Resveratrol a polyphenolic phytoalexin possesses a variety of bioactivities associated with health promotion. Resveratrol is readily absorbed along with the other human dietary sources like 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. The cardioprotective activity of resveratrol is associated with the inhibition of platelet aggregation and LDL oxidation and the promotion of artery vasorelaxation. As a chemopreventing 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 with the pathogenesis of many chronic diseases including heart disease and diabetes. In addition, the estrogenic activity of resveratrol may help in the prevention of post-menopausal osteophoresis. This review reveals potential health benefits and discusses the current preclinical studies of resveratrol.