Abstract

Resveratrol is a phytoalexin with cancer chemopreventive properties in preclinical models of carcinogenesis. The mechanisms via which resveratrol is thought to exert chemopreventive efficacy are inhibition of cyclooxygenase enzymes, inhibition of angiogenesis, modulation of drug metabolising enzymes, antioxidation and alterations of cell cycle components and apoptotic machinery. Pharmacokinetic evidence in rodents and humans suggests that the bioavailability of resveratrol is very low and that resveratrol conjugates are the major circulating agent-derived species. The recent realisation that resveratrol can mimic caloric restriction in several species has generated a lot of interest. Attempts to design analogues with the aim of optimising resveratrol pharmacology have furnished stilbenes with different aryl subtituents, e. g., methoxy instead of hydroxy. Some of these derivatives possess more potent pharmacological properties than the lead compound. More work is required to elucidate the role of metabolites in the pharmacological activity of resveratrol.