目的研究石上柏提取物、各萃取部位抗肿瘤活性及石上柏的抗肿瘤作用物质基础。方法采用MTT法以人癌细胞评估石上柏乙醇总提取物及其石油醚、二氯甲烷、乙酸乙酯萃取部位和溶剂萃取后剩余水部位的体外抗肿瘤活性,筛选出抗肿瘤活性较好的部位,并采用制备型液相色谱分离纯化及波谱技术鉴定其主要化学成分结构。结果石上柏二氯甲烷和乙酸乙酯萃取部位具有较好的体外抗肿瘤活性,从乙酸乙酯萃取部位中分离鉴定出4个化合物:穗花杉双黄酮(I)、罗伯斯特双黄酮(Ⅱ)、2",3"-二氢-3’,3'''-双芹菜素(Ⅲ)及3’,3'''-双柚皮素(Ⅳ),其中Ⅲ和Ⅳ为首次从该植物中分离得到。结论石上柏抗肿瘤活性成分可能集中在二氯甲烷和乙酸乙酯萃取部位,化合物I、Ⅱ、Ⅲ及Ⅳ可能是其发挥抗肿瘤作用的物质基础。
Objective To investigate the anticancer effect of extracts and reveal the active components in S. doederleinii. Methods Anticancer effect of the four extracts of ethanol, petroleum ether, dichloromethane, ethyl acetate from S. doederleinii and the residual water portion on human tumor cell lines cultured in vitro was tested by MTT assay. The active components were separated from the screened extract by preparative-HPLC and identified by MS and NMR. Results Dichloromethane and ethyl acetate extracts were found to be the effective fractions from S. doederleinii. Four compounds were separated from ethyl acetate extract and identified as amentoflavone ( I ), robustflavone ( Ⅱ ), 2", 3"-dihydro-3r, 3"'-biapigenin (Ⅲ) and 3', 3"'-binaringenin (IV). Compounds Ⅲ and 1V were identified from this plant for the first time. Oonclusions Anticancer components of S. doederleinii may concentrated in the extracts of dichloromethane and ethyl acetate, and compounds I , Ⅱ , Ⅲ and IV separated from ethyl acetate extract may have the most antitumor activities.