牛膝中牛膝甾酮25位异构体构型的确定及其抗肿瘤活性的研究

目的牛膝 (AchyranthesbidentataBl.)中牛膝甾酮 2 5位异构体的分离、鉴定、构型确定以及肿瘤抑制活性的测定。方法利用硅胶吸附柱色谱和HPLC法进行分离 ,利用理化性质和波谱分析对化合物进行鉴定 ;利用体外实验法测定其活性。结果 2个非对映异构体化合物分别鉴定为 2 5 R牛膝甾酮 (2 5 Rinokosterone ,1)和 2 5 S牛膝甾酮 (2 5 Sinokosteone ,2 )。化合物 1具有一定的肿瘤抑制活性。结论 2个化合物均为首次从牛膝中分离得到 ,首次确定了其绝对构型 ,并首次对牛膝甾酮 2个 2 5位异构体进行了1H NMR、13 C NMR数据归属。牛膝中发挥肿瘤抑制作用的成分主要应为皂苷类成分。

Study on the 25-epimers of Inokosterone in Achyranthes bidentata Bl.and their antitumor activities

Objective To study the two 25-epimers of inokosterone isolated from Achyranthes bidentata Bl.Methods Column chromatography,HPLC and spectroscopic analysis were empolyed for isolation and identification; bioactivities were investigated by the in vitro method.Results 25-R inokosterone (1) and 25-S inokosteone (2) were obtained and 1 showed an antitumor activity to a certain degree.Conclusion Compounds 1 and 2 were first isolated from Achyranthes bidentata Bl.and the 1H-NMR? 13C-NMR data were summarized for the first time.The main constituent of antitumor effect belongs to triterpene sapoins.