Abstract： Betulinic acid(BA)is a lupinane-type pentacyclic triterpenoid with high content in a variety of Chinese medicinal materials,such as Majiazi(马甲子),Duzhong(杜仲),and Suanzaoren(酸枣仁).Studies have demonstrated that BA has anti-tumor,anti-inflammatory,anti-HIV,anti-malarial,antimicrobial,and antioxidant activities.It has attracted much attention in the treatment of tumors because of the low toxic-ity and high efficiency.Accordingly,extensive studies have been conducted about the related mechanisms,including the mitochondrial path-way,the Sp transcription factor pathway,and autophagy,while the overall picture remains unclear.In this paper,we reviewed the anti-tumor mechanism of BA,clarified the existing findings regarding different tumors,and analyzed the research hotspots,aiming to provide references for the research on BA and anti-tumor drugs with BA and its analogs as the main pharmacodynamic components.