Challenges in Analyzing the Biological Effects of Resveratrol

Erdoğan, Cihan Süleyman; Vang, Ole

doi:10.3390/nu8060353

Cited by 42 publications

(31 citation statements)

References 128 publications

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“…The plasma resveratrol concentrations measured at after two and four weeks of resveratrol administration ranged from 0.7 to 2.55 μ M and were in agreement with average plasma concentration ( C av ) of resveratrol reported in previous studies [19]. We did not investigate the compound concentration that reach the maximum plasma level ( C max ) and the area under the curve (AUC) or perform other detailed pharmacokinetic analyses in the present study because the pharmacokinetics of resveratrol have been extensively studied in humans [19–21]. As expected, resveratrol was not detected in any of the plasma samples collected at baseline or in the samples derived from the control group (Figure 1(a)).…”

Section: Resultssupporting

confidence: 90%

The Repeated Administration of Resveratrol Has Measurable Effects on Circulating T‐Cell Subsets in Humans

Espinoza

Trung

Inaoka

et al. 2017

Oxidative Medicine and Cellular Longevity

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Preclinical studies have shown that resveratrol exerts immunomodulatory effects with potential clinical value in the amelioration of autoimmune disorders and cancer prevention; however, little is known about the in vivo effects of this naturally occurring polyphenol on human immune cells. We assessed the effects of repeated doses of resveratrol (1000 mg/day for 28 days) on circulating immune cells in healthy Japanese individuals. Resveratrol was safe and well tolerated and was associated with significant increases in the numbers of circulating γδ T cells and regulatory T cells and resulted in small, yet significant, decreases in the plasma levels of the proinflammatory cytokines TNF-α and MCP-1 and a significant increase in the plasma antioxidant activity compared with the corresponding antioxidant baseline activity and with that in four control individuals. In in vitro studies, resveratrol significantly improved the growth of γδ T cells and regulatory T cells. These findings demonstrate that resveratrol has some clear biological effects on human circulating immune cells. Further studies are necessary to interpret the long-term immunological changes associated with resveratrol treatment.

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Section: Resultssupporting

confidence: 90%

The Repeated Administration of Resveratrol Has Measurable Effects on Circulating T‐Cell Subsets in Humans

Espinoza

Trung

Inaoka

et al. 2017

Oxidative Medicine and Cellular Longevity

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“…For the same reason, we do not review the efforts based on formulations or vehiculation by carriers, such as liposomes and nanoparticles (reviewed, e.g., in Ref. ).…”

Section: Strategies To Improve Bioefficacy Of Resveratrolmentioning

confidence: 99%

“…However, even 1 μM concentrations are hard to reach in animals through oral administration of resveratrol, largely because of elaboration by phase II metabolism . Therefore, translation of laboratory results into applications for human health may be problematic . Hence, it would be of great help to increase resveratrol levels, even modestly, and/or to modify its tissue distribution.…”

Section: Introductionmentioning

confidence: 99%

Resveratrol derivatives as a pharmacological tool

Biasutto

Mattarei

Azzolini

et al. 2017

Annals of the New York Academy of Sciences

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Prodrugs of resveratrol are under development. Among the long-term goals, still largely elusive, are (1) modulating physical properties (e.g., water-soluble derivatives bearing polyethylene glycol chains), (2) changing distribution in the body (e.g., galactosyl derivatives restricted to the intestinal lumen), (3) increasing absorption from the gastrointestinal tract (e.g., derivatives imitating the natural substrates of endogenous transporters), and (4) hindering phase II metabolism (e.g., temporarily blocking the hydroxyls), all contributing to (5) increasing bioavailability. The chemical bonds that have been tested for functionalization include carboxyester, acetal, and carbamate groups. A second approach, which can be combined with the first, seeks to reinforce or modify the biochemical activities of resveratrol by concentrating the compound at specific subcellular sites. An example is provided by mitochondria-targeted derivatives. These proved to be pro-oxidant and cytotoxic in vitro, selectively killing fast-growing and tumor cells when supplied in the low micromolar range. This suggests the possibility of anticancer applications.

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“…RSV has poor water solubility and thus has to be bound to plasma proteins to assure its body distribution and bioavailability [66]. Indeed, in its transport, RSV can bind to serum proteins [67] such as lipoproteins, hemoglobin, and albumin which facilitate its carrier mediated cellular uptake and then it can passively diffuse through the plasma membrane [68,69] investigated the binding properties of RSV to plasma proteins, such as human serum albumin (HSA) and hemoglobin (Hb) and confirmed that both complexes formed are spontaneous and exothermic. The binding constant of RSV-HSA complex is larger than that of RSV-Hb, which indicates the higher affinity of HSA to RSV.…”

Section: Distributionmentioning

confidence: 99%

Reduction of Hepatotoxicity Induced by Doxorubicin

Bengaied¹,

Ribeiro²,

Amri³

et al. 2017

J Integr Oncol

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Doxorubicin (DOX) has been used in the treatment of variety of cancers but its administration is limited by a dosedependent toxicity. Its cytotoxic effects on malignant cells have shown an increase in the risk of cardiotoxicity, hepatoxicity, renal insufisance.Antioxydants have been explored for both their cancer preventive properties and chemodulatory of DOX toxicity. Resveratrol (RSV) is a polyphenolic constituent of several dietary mainly of grapes and wine origin recently its anticancer potential has been extensively explored, revealing its anti-proliferative effect on different cancer cell lines, both in vitro and in vivo. RSV is also known to have modulatory effects on cell apoptosis, migration and growth via various signaling pathways. Though, RSV possesses great medicinal value, its applications as a therapeutic drug is limited. Problems like low oral bioavailability and poor aqueous solubility make RSV an unreliable candidate for therapeutic purposes. Additionally, the rapid gastrointestinal digestion of RSV is also a major barrier for its clinical translation. Hence, to overcome these disadvantages RSV-based nanodelivery systems have been considered in recent times. Nanodelivery systems of RSV have shown promising results in its uptake by the epithelial system as well as enhanced delivery to the target site. Herein we have tried to bring new new insights into the molecular mechanisms of DOX toxicity with respect to DNA damage, free radicals and whether RSV can be a playmaker as chemodulatory of DO x .

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Challenges in Analyzing the Biological Effects of Resveratrol

Cited by 42 publications

References 128 publications

The Repeated Administration of Resveratrol Has Measurable Effects on Circulating T‐Cell Subsets in Humans

The Repeated Administration of Resveratrol Has Measurable Effects on Circulating T‐Cell Subsets in Humans

Resveratrol derivatives as a pharmacological tool

Reduction of Hepatotoxicity Induced by Doxorubicin

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