In recent years, resveratrol has become a popular nutritional supplements used by humans all over the world. Much research has been conducted to determine the efficacy of its use both in preventive and therapeutic dimensions. Usage of functional foods with a history of ethno-use with no known side effects is an area of great interest in improving the overall health condition of the population. Resveratrol, with its known potency and wide variety of health benefits has shown promising results in minimizing cardiovascular complications including hypertension, hypertrophy, ischemic heart disease and atherosclerosis. However, a great deal of controversy exists regarding the use of resveratrol as an anti-aging compound. In this review, progress in the chemical and biological production of resveratrol and its derivatives, their biological targets, bioavailability as well as the mechanisms of resveratrol cardio-protection will be discussed.