人参二醇与人参三醇衍生物的氧化及细胞毒活性

The Oxidation and Cytotoxic Activity Screening of Panaxadiol and Panaxatriol Derivatives

目的以人参二醇和人参三醇为起始原料制备达玛烷型三萜衍生物,并进行体外细胞毒活性筛选.方法以人参二醇和人参三醇经PCC(氯铬酸吡啶盐)氧化、DDQ(二氯二氰基苯醌)氧化后的产物为原料,进一步与间氯过氧苯甲酸(m-CPBA)进行氧化反应,得到的开环产物采用MTT法进行体外细胞毒活性筛选.结果共制备了4个开环产物(化合物2、4、6、8).结论这4个开环产物均为新化合物,化合物2和4对几种肿瘤细胞株具有显著的细胞毒活性.

Objective To study the synthesis of dammarane-type triterpene derivatives by using Panaxadiol and Panaxatriol as starting materials and screen their cytotoxic activity in vitro.Methods The products derived from PCC oxidation and DDQ oxidation of panaxadiol and panaxatriol,were further oxidized with m-chloroperoxybenzoic acid(m-CPBA),as a result,four ring opening products were obtained,which were subjected to in vitro cytotoxic activity screening with MTT method.Results Four ring-opening derivatives were prepared(Compound2,4,6,8).Conclusion The four ring-opening derivatives are new compounds,and compound2and4show significant cytotoxicity against several cancer cell lines.