Abstract: Anthocyanins are naturally occurring polyphenols that impart bright color to fruits, vegetables and plants and exhibit various pharmacological activities according to amount of related research reports in recent years. Antioxidant activity of anthocyanins plays a key role in various health benefits such as anti-inflammatory, anti-obesity, anti-cancer and hypoglycaemic effects and so on. These activities give anthocyanins considerable potential in food industry as safe effective food colourants, functional foods and nutraceuticals, and as well as a nature plant sources of medicines. But, actually, as its pharmacological activities, the lack of its mechanism still need to have a more detailed and in-depth discussion. Based on the study of anthocyanins in vivo, including anti-cancer, cardioprotection, hyperglycemic, hypolipemic and the neurodegenerative disease were summarized and outlined in this article, in order to provide a theoretical basis for the future exploration.