Gambogic acid,the natural compound extract from gamboges,might be a kind of highly effective anticancer drug candidate with low toxicity to normal tissue.In this review,we conclude that gambogic acid mainly can cause cell cycle arrest,induce cancer cell apoptosis,repress telomerase and Topo Ⅱalpha,possess the high antiangiogenic activities and antiinvasion properties,and reverse multidrug resistance.