香加皮中C21甾体化合物的体外抗肿瘤活性及其构效关系研究

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MTF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（1C5012。9ng·L-1）、宫颈癌Hela细胞株（IC5d8．63ng·L-1）、人乳腺癌MCF-7细胞株（IC5018．5ng·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。

Study on Antitumor Activity and Structure-activity Relationship of C21 Steroids from Periplocae Cortex

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 Perip-locae Cortex. Results： Among the five compounds, compound 1 possessed observably antitumor activity against SMMC-7721 （ IC50 12. 9 ng ？ L_1），Hela（ IC50 8. 63 ng ？ L_1） and MCF-7（ IC50 18. 5 ng ？ L_i ） 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 cy-totoxic activity of C21 steroids from Periplocae Cortex.