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.