生化学と薬理学: オープンアクセス
オープンアクセス

概要

Pharmacological Properties of Resveratrol. A Pre-Clinical and Clinical Review

Muñoz O, Muñoz R and Bustamante S

Resvertrol (Resv) is an extensively studied molecule – as of 2015 PubMed held more than 7100 publications on the subject. The First International Resveratrol Conference in 2010 found insufficient evidence to justify recommending chronic administration of Resv in humans, a finding in stark contrast with the claims of its therapeutic effects often made by the media, based on its supposed role in the beneficial properties of red wine and in the so-called French Paradox. However, pharmacological studies carried out on different formulations of Resv from 2010 onwards suggest that these recommendations should be reviewed. Pharmacokinetic Resv is characterized by high inter-individual variability within pharmacokinetic parameters. Resv exhibits a rapid absorption rate, with extensive pre-systemic metabolism by human cytochrome P 450 and intestinal microbiota. Its metabolism leads mainly to conjugation products, the biological activity of which is still under discussion. It is also rapidly cleared by the kidneys. Finally, the estimated bioavailability of Resv is around 1% of orally-administered doses. Clinical trials have shown that Resv seems to exert a therapeutic effect on endothelial dysfunction consistent with in vitro observations demonstrating that Resv stimulates the eNOS enzyme. Inflammatory markers and CRP reductions obtained from doses of Resv equal to or less than 20 mg/day are not observed in larger doses, which imply hermetic behavior. Resv has also been shown to reduce the atherogenic potential of LDL cholesterol by reducing oxidized LDL and ApoB levels, which would in turn reduce atherogenesis. Resv is a well-tolerated compound; short-term clinical trials have shown frequent gastrointestinal discomfort or spontaneously resolving diarrhea only with the administration of high doses.