethnopharmacology; Drugs, Chinese Herbal; Coumarins; Pyranocoumarins; Phytochemicals; Apiaceae; Plant Extracts
PubMed: 38138641
DOI: 10.3390/molecules28248153 -
PloS One 2023Centranthus kellereri is a Bulgarian endemic plant species, found only in two locations in the world: The Balkans Mountains (Stara Planina), above the town of Vratsa,...
Phytochemical and biological investigations on Centranthus kellereri (Stoj., Stef. & T. Georgiev) Stoj. & Stef. and C. ruber (L.) DC. and their potential as new medicinal and ornamental plants.
INTRODUCTION
Centranthus kellereri is a Bulgarian endemic plant species, found only in two locations in the world: The Balkans Mountains (Stara Planina), above the town of Vratsa, and The Pirin Mountains, above the town of Bansko, Bulgaria. Being endemic and endangered species precluded any significant research on it. The hypothesis of this study was that the populations of C. kellereri may represent genetically, phytochemically, and morphologically distinct forms and these will differentiate from C. ruber. Furthermore, C. kellereri possibly imperfect embryology may preclude its more widespread distribution under natural conditions.
RESULTS
This study revealed the phytochemical profile, antioxidant activity, embryology, surface microstructural morphological traits, and genetic differences between the C. kellereri plants from the only two natural populations and compares them to the ones of the related and better-known plant C. ruber. The essential oil (EO) content in aboveground plant parts and in roots was generally low and the EO composition varied significantly as a function of plant part, year of sampling, location, and species. Methylvaleric acid was a major EO constituent in the C. kellereri EO, ranging between 60.2% and 71.7% of the total EO. The EO included monoterpenes, sequiterpenes, long-chain alkanes and fatty acids. Phytochemical analyses of plant tissue revealed the occurrence of 32 compounds that were tentatively identified as 6 simple phenolics, 18 flavonoids, 1 quinone, 1 lipid, 1 alkaloid, 2 diterpenes, and 3 triterpenes. There were differences in detected compounds between the C. kellereri plants at the two locations and between the roots and shoots in both species. The total phenols and flavonoids varied between the two species but were also dissimilar between the plants from the two populations of C. kelleri. Free radical scavenging activity, measured with ABTS and DPPH in aqueous and methanol extracts, had similar values; however, overall, C. kellereri from Vratsa showed the highest antioxidant activity while C. ruber had the lowest activity. Genetic analyses showed a clear differentiation between C. kellereri and C. ruber, and between the two populations of C. kellereri. Embryological studies revealed the peculiarities of the male and female generative spheres of the two species that were defined as being sexually reproducing. The pollen had high viability; however, the low viability of seeds demonstrated possible high sensitivity of C. kellereri to the environmental conditions, perhaps the main factor modifying and restricting the population sizes. The SEM analyses exposed differences in surface microstructural traits between the species (C. kellereri and C. ruber) but also between the two populations of C. kellereri. The observed dissimilarities in genetic makeup, micromorphological characteristics, and phytochemical composition strongly indicate that the two populations can be classified as distinct subspecies or varieties of C. kellereri; var. pirinensis and var. balkanensis. Further research is needed to introduce C. kellereri into culture and develop it as a high-value specialty crop or ornamental in order to conserve C. kellereri natural populations. C. kellereri may be utilized as a source for phytochemicals of interest and as an ornamental plant like C. ruber; however, it may have a greater environmental plasticity and adaptation as evidenced by its current locations.
Topics: Antioxidants; Plant Extracts; Phytochemicals; Oils, Volatile; Phenols; Flavonoids
PubMed: 37934763
DOI: 10.1371/journal.pone.0293877 -
Fitoterapia Jul 2024The genus Antidesma L. (Phyllanthaceae) consists of 102 species and is distributed throughout the subtropical, temperate, and subpolar regions. Numerous species in this... (Review)
Review
The genus Antidesma L. (Phyllanthaceae) consists of 102 species and is distributed throughout the subtropical, temperate, and subpolar regions. Numerous species in this genus are employed in ethnomedical practices to treat a range of ailments including anaemia, diabetes, herpes, skin infections, typhoid, throat and lung diseases, gastrointestinal, jaundice, rheumatic, and many more diseases. This review aimed to highlight the ethnopharmacological uses, phytochemical components, biological activities, and future research opportunities of the genus. A total number of 112 research papers published between the period 1977 and 2023 were considered and reviewed were retrieved from scientific databases such as Scopus, Web of Science, Elsevier Scient Direct, Google Scholar, and PubMed. The literature study revealed that both plant extracts and phytochemicals exhibited a wide range of biological activities including antidiabetes, anticancer, antimicrobial, anti-inflammation, and many other activities. Overall, a total number of 236 compounds have been encountered from the different species of Antidesma. These compounds belong to different chemical groups such as alkaloids, flavonoids, fatty acids, lignans, sterols, terpenoids, coumarins, and others. Three compounds such as antidesmone, amentoflavone, and β-sitosterol were found to be possible chemotaxonomic markers for the genus Antisema. Furthermore, only 16 species have been investigated in the context of phytochemistry and pharmacological activities of the genus so far. This review could serve as a comprehensive resource for future research in drug discovery and also lay the groundwork for the exploration of additional species within this genus for pharmaceutical applications.
Topics: Phytochemicals; Humans; Medicine, Traditional; Ethnopharmacology; Plant Extracts; Phytotherapy; Molecular Structure; Animals
PubMed: 38772510
DOI: 10.1016/j.fitote.2024.106023 -
Medicinal Research Reviews Nov 2023The high incidence of oral cancer combined with excessive treatment cost underscores the need for novel oral cancer preventive and therapeutic options. The value of... (Review)
Review
The high incidence of oral cancer combined with excessive treatment cost underscores the need for novel oral cancer preventive and therapeutic options. The value of natural agents, including plant secondary metabolites (phytochemicals), in preventing carcinogenesis and representing expansive source of anticancer drugs have been established. While fragmentary research data are available on antioral cancer effects of phytochemicals, a comprehensive and critical evaluation of the potential of these agents for the prevention and intervention of human oral malignancies has not been conducted according to our knowledge. This study presents a complete and critical analysis of current preclinical and clinical results on the prevention and treatment of oral cancer using phytochemicals. Our in-depth analysis highlights anticancer effects of various phytochemicals, such as phenolics, terpenoids, alkaloids, and sulfur-containing compounds, against numerous oral cancer cells and/or in vivo oral cancer models by antiproliferative, proapoptotic, cell cycle-regulatory, antiinvasive, antiangiogenic, and antimetastatic effects. Bioactive phytochemicals exert their antineoplastic effects by modulating various signaling pathways, specifically involving the epidermal growth factor receptor, cytokine receptors, toll-like receptors, and tumor necrosis factor receptor and consequently alter the expression of downstream genes and proteins. Interestingly, phytochemicals demonstrate encouraging effects in clinical trials, such as reduction of oral lesion size, cell growth, pain score, and development of new lesions. While most phytochemicals displayed minimal toxicity, concerns with bioavailability may limit their clinical application. Future directions for research include more in-depth mechanistic in vivo studies, administration of phytochemicals using novel formulations, investigation of phytocompounds as adjuvants to conventional treatment, and randomized clinical trials.
Topics: Humans; Neoplasms; Antineoplastic Agents; Plants; Phytochemicals; Mouth Neoplasms
PubMed: 37143373
DOI: 10.1002/med.21969 -
Journal of Fish Diseases Jun 2024Vibrio harveyi and Vibrio parahaemolyticus are species of the Vibrio genus that often cause disease and mass mortality in crustaceans. If not handled quickly and...
Vibrio harveyi and Vibrio parahaemolyticus are species of the Vibrio genus that often cause disease and mass mortality in crustaceans. If not handled quickly and appropriately, these diseases can cause considerable losses to farmers. Therefore, it is necessary to find a solution with safe and environmentally friendly disease prevention technology using natural ingredients, among others from plants, namely oil palm. Some parts of oil palm, namely leaves, fronds, fibres and oil palm pulp, which are palm waste, contain antibacterial compounds. This study aimed to assess the antibacterial activity of palm waste extracts, namely pulp, leaves, fronds and fibres using n-hexane, ethyl acetate, chloroform, ethanol and water maceration solvents against pathogenic bacteria V. harveyi and V. parahaemolyticus, and identify active compounds contained in palm waste. The results of the research are expected to produce innovative and sustainable solutions to control diseases in shrimp farming, contribute to the development of a sustainable fishing industry and open up the potential for utilizing palm waste as a value-added resource in the field of aquatic health. The results of observations on antibacterial activity tests and identifying the content of palm waste extract compounds were analysed descriptively displayed in the form of figures, tables and graphs. The results showed that palm waste extracts (pulp, leaves, fronds and fibres) with ethyl acetate and ethanol maceration solvents had very strong antibacterial potential, namely 20.14 ± 0.31 mm-25.52 ± 1.42 mm on V. harveyi bacteria and 20.41 ± 0.55 mm-25.00 ± 0.51 mm on V. parahaemolyticus bacteria. Palm extracts with n-hexane (>20 mm) and chloroform solvents generally have strong category antibacterial potential (10-20 mm), and palm extracts in water solvents have medium category potential (5-10 mm) against V. harveyi and V. parahemolyticus bacteria. The results of phytochemical tests on palm waste extracts with ethyl acetate and ethanol maceration solvents contain bioactive compounds of flavonoids, saponins, polyphenols and alkaloid tannins, steroids and triterpenoids. Palm extracts with n-hexane and chloroform solvents generally contain saponins, alkaloids, steroids and triterpenoids, while palm waste extracts with water solvents contain saponins.
Topics: Anti-Bacterial Agents; Vibrio; Vibrio parahaemolyticus; Plant Extracts; Arecaceae; Phytochemicals
PubMed: 38300462
DOI: 10.1111/jfd.13924