南方医科大学学报

南方医科大学学报 ›› 2014, Vol. 34 ›› Issue (10): 1511-.

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苯并二氢吡喃衍生物对人类乳腺癌细胞增殖的影响

侯进，李萍，曾菊绒，胥晓丽，熊晓云，弥曼   

  • 出版日期:2014-10-20 发布日期:2014-10-20

Effect of xy2004, a centchroman derivative, on proliferation of MCF-7 cells in vitro and
the mechanism

  • Online:2014-10-20 Published:2014-10-20

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摘要： 目的研究苯并二氢吡喃衍生物xy2004对乳腺癌细胞增殖的影响。方法采用MTT比色法测定化合物对MCF-7细胞的
增殖作用；用流式细胞术测定化合物对细胞凋亡的影响，用放射性配体结合法考察化合物与雌激素受体（ER）的亲和力，用蛋白
印记杂交法观察细胞内凋亡蛋白的变化。结果低浓度的xy2004促进MCF-7细胞增殖，其增殖作用可被tamoxifen阻断；高浓
度xy2004 抑制MCF-7 细胞增殖，诱导细胞凋亡，Bax 蛋白表达增强，Bcl-2 蛋白表达降低；xy2004 对ERα和ERβ的IC50分别为
7.38×10-5 mol/L 和4.12×10-7 mol/L。结论化合物xy2004低浓度促进MCF-7细胞增殖，其增殖作用机制与ERα激动有关，高浓
度抑制MCF-7细胞增殖，抗增殖作用与诱导细胞凋亡相关。

Abstract: Objective To investigate the effect of xy2004, a centchroman derivative, on the proliferation of MCF-7 cells and the
mechanisms. Methods The effects of xy2004 on MCF-7 cell proliferation and apoptosis were evaluated with MTT assay and
flow cytometry, respectively. The expressions of the apoptosis-related proteins were examined with Western blotting.
Competitive estrogen-receptor binding assay was used to investigate the affinity of xy2004 to estrogen receptors (ER). Results
xy2004 induced proliferation of MCF-7 cells at low concentrations but inhibited cell proliferation at high concentrations. The
application of tamoxifen inhibited xy2004-induced proliferation of MCF-7 cells. The relative binding affinity of xy9906 to ERα
and ERβ, presented as the IC50 value, was 7.38×10-5 mol/L and 4.12×10-7 mol/L, respectively. Treatment of MCF-7 cells with
high-concentration xy2004 reduced the cellular expression of Bcl-2 protein and increased Bax protein expression. Conclusion
At low concentrations, xy2004 directly stimulates the proliferation of MCF -7 cells through ligand-receptor binding, and at
high concentrations, it inhibits the cell proliferation by regulating the expression levels of the apoptosis-related proteins.