蟾蜍甾烯对舌鳞癌细胞Tca-8113的细胞毒性及构效关系分析  

Antitumor Activity of bufadienolides on Tongue squamous carcinoma Cells T ca-8113 Cells and ItsStructure-Activity Relationship

作　　者：宫辉[1] 周婧[2] 高玲娟[1] 

机构地区：[1]南京市妇幼保健院,江苏南京210004 [2]南京中医药大学,江苏南京210046

出　　处：《中医药信息》2012年第5期14-17,共4页Information on Traditional Chinese Medicine

基　　金：国家自然科学基金青年基金项目(81102762;30901894;国家科技支撑计划项目(2011BAI04B04);教育部新教师基金项目(20093237120013);霍英东教育基金会第十二届高等院校青年教师基金(121044)

摘　　要：目的:通过研究比较蟾蜍甾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Tca-8113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Tca-8113细胞有明显的增殖抑制作用,其作用强度大小依次为Bul>Cbg>Btl>Arg>Tel>Deb>Hel>Ctl>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A、B母核中,羟基数量不同,以及是否含有乙酰基,对活性的影响趋势也不相同。结论:10种蟾蜍甾烯类化合物均能有效抑制Tca-8113细胞的增殖,呈现明显的剂量依赖性和构效关系。Objective： To investigate the comparison of correlation between the toad -tumor activity. Method：The modified MTI＂ assay was adopted to measure the inhibitory effect of bufadienolides at different concentra- tions and chmical structures on Tca -8113 cells, and analysed the relationship between their chemical struc- tures and cytotoxicity. Results： Ten bufadienolides could inhibit the proliferation of Tca -8113 cells effective- ly, and their sequence of cytotoxicities on Tca - 8113 cells showed Bul 〉 Cbg 〉 Btl 〉 Arg 〉 Tel 〉 Deb 〉 Hel 〉 Ctl 〉 Gtl 〉 Rbg. It indicated that the chemical structure of A - type nucleus with 14 - epoxy was significantly lower than that of B -type nucleus with lg -hydroxy. In A, B nucleus, the hydroxyl number, and whether it contains acetyl- activity trends are also different. Conclustion： The bufadienolides has an inhibitory effect on proliferation of Tca -8113 cell line, and their cytotoxicities show obvious concentration dependent manners and structure -activity relationship.

关 键 词：蟾蜍甾烯 TCA-8113 抗癌活性 构效关系 

分 类 号：R739.8[医药卫生—肿瘤] R285[医药卫生—临床医学]