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目的:观察金雀异黄素(genistein,GEN)衍生物即5,4′-二-正辛烷氧基-7-二氟甲基金雀异黄素(5,4′-Di-n-octox-yl-7-gem-difluoromethylene-genistein,DodFMG)抑制人乳腺癌MCF-7细胞生长作用。方法:体外培养人乳腺癌MCF-7细胞和人乳腺HBL-100细胞,MTT法测定细胞活性;集落形成法检测细胞的平皿集落形成能力。结果:DodFMG对MCF-7细胞活性有明显的抑制作用,呈剂量依赖性,IC50值为11μmol/L;对HBL-100细胞的抑制作用较弱,IC50值为65μmol/L,其对MCF-7细胞的细胞毒选择指数为5.9(65/11)。DodFMG以浓度依赖方式抑制MCF-7细胞集落形成。结论:DodFMG是一种具有相对选择性的新型抗乳腺癌活性新化学实体。
Objective: To observe the effect of genistein (GEN) derivatives, namely 5,4’-di-n-octoxy-7-difluoromethyl genistein -yl-7-gem-difluoromethylene-genistein, DodFMG) inhibits the growth of human breast cancer MCF-7 cells. Methods: Human breast cancer MCF-7 cells and human breast HBL-100 cells were cultured in vitro. The cell viability was measured by MTT assay. The colony forming ability of cells was detected by colony formation assay. Results: DodFMG significantly inhibited the activity of MCF-7 cells in a dose-dependent manner with an IC50 value of 11μmol / L; its inhibitory effect on HBL-100 cells was weak with an IC50 value of 65μmol / L, The cytotoxicity index of the cells was 5.9 (65/11). DodFMG inhibited MCF-7 cell colony formation in a concentration-dependent manner. Conclusion: DodFMG is a new selective anti-breast cancer active chemical entity.