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目的:探讨金雀异黄素(gen)衍生物5,4’-二-正辛烷氧基-7-二氟亚甲基异黄酮(5,4’-Di-n-octoxyl-7-gem-difluoromethylenegenisteinDOdFMG)体外选择性抑制人乳腺癌细胞增殖和诱导凋亡作用。方法:MTT法检测DOdFMG对MCF-7和HBL-100细胞生长的影响;流式细胞术和AO/EB荧光双染法测定DOdFMG诱导MCF-7细胞凋亡作用及对细胞周期的影响。结果:DOdFMG抑制MCF-7细胞生长,呈时间剂量依赖,比gen具有更强选择性和抗肿瘤活性;DOdFMG能诱导MCF-7细胞凋亡,DOdFMG40.0μM组比gen100μM组诱导凋亡的活性更强,DOdFMGMCF-7将MCF-7细胞阻滞于S期和G2期,呈浓度依赖。结论:DOdFMG能抑制人乳腺癌细胞系(MCF-7)细胞生长和诱导凋亡,是一种高效、毒副作用小的新型治疗乳腺癌候选药物。
OBJECTIVE: To investigate the effects of genistein 5,4’-di-n-octoxyl-7-gem -difluoromethylenegenisteinDOdFMG) selectively inhibits the proliferation and induces apoptosis of human breast cancer cells in vitro. Methods: The effect of DOdFMG on the growth of MCF-7 and HBL-100 cells was detected by MTT assay. The effect of DOdFMG on the apoptosis of MCF-7 cells and the cell cycle were detected by flow cytometry and AO / EB double staining. Results: DOdFMG inhibited the growth of MCF-7 cells in a dose-and time-dependent manner, which was more selective and anti-tumor than gen. DOdFMG induced the apoptosis of MCF-7 cells. DOdFMG40.0μM group had more activity than gen100μM group Strong, DOdFMGMCF-7 MCF-7 cells in the S phase and G2 phase, in a concentration-dependent manner. Conclusion: DOdFMG can inhibit the growth of human breast cancer cell line (MCF-7) and induce apoptosis. It is a novel drug candidate for treating breast cancer with high efficiency and little side effects.