托盘根三萜类化学成分及其抗肿瘤活性研究

Studies on Triterpene with Antitumor Activities from the Root of Rubus Crataegifolius Bunge.

目的:对蔷薇科悬钩子属植物托盘根部分的三萜类化学成分及其抗肿瘤活性进行研究。方法:运用硅胶柱色谱、Sephadex LH-20柱色谱﹑制备HPLC等色谱分离手段对托盘根乙醇提取物进行化学成分的分离纯化,根据理化性质及波谱数据鉴定其结构;选取小鼠肝癌H22细胞,观察三萜类化学成分注射给药对H22细胞小鼠移植瘤的抑瘤率。结果:从托盘根体积分数为75%乙醇的提取物中分离纯化得到2个三萜酸类化合物,分别为2α,3α-dihydroxy-19-oxo-18,19-seco-urs-11,13(18)-diene-28-oic acid(1)和2α,3α,19α-trihydroxy-11-oxo-urs-12-en-28-oic acid(2),20 mg/kg熊果酸腹腔注射对H22细胞小鼠移植瘤的抑瘤率为46.4%。结论:化合物1和2均为首次从该植物中分离得到,熊果酸具有较好的抑瘤作用。

Objective:To investigate the triterpenoid chemical components and their anti-tumor activity from the root of Rubus crataegifolius Bunge.,a plant from the Rosaceae family.Methods:Chemical components were separated and purified using various chromatographic methods such as silica gel column chromatography,Sephadex LH-20 column chromatography,and preparative HPLC.Their structure had been elucidated based on their physical and chemical properties as well as spectral data.Mouse hepatoma H22 cells were selected to observe the tumor inhibition rate of triterpenoid chemical components administered by injection on transplanted H22 tumors in mice.Results:Two triterpenoid acid compounds,2α,3α-dihydroxy-19-oxo-18,19-seco-urs-11,13(18)-diene-28-oic acid(1)and 2α,3α,19α-trihydroxy-11-oxo-urs-12-en-28-oic acid(2),were isolated and purified from the 75%ethanol extract of the root of R.crataegifolius Bunge.The tumor inhibition rate of H22 cell-transplanted tumors in mice by intraperitoneal injection of ursolic acid at 20 mg/kg was 46.4%.Conclusion:Compounds 1 and 2 were isolated from this plant for the first time,and ursolic acid exhibited significant anti-tumor activity.