Resveratrol is a naturally occurring stilbene, a kind of polyphenolic compounds, found in a limited number of plant species such as grape, peanut, and pine. It has been considered as a phytoalexin in plants, and many studies have also shown its health benefits such as antioxidant activities, cancer prevention, blood thinning, and life span extension. This paper reviews the characteristics of resveratrol in aspects of synthesis, extraction, purification, and determination. In particular, the new outcomes of physiology function and the transgenic approaches have been presented. The challenges and chances for genetic engineering and health-related industries were also discussed.