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目的通过研究3,4,6,7,12,12b-六氢吡嗪[1’,2’:1,2]吡啶并[3,4-b]吲哚-1(2H)-酮(PI)的细胞毒抗肿瘤作用,探究PI是否可作为具可修饰性的新型抗肿瘤先导化合物。方法采用四甲基偶氮唑盐比色法(MTT法)研究PI和Fascaplysin(F)对人肝癌细胞(Bel-7402)、人宫颈癌细胞(Hela)、人乳腺癌细胞(T47D)和小鼠红白血病细胞(MEL)等肿瘤细胞的增殖抑制作用并进行对比,并选取Hela细胞观察PI处理Hela细胞后的形态学变化。结果 PI和F药理活性有相似性,在低质量浓度时,PI对HeLa细胞生长的抑制作用比F的抑制作用显著,同时PI对Hela细胞的抑制作用具有量效关系;PI处理HeLa细胞后的形态学变化具有典型细胞凋亡的形态学特征。结论 PI通过诱导肿瘤细胞凋亡产生细胞毒抗肿瘤作用。
AIM: To investigate the effect of 3,4,6,7,12,12b-hexahydropyrazino [1 ’, 2’: 1,2] pyrido [3,4-b] indol- ) Cytotoxicity of anti-tumor effect, to explore whether PI can be used as a modifiable novel antitumor lead compounds. Methods Methyl thiazolyl tetrazolium (MTT) assay was used to study the effect of PI and Fascaplysin (F) on the proliferation of Bel-7402, Hela, T47D and small Mouse erythroleukemia cells (MEL) and other tumor cells were compared and the proliferation of Hela cells was observed Hepatic cells treated with PI morphological changes. Results The pharmacological activities of PI and F were similar. At low concentration, the inhibitory effect of PI on HeLa cell growth was more significant than that of F, and PI had a dose-response relationship with Hela cells. After PI treatment of HeLa cells Morphological changes have typical morphological features of apoptosis. Conclusion PI induces cytotoxicity and anti-tumor effect by inducing tumor cell apoptosis.