番荔枝内酯类化合物体外抗肿瘤活性研究  

Antitumor activity of annonaceous acetogenins

作　　者：张宁[1] 刘嘉[1] 杨海军[1] 张威[1] 曾庆琪[1] 李祥[2] 

机构地区：[1]江苏建康职业学院,南京210029 [2]南京中医药大学,南京210046

出　　处：《中南药学》2017年第3期292-295,共4页Central South Pharmacy

摘　　要：目的研究不同结构类型的番荔枝内酯对多种人肿瘤细胞的体外抗肿瘤活性,探讨其构效关系。方法选取代表不同结构类型的番荔枝内酯单体,以人宫颈癌细胞株(Hela)、人肺癌细胞株(A-5408)、人乳腺癌细胞株(MCF-7)、人胃癌细胞株(SGC-790 1)和人肝癌细胞株(SMMC-75 41)为瘤株,用MTT法筛选各番荔枝内酯单体的抗肿瘤活性。结果邻双四氢呋喃番荔枝内酯(1~5)的抗肿瘤活性大于间位双四氢呋喃番荔枝内酯(6~10)和单四氢呋喃番荔枝内酯(11~12);间位双四氢呋喃番荔枝内酯对部分肿瘤细胞的抗癌活性比单四氢呋喃番荔枝内酯强;赤式双四氢呋喃环番荔枝内酯(6)比苏式构型(7)活性更强;顺式番荔枝内酯(12)有时显示更显著的抗癌选择活性;S构型比R构型的番荔枝内酯具有更好的选择活性。结论通过体外抗肿瘤活性研究,进一步揭示了番荔枝内酯的构效关系。Objective To determine the antitumor activity against human tumor cell lines of diverse annonaceous acetogenins（ACGs） and the structure-activity relationship. Methods Different stuctures of ACGs were selected to compare the anti-tumor activity of monomeric compounds by MTT methods, represented with human uterine cervix carcinoma cell line（Hela）, human lung carcinoma cell line（A-5408）, human breast carcinoma cell line（MCF-7）, human stomach carcinoma cell line（SGC-7901） and human liver carcinoma cell line（SMMC-754）. Results The bis-adjacent-THF ACGs had relatively high activities（1-5）; part of the non-adjacent bis-THF ACGs were superior to the mono-THF ACGs; the ACGs with stereochemical arrangement of thre o/trans/threo/trans/erythro（6）were gently more active than those with threo/trans/threo/trans/threo（7）, and the ACGs with cis THF ring partly produced notable selective cytotoxicity. Moreover, the ACGs with S configuration had more selective cytotoxicit y than with R configuration. Conclusion There is close ACGs structure-activity relationship in antitumor activity.

关 键 词：番荔枝内酯 抗肿瘤活性 构效关系 

分 类 号：R285.5[医药卫生—中药学]