三萜是一类具有独特空间结构的生物活性天然产物，不仅在抗炎、抗菌、保肝护肾等方面有着重要的应用价值，还具有很强的抗肿瘤活性，极有可能被开发为新一代的抗癌药物。对三萜类化合物抗肿瘤的作用机制、构效关系以及成药特性改良等方面进行综述，可为深入研究三萜的抗肿瘤特性，进一步开发抗癌药物提供科学研究基础。

As a kind of bioactive natural products with unique space structure, triterpenoid is widely used in diminishing inflammation, antibacterial, and protecting liver and kidney. Because of the strong ability of antitumor, it is likely to be developed as a new generation of anticancer drugs. In this review, the antineoplastic mechanism, structure-activity relationship, and pharmacophore improvement were summarized for further research on the antitumor properties of triterpenoid.