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Resveratrol: Improving Human Health and Preventing Diseases
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Resveratrol: Improving Human Health and Preventing Diseases

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Bioactives and Nutraceuticals".

Deadline for manuscript submissions: 20 December 2024 | Viewed by 11509

Special Issue Editor

Dr. José Díaz-Chávez

E-Mail Website
Guest Editor
1. Instituto Nacional de Cancerología (INCAN), Avenida San Fernando No. 22, Sección XVI Tlalpan, Ciudad de México 14080, Mexico
2. Unidad de Investigación Biomédica en Cáncer, Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México (UNAM), Coyoacán, Ciudad de México 04510, Mexico
Interests: resveratrol; cancer; DNA repair
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Resveratrol (RV) is a natural phenol found in red grapes, mulberries, peanuts, wine, and tea, and it can be extracted from red wine during the fermentation of grape skin. The mechanism by which RV exerts favorable effects is related to the induction of genes for oxidative phosphorylation and mitochondrial biogenesis. It has been reported that RV plays a role as an anti-inflammatory, antioxidant, and antiviral, and exerts anticancer activities through many different mechanisms. Patients with higher anxiety traits, depression, and fatigue showed a distinct metabolic profile, indicative of a different energy homeostasis, hormonal metabolism, and gut microbial activity. The daily consumption of RV resulted in a significant modification in the microbial metabolism, with potential long-term health consequences. A human intervention study indicated that the consumption of RV increased the prevalence of Enterococcus, Prevotella, and Bacterioides uniformis. Several beneficial effects have been observed in human beings, but other studies are necessary to continue with the scientific research in this field. Indeed, new knowledge concerning the “Health Benefits of Resveratrol” could enable the development of novel functional foods or nutraceuticals, incorporating resveratrol, suitable for preventing or treating diseases, such as cancer, cardiovascular diseases, obesity, dyslipidemia, insulin resistance and diabetes, liver diseases, and other disorders.

Dr. José Díaz-Chávez
Guest Editor

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Keywords

  • resveratrol supplementation
  • resveratrol metabolites
  • sirtuins
  • aging
  • epigenetic
  • benefits in chronic disease
  • treatment

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Related Special Issue

Published Papers (5 papers)

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Research

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18 pages, 4986 KiB  
Article
Differential Cytoprotective Effect of Resveratrol and Its Derivatives: Focus on Antioxidant and Autophagy-Inducing Effects
by Kamilla Varga, Alexandra Paszternák, Virág Kovács, Annamária Guczogi, Noémi Sikur, Dimitrisz Patakfalvi, Fruzsina Bagaméry, Éva Szökő and Tamás Tábi
Int. J. Mol. Sci. 2024, 25(20), 11274; https://doi.org/10.3390/ijms252011274 - 20 Oct 2024
Viewed by 589
Abstract
Numerous beneficial effects of resveratrol were reported; however, its pharmacological profile is contradictious. Previously, we have demonstrated that resveratrol has a dose-dependent cytoprotective effect and the essential role of autophagy induction was demonstrated. Resveratrol suffers from unfavorable pharmacokinetics, hindering its clinical use. Our [...] Read more.
Numerous beneficial effects of resveratrol were reported; however, its pharmacological profile is contradictious. Previously, we have demonstrated that resveratrol has a dose-dependent cytoprotective effect and the essential role of autophagy induction was demonstrated. Resveratrol suffers from unfavorable pharmacokinetics, hindering its clinical use. Our aim was to study the cytoprotective effect of resveratrol derivatives to better understand structure–activity relationships that may facilitate the development of compounds with better druglike characteristics. Serum-deprivation-induced caspase activation, free radical generation, mitochondrial membrane depolarization and autophagy were detected in the presence of resveratrol analogs with different oxidation states on mouse embryonal fibroblasts. Distinct cytoprotective mechanisms of the examined compounds were revealed. Monomethyl resveratrol had similar potency to resveratrol (EC50: 85.3 vs. 84.2 μM); however, autophagy induction was not essential for its cytoprotective effect. Oxyresveratrol was found to be a strong antioxidant that can induce direct cytoprotection rather than autophagy. Trimethyl-resveratrol, lacking free hydroxyl groups, induced damage that was too significant and hardly compensated by the activation of cytoprotective machineries, and caspase activation was reduced by only 24.5%. Based on our results, methylation of resveratrol reduces its antioxidant activity, while autophagy induction can still contribute to its cytoprotective effect. The introduction of an additional hydroxyl group, however, augments the antioxidant properties, inducing cytoprotection without autophagy induction. Full article
(This article belongs to the Special Issue Resveratrol: Improving Human Health and Preventing Diseases)
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24 pages, 5309 KiB  
Article
Exploration of Nutraceutical Potentials of Isorhapontigenin, Oxyresveratrol and Pterostilbene: A Metabolomic Approach
by Yu Dai, Jingbo Wang, Yuhui Yang, Hongrui Jin, Feng Liu, Hui Liu, Paul C. Ho and Hai-Shu Lin
Int. J. Mol. Sci. 2024, 25(20), 11027; https://doi.org/10.3390/ijms252011027 - 14 Oct 2024
Viewed by 797
Abstract
Resveratrol (trans-3,5,4′-trihydroxystilbene, RES) is one of the most well-known natural products with numerous health benefits. To explore the nutraceutical potentials of some dietary RES derivatives including isorhapontigenin (trans-3,5,4′-trihydroxy-3′-methoxystilbene, ISO), oxyresveratrol (trans-3,5,2′,4′-tetrahydroxystilbene, OXY) and pterostilbene (trans-3,5-dimethoxy-4′-hydroxystilbene, [...] Read more.
Resveratrol (trans-3,5,4′-trihydroxystilbene, RES) is one of the most well-known natural products with numerous health benefits. To explore the nutraceutical potentials of some dietary RES derivatives including isorhapontigenin (trans-3,5,4′-trihydroxy-3′-methoxystilbene, ISO), oxyresveratrol (trans-3,5,2′,4′-tetrahydroxystilbene, OXY) and pterostilbene (trans-3,5-dimethoxy-4′-hydroxystilbene, PTS), their impacts on metabolism and health were assessed in Sprague Dawley rats after a two-week daily oral administration at the dose of 100 µmol/kg/day. Non-targeted metabolomic analyses were carried out with the liver, heart, brain and plasma samples using gas chromatography–tandem mass spectrometry (GC-MS/MS). Notable in vivo health benefits were observed, as the rats received ISO, PTS or RES showed less body weight gain; the rats received OXY or RES displayed healthier fasting blood glucose levels; while all of the tested stilbenes exhibited cholesterol-lowering effects. Additionally, many important metabolic pathways such as glycolysis, pentose phosphate pathway, tricarboxylic acid cycle and fatty acid oxidation were found to be modulated by the tested stilbenes. Besides the reaffirmation of the well-known beneficial effects of RES in diabetes, obesity, cardiovascular disease and Alzheimer’s disease, the metabolomic analyses also suggest the anti-diabetic, cardio-, hepato- and neuro-protective activities of ISO; the anti-diabetic, cardio-, hepato- and neuro-protective effects of OXY; and the anti-aging, anti-inflammatory, cardio-, hepato- and neuro-protective potential of PTS. Interestingly, although these stilbenes share a similar structure, their biological activities appear to be distinct. In conclusion, similarly to RES, ISO, OXY and PTS have emerged as promising candidates for further nutraceutical development. Full article
(This article belongs to the Special Issue Resveratrol: Improving Human Health and Preventing Diseases)
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23 pages, 3427 KiB  
Article
Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions
by Natalia Rosiak, Ewa Tykarska and Judyta Cielecka-Piontek
Int. J. Mol. Sci. 2024, 25(5), 2774; https://doi.org/10.3390/ijms25052774 - 28 Feb 2024
Cited by 2 | Viewed by 1655
Abstract
In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented [...] Read more.
In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented using mathematical equations such as the Gordon–Taylor and Couchman–Karasz equations, facilitated the determination of predicted values for glass transition (Tg), PTR’s miscibility with PVP, and the strength of PTR’s interaction with the polymers. Fourier-transform infrared (FTIR) analysis validated interactions maintaining PTR’s amorphous state and identified involved functional groups, namely, the 4′–OH and/or –CH groups of PTR and the C=O group of PVP. The study culminated in evaluating the impact of amorphization on water solubility, the release profile in pH 6.8, and in vitro permeability (PAMPA-GIT and BBB methods). In addition, it was determined how improving water solubility affects the increase in antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays) and neuroprotective (inhibition of cholinesterases: AChE and BChE) properties. The apparent solubility of the pure PTR was ~4.0 µg·mL−1 and showed no activity in the considered assays. For obtained ASDs (PTR-PVP30/PTR-PVPVA64, respectively) improvements in apparent solubility (410.8 and 383.2 µg·mL−1), release profile, permeability, antioxidant properties (ABTS: IC50 = 52.37/52.99 μg·mL−1, DPPH: IC50 = 163.43/173.96 μg·mL−1, CUPRAC: IC0.5 = 122.27/129.59 μg·mL−1, FRAP: IC0.5 = 95.69/98.57 μg·mL−1), and neuroprotective effects (AChE: 39.1%/36.2%, BChE: 76.9%/73.2%) were confirmed. Full article
(This article belongs to the Special Issue Resveratrol: Improving Human Health and Preventing Diseases)
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Review

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20 pages, 2129 KiB  
Review
Resveratrol as a Promising Nutraceutical: Implications in Gut Microbiota Modulation, Inflammatory Disorders, and Colorectal Cancer
by Vidhya Prakash, Chinchu Bose, Damu Sunilkumar, Robin Mathew Cherian, Shwetha Susan Thomas and Bipin G. Nair
Int. J. Mol. Sci. 2024, 25(6), 3370; https://doi.org/10.3390/ijms25063370 - 16 Mar 2024
Cited by 13 | Viewed by 4892
Abstract
Natural products have been a long-standing source for exploring health-beneficial components from time immemorial. Modern science has had a renewed interest in natural-products-based drug discovery. The quest for new potential secondary metabolites or exploring enhanced activities for existing molecules remains a pertinent topic [...] Read more.
Natural products have been a long-standing source for exploring health-beneficial components from time immemorial. Modern science has had a renewed interest in natural-products-based drug discovery. The quest for new potential secondary metabolites or exploring enhanced activities for existing molecules remains a pertinent topic for research. Resveratrol belongs to the stilbenoid polyphenols group that encompasses two phenol rings linked by ethylene bonds. Several plant species and foods, including grape skin and seeds, are the primary source of this compound. Resveratrol is known to possess potent anti-inflammatory, antiproliferative, and immunoregulatory properties. Among the notable bioactivities associated with resveratrol, its pivotal role in safeguarding the intestinal barrier is highlighted for its capacity to prevent intestinal inflammation and regulate the gut microbiome. A better understanding of how oxidative stress can be controlled using resveratrol and its capability to protect the intestinal barrier from a gut microbiome perspective can shed more light on associated physiological conditions. Additionally, resveratrol exhibits antitumor activity, proving its potential for cancer treatment and prevention. Moreover, cardioprotective, vasorelaxant, phytoestrogenic, and neuroprotective benefits have also been reported. The pharmaceutical industry continues to encounter difficulties administering resveratrol owing to its inadequate bioavailability and poor solubility, which must be addressed simultaneously. This report summarizes the currently available literature unveiling the pharmacological effects of resveratrol. Full article
(This article belongs to the Special Issue Resveratrol: Improving Human Health and Preventing Diseases)
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16 pages, 1242 KiB  
Review
Resveratrol and Gut Microbiota Synergy: Preventive and Therapeutic Effects
by Milos Gostimirovic, Jovana Rajkovic, Ana Bukarica, Jovana Simanovic and Ljiljana Gojkovic-Bukarica
Int. J. Mol. Sci. 2023, 24(24), 17573; https://doi.org/10.3390/ijms242417573 - 17 Dec 2023
Cited by 6 | Viewed by 2992
Abstract
The role of an imbalanced high-fat diet in the pathophysiology of common chronic noncommunicable diseases has been known for years. More recently, the concept of ‘gut microbiota’ and the interaction between their composition and gut metabolites produced from the intake of dietary products [...] Read more.
The role of an imbalanced high-fat diet in the pathophysiology of common chronic noncommunicable diseases has been known for years. More recently, the concept of ‘gut microbiota’ and the interaction between their composition and gut metabolites produced from the intake of dietary products have gained the focus of researchers, mostly from the perspective of the prevention of cardiovascular and metabolic disorders, which are still the leading cause of death globally. The aim of this work is to highlight the health benefits of the interaction between resveratrol (RSV), red grape polyphenol, and gut microbiota, through aspects of their therapeutic and preventive potentials. Since changed microbiota (mostly as a consequence of antibiotic overuse) contribute to the persistence of post (‘long’)-COVID-19 symptoms, these aspects will be covered too. Data were obtained from the electronic databases (MedLine/PubMed), according to specific keywords regarding the protective role of resveratrol, the gut microbiota, and their synergy. RSV exerts beneficial properties in the modulation of cardiovascular, metabolic, and post-COVID-19-related disorders. In healthy individuals, it maintains an ergogenic capacity, prevents oxidative stress, and modulates the inflammatory response. Overall, it improves quality of life. The RSV–gut-microbiota interaction is beneficial in terms of maintaining human health. Along with physical activity, it is key for the prevention of chronic noncommunicable diseases. Full article
(This article belongs to the Special Issue Resveratrol: Improving Human Health and Preventing Diseases)
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