【摘要】 目的:研究香加皮中分离得到的5个C21甾体化合物的体外抗肿瘤作用并探讨其构效关系。方法:首次采用MTT法对香加皮中分离获得的C21甾体化合物1-5进行3种肿瘤细胞株的体外抗肿瘤活性实验。结果:体外抗肿瘤活性实验结果显示:化合物1对人肝癌SMMC-7721细胞株(IC5012.9 ng·L-1)、宫颈癌Hela细胞株(IC5d8.63 ng·L-1)、人乳腺癌MCF-7细胞株(IC5018.5 ng·L-1)均有较强的细胞毒活性,其他化合物细胞毒活性相对较弱。结论:化合物1(杠柳苷M)具有较强的细胞毒活性,初步的构效关系显示C-3位的不同取代基团对香加皮中C21甾体化合物的细胞毒活性有一定影响。更多还原

【Abstract】 Objective: To investigate the antitumor activity of five C21 steroids and illuminate the structure-activity relationship. Methods: MTT assay was firstly used to explore the cytotoxic activity against three cancer cell lines in vitro of compound 1- 5 isolated from Periplocae Cortex. Results: Among the five compounds,compound 1 possessed observably antitumor activity against SMMC-7721( IC 50 12. 9 ng·L- 1),Hela( IC 50 8. 63 ng·L- 1) and MCF-7( IC 50 18. 5 ng·L- 1) cancer cell lines. Conclusion: Compound 1( Periplocoside M) possessed observably cytotoxic activity. The SAR of the five compounds indicated that C-3 was an important position for keeping the cytotoxic activity of C21 steroids from Periplocae Cortex.更多还原