ABSTRACT: Resveratrol (3,5,4′-trihydroxystilbene) is a natural polyphenolic phytochemical with a variety of bioactivities associated with health promotion. Resveratrol is readily absorbed with the other absorbable digestion products of its main human dietary sources (peanuts, peanut butter, grapes, and red wine). The polyphenolic structure of resveratrol confers antioxidant activity and may reduce oxidant-induced apoptosis and low-density lipoprotein (LDL) oxidation. Resveratrol may be responsible, in part, for the correlation between increased wine consumption and decreased risk of coronary heart disease. The cardioprotective activity of resveratrol is associated with the inhibition of platelet aggregation and LDL oxidation and the promotion of artery vasorelaxation. As a chemoprevention agent, resveratrol has been shown to inhibit tumor initiation, promotion, and progression, as well as inhibit the growth of cancerous cells through increased apoptosis and/or cell cycle blockage. Inflammatory processes are associated in the pathogenesis of many chronic diseases including heart disease and cancer. Resveratrol has been shown to reduce inflammation via inhibition of prostaglandin production, cyclooxygenase-2 activity, and nuclear factor-кB activity. In addition, the estrogenic activity of resveratrol may help prevent post-menopausal bone loss. Modulation of cellular signal transduction pathways (such as mitogen-activated protein kinases) may explain, in part, the diverse bioactivities associated with resveratrol. Scientific information summarized in this review supports the many potential health benefits of resveratrol; however, further understanding of the bioavailability, metabolism, and cellular effects of resveratrol is necessary.