Mangiferin is a naturally derived C-glucosyl flavone, which can be isolated from many plants as a potent pharmaceutical compound. Previous studies indicated that mangiferin exerts an array of pharmacological activities, including anti-diabetes, anti-tumor, anti-inflammation, anti-oxidation, treatment of eye diseases, nervous system protection, kidney protection, and improvement of cardiovascular diseases. Due to its various biological activities, mangiferin has great potential for prevention and treatment of many diseases. This paper summarizes the research progress and the mechanism of mangiferin pharmacodynamics, so as to provide a scientific basis for the further research and utilization of mangiferin.