10种蟾蜍甾烯类化合物对宫颈癌细胞Hela的细胞毒性及构效关系分析  

Antitumor Activity of Ten bufadienolides on Hela Cells and Its Structure-Activty Relationship

作　　者：王剑[1] 马宏跃[1] 丁安伟[1] 张军峰[2] 詹瑧[2] 唐于平[1] 

机构地区：[1]南京中医药大学药学院江苏省方剂高技术研究重点实验室,江苏南京210046 [2]南京中医药大学基础医学院,江苏南京210046

出　　处：《中医药信息》2012年第2期8-12,共5页Information on Traditional Chinese Medicine

基　　金：国家自然科学青年基金(81102762;30901894);霍英东教育基金会第十二届高等院校青年教师基金(121044);中药制药过程新技术国家重点实验室开放课题(SKL2010Z0404);江苏省中医药局康缘中医药科技创新基金(HZ1007KY)

摘　　要：目的:本研究比较蟾蜍甾烯(Bu)类化合物体外对宫颈癌Hela细胞的增殖抑制作用,并探讨化合物结构与其抗肿瘤活性之间的相关性。方法:采用改良MTT法测定不同浓度的蟾蜍甾烯(Bu)类化合物与Hela细胞共培养一定时间后对细胞的增殖抑制作用;分析10种化合物化学结构与细胞毒性的相关性。结果:10种蟾蜍甾烯类化合物对Hela细胞有明显的增殖抑制作用,其作用强度大小依次为Bul>Bt>Arg>Hel>Tel>Deb>Ctl>Cbg>Gtl>Rbg。含有14-氧环的A型母核的活性明显低于含有14-OH的B型结构母核。在相同母核中,对仅含一个羟基的化合物,存在乙酰基使细胞毒性增强。结论:10种蟾蜍甾烯类化合物均能有效抑制Hela细胞的增殖,呈现明显的剂量依赖性和构效关系。Objective ： To investigate the growth inhibitory effect of bufadienolides on Hela cell line and the rela- tionship between their structures and antitumor activity. Method： The modified MTT assay was adopted to measure the inhibitory effect of bufadienolides at different concentrations and chemical structures on Hela cells, and analysed the relationship between their chemical structures and eytotoxicity. Results：Ten bufadieno- lides could inhibit the proliferation of Hela cells effectively, and their sequence of cytotoxicities on Hela cells showed Bul 〉 Btl 〉 Arg 〉 Hel 〉 Tel 〉 Deb 〉 Ctl 〉 Cbg 〉 Gtl 〉 Rbg. It indicated that the chemical structure of A - type nucleus with 14 - epoxy was significantly lower than that of B - type nucleus which with 14 - hydrox- y. Similarly, among the same nucleus structures, the compounds with only one hydroxy of acetyl group of bu- fadienolides could enhance their cytotoxicity. Conclusion： The bufadienolides has an inhibitory effect on prolif- eration of Hela cell line, and their cytotoxicities show obvious concentration dependent manners and structure - activty relationship.

关 键 词：蟾蜍甾烯 HELA 抗癌活性 构效关系 

分 类 号：R285.5[医药卫生—中药学]