Resveratrol is a polyphenol compound, at high level in grapes in particular. Resveratrol can exert the effects of antitumor, anti-cardiovascular disease, regulation of immunity, etc. This article summarized the antitumor effect and the molecular targets of resveratrol and the underlying mechanisms, including inhibition of proliferation, promotion of apoptosis, decrease of invasion ability and enhancement of radiotherapy sensitivity for tumor cells. Furthermore, we provided an outlook regarding the beneficial effec...