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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: In this study, we compared the inhibitory effect of budesciferin on the proliferation of cervical cancer Hela cells and explored the relationship between the structure of the compound and its anti-tumor activity. Methods: MTT assay was used to determine the inhibitory effect of different concentrations of budesciferin (Bu) compound on the proliferation of Hela cells co-cultured for a certain period of time. The correlation between chemical structure and cytotoxicity of 10 compounds was analyzed. Results: Ten kinds of toad steroid compounds had obvious proliferation inhibitory effects on Hela cells. The order of their intensities was Bul> Bt> Arg> Hel> Tel> Deb> Ctl> Cbg> Gtl> Rbg. The A-type parent nucleus containing the 14-oxo ring is significantly less active than the B-type parent nucleus containing 14-OH. In the same mother nucleus, for compounds containing only one hydroxyl group, the presence of acetyl groups enhances cytotoxicity. CONCLUSION: All ten kinds of toad steroids can effectively inhibit the proliferation of Hela cells in a dose-dependent and structure-activity relationship.