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Flavonoids’ and Other Polyphenols’ Pharmacological Activities for Phytopharmaceutical and Medicinal Applications, 2nd Edition

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Natural Products Chemistry".

Deadline for manuscript submissions: 31 October 2025 | Viewed by 10989

Special Issue Editors


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Guest Editor
Department of Pharmaceutical Botany, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand
Interests: natural products; medicinal plants; flavonoids; pharmacological activities; anti-aging; cosmeceuticals; nutricosmetics; phytopharmaceutical products
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Guest Editor
Graduate School of Medical Sciences, Kanazawa University, Ishikawa 920-1192, Japan
Interests: medicinal plants; traditional medicines; quality evaluation of herbal medicines
Special Issues, Collections and Topics in MDPI journals

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Guest Editor Assistant
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand
Interests: pharmacognostic evaluation; medicinal plant identification; molecular pharmacognosy; traditional medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

In today's era of modern phytopharmaceutical and medicinal product development, the interest of industrial sectors and consumers in natural plant products consisting of the bioactive molecules flavonoids and other polyphenols has remarkably increased. Furthermore, a huge number of extracts from medicinal plants and several traditional medicines have been researched to discover their major bioactive molecules. This provides powerful potential pharmacological activities to develop phytopharmaceutical and medicinal products, including seed compounds for pharmaceuticals, as well as cosmeceuticals, cosmetics, nutricosmetics, supplements and other plant-based products with healthy benefits. This Special Issue aims to explore the potential of natural plant products, especially the bioactive molecules of flavonoids and other polyphenols from interesting medicinal plants worldwide, as well as from several traditional medicines whose attractive efficacies for phytopharmaceutical and medicinal applications are waiting to be discovered.

This Special Issue cordially welcomes potential authors to contribute and share their original articles, short communications, and review articles focusing on the natural plant products, particularly the bioactive molecules of flavonoids and other polyphenols medicinal plants and/or traditional medicines for pharmaceutical and medicinal applications. Research works on in vitro, in cellulo and in vivo biological/phytopharmaceutical activities are also welcome for submission to this Special Issue. Additionally, the study on innovative extraction methods and/or green extraction to validate the methods for separation and quantification of these natural plant bioactive molecules and/or increase their biological potential, e.g., antioxidant, anti-inflammation, anti-aging, anti-diabetic, anti-Parkinson's and other pharmaceutical activities, are also invited to share their valuable research studies in our Special Issue.

We sincerely look forward to receiving your great contributions.

Dr. Duangjai Tungmunnithum
Prof. Dr. Youhei Sasaki
Guest Editors

Dr. Aekkhaluck Intharuksa
Guest Editor Assistant

Manuscript Submission Information

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Keywords

  • natural plant products
  • flavonoids
  • polyphenols
  • medicinal plants
  • traditional medicines
  • biological activity
  • pharmacological activity
  • phytopharmaceutical and medicinal applications

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Related Special Issue

Published Papers (4 papers)

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Research

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19 pages, 3390 KiB  
Article
Garcinia mangostana L. Pericarp Extract and Its Active Compound α-Mangostin as Potential Inhibitors of Immune Checkpoint Programmed Death Ligand-1
by Sandar Naing, Nichawadee Sandech, Arnatchai Maiuthed, Sumet Chongruchiroj, Jaturong Pratuangdejkul and Pattamapan Lomarat
Molecules 2023, 28(19), 6991; https://doi.org/10.3390/molecules28196991 - 9 Oct 2023
Cited by 6 | Viewed by 2737
Abstract
α-Mangostin, a major xanthone found in mangosteen (Garcinia mangostana L., Family Clusiaceae) pericarp, has been shown to exhibit anticancer effects through multiple mechanisms of action. However, its effects on immune checkpoint programmed death ligand-1 (PD-L1) have not been studied. This study investigated [...] Read more.
α-Mangostin, a major xanthone found in mangosteen (Garcinia mangostana L., Family Clusiaceae) pericarp, has been shown to exhibit anticancer effects through multiple mechanisms of action. However, its effects on immune checkpoint programmed death ligand-1 (PD-L1) have not been studied. This study investigated the effects of mangosteen pericarp extract and its active compound α-mangostin on PD-L1 by in vitro and in silico analyses. HPLC analysis showed that α-mangostin contained about 30% w/w of crude ethanol extract of mangosteen pericarp. In vitro experiments in MDA-MB-231 triple-negative breast cancer cells showed that α-mangostin and the ethanol extract significantly inhibit PD-L1 expression when treated for 72 h with 10 µM or 10 µg/mL, respectively, and partially inhibit glycosylation of PD-L1 when compared to untreated controls. In silico analysis revealed that α-mangostin effectively binds inside PD-L1 dimer pockets and that the complex was stable throughout the 100 ns simulation, suggesting that α-mangostin stabilized the dimer form that could potentially lead to degradation of PD-L1. The ADMET prediction showed that α-mangostin is lipophilic and has high plasma protein binding, suggesting its greater distribution to tissues and its ability to penetrate adipose tissue such as breast cancer. These findings suggest that α-mangostin-rich mangosteen pericarp extract could potentially be applied as a functional ingredient for cancer chemoprevention. Full article
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17 pages, 2878 KiB  
Article
Enhancement of Bottle Gourd Oil Activity via Optimized Self-Dispersing Lipid Formulations (SDLFs) to Mitigate Isoproterenol-Evoked Cardiac Toxicity in Rats via Modulating BNP, MMP2, and miRNA-21 and miRNA-23a Genes’ Expression
by Shereen S. El-Mancy, Sylvia A. Boshra, Osama S. Elnahas, Sahar M. Fayez and Nermin M. Sheta
Molecules 2023, 28(16), 6168; https://doi.org/10.3390/molecules28166168 - 21 Aug 2023
Cited by 2 | Viewed by 1418
Abstract
Bottle gourd (BG) oil (family Cucurbitaceae) has several pharmacological activities including a reduction of the hazard of cardiovascular and atherosclerosis conditions. This work aimed to develop and optimize self-dispersing lipid formulations (SDLFs) of BG oil by applying a full 32 factorial design. [...] Read more.
Bottle gourd (BG) oil (family Cucurbitaceae) has several pharmacological activities including a reduction of the hazard of cardiovascular and atherosclerosis conditions. This work aimed to develop and optimize self-dispersing lipid formulations (SDLFs) of BG oil by applying a full 32 factorial design. The formulation variables (oil concentration and surfactant mixture ratio) showed an obvious impact on the characters of the prepared BG-SDLFs including droplet size (DS), polydispersity index (PDI), emulsification time (ET), and transmission percentage (Tr%). The optimum BG-SDLF composed of 30% oil and Tween 80/Cremophor® RH40 (1:1) showed good emulsification characteristics and a better drug release profile compared with BG oil. In vivo study in isoproterenol-injected rats showed that BG oil and the optimized BG-SDLF improved cardiac function, by elevating the miRNA-23a gene expression level and decreasing miRNA-21 gene expression. They also caused the inhibition of the plasma B-type natriuretic peptide (BNP), N-terminal proatrial natriuretic peptide (NT-pro-BNP), cystatin c, galectin-3, lipoprotein-associated phospholipase A2 (Lp-PLA2), matrix metallopeptidase 2 (MMP2), cardiac troponin I (cTnI), and cardiac troponin T (cTnT). Our study demonstrated that BG oil and the optimized BG-SDLF provided a cardioprotection against isoproterenol-induced cardiac toxicity with better results in groups treated with the optimized BG-SDLF. Full article
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Review

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32 pages, 8834 KiB  
Review
Mechanisms of Flavonoids and Their Derivatives in Endothelial Dysfunction Induced by Oxidative Stress in Diabetes
by Baolei Dou, Yingying Zhu, Mengwei Sun, Lina Wang, Yu Tang, Shuo Tian and Furong Wang
Molecules 2024, 29(14), 3265; https://doi.org/10.3390/molecules29143265 - 10 Jul 2024
Viewed by 1567
Abstract
Diabetic complications pose a significant threat to life and have a negative impact on quality of life in individuals with diabetes. Among the various factors contributing to the development of these complications, endothelial dysfunction plays a key role. The main mechanism underlying endothelial [...] Read more.
Diabetic complications pose a significant threat to life and have a negative impact on quality of life in individuals with diabetes. Among the various factors contributing to the development of these complications, endothelial dysfunction plays a key role. The main mechanism underlying endothelial dysfunction in diabetes is oxidative stress, which adversely affects the production and availability of nitric oxide (NO). Flavonoids, a group of phenolic compounds found in vegetables, fruits, and fungi, exhibit strong antioxidant and anti-inflammatory properties. Several studies have provided evidence to suggest that flavonoids have a protective effect on diabetic complications. This review focuses on the imbalance between reactive oxygen species and the antioxidant system, as well as the changes in endothelial factors in diabetes. Furthermore, we summarize the protective mechanisms of flavonoids and their derivatives on endothelial dysfunction in diabetes by alleviating oxidative stress and modulating other signaling pathways. Although several studies underline the positive influence of flavonoids and their derivatives on endothelial dysfunction induced by oxidative stress in diabetes, numerous aspects still require clarification, such as optimal consumption levels, bioavailability, and side effects. Consequently, further investigations are necessary to enhance our understanding of the therapeutic potential of flavonoids and their derivatives in the treatment of diabetic complications. Full article
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15 pages, 1688 KiB  
Review
Polyphenols and Neurodegenerative Diseases: Potential Effects and Mechanisms of Neuroprotection
by Raziel Alejandro Arias-Sánchez, Luz Torner and Bertha Fenton Navarro
Molecules 2023, 28(14), 5415; https://doi.org/10.3390/molecules28145415 - 14 Jul 2023
Cited by 34 | Viewed by 4230
Abstract
The increase in people’s longevity has, consequently, led to more brain involvement and neurodegenerative diseases, which can become complicated and lead to chronic degenerative diseases, thereby presenting greater public health problems. Medicinal plants have been used since ancient times and contain high concentrations [...] Read more.
The increase in people’s longevity has, consequently, led to more brain involvement and neurodegenerative diseases, which can become complicated and lead to chronic degenerative diseases, thereby presenting greater public health problems. Medicinal plants have been used since ancient times and contain high concentrations of molecules, including polyphenols. It has been proven that polyphenols, which are present in various natural sources can provide curative effects against various diseases and brain disorders through neuroprotective effects. These neuroprotective effects are mainly attributed to their ability to cross the blood–brain barrier, eliminate reactive oxygen species, and cause the chelation of metal ions. Polyphenols increase the concentration of neurotrophic factors and bind directly to the membrane receptors of these neurotrophic factors, to modulate and activate the signaling cascades that allow the plasticity, survival, proliferation, and growth of neuronal cells, thereby allowing for better learning, memory, and cognition. Moreover, polyphenols have no serious adverse side effects resulting from their consumption. Full article
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