目的:探讨槲皮素(quercetin,Que)的植物雌激素作用及其可能的受体作用机制。方法:采用噻唑蓝(MTT)比色法测定槲皮素对雌激素依赖性乳腺癌细胞T47D和非雌激素依赖性乳腺癌细胞MDA-MB231的细胞增殖作用,流式细胞术对T47D细胞的增殖情况进行分析。Western blot方法测定槲皮素对T47D细胞雌激素受体两种亚型ERα和ERβ表达的影响,并以雌激素受体拮抗剂ICI182,780为工具药来评价槲皮素发挥雌激素样作用与雌激素受体的关系。结果:与溶剂对照组相比较,槲皮素(10,20,40μmol·L-1)能显著促进T47D细胞的增殖,而抑制雌激素受体阴性MDA-MB231细胞,并将T47D细胞周期由G1期向S期推进,促进DNA合成,提高细胞分裂增殖指数;且槲皮素促进T47D细胞增殖作用被雌激素受体拮抗剂所拮抗,槲皮素在10μmol·L-1可明显诱导T47D细胞ERα蛋白表达,而对ERβ表达没有影响。当与ICI 182,780共孵育T47D细胞ERα表达被拮抗。结论:槲皮素具有雌激素活性,此作用是通过影响雌激素受体ERα蛋白表达介导的。
OBJECTIVE To investigate the phytoestrogenic effects and its possible receptor mechanism of quercetin.METHODS Effects of quercetin on the cell proliferation were tested in ER-positive T47 D cells and ER-negative MDA-MB231 cells by MTT measurement.Cell cycle was examined by flow cytometry.And T47 D cells were treated with quercetin for 48 h,total cell extracts were examined for the levels of ERαand ERβprotein by Western blot analysis.The estrogen-like effects of quercetin and the its relationship with estrogen-receptors were evaluated by pure estrogen receptor antagonist ICI182,780.RESULTSQuercetin(10,20,40μmol·L-1)stimulated proliferation of ER-positive T47 D cells compared with solvent control,whereas ER-negative MDA-MB231 cell was inhibited,and the cell cycle was impelled from G1 to S to synthesize DNA,and PI also increased.The bossting function on T47 D cell proliferation was inhibited by estrogen receptor antagonist ICI182,780.Quercetin(10μmol·L-1)could evidently induce expression of ERαprotein,but without any effect on ERβprotein levels.When jointly incubated with ICI182,780,ERαprotein could be inhibited.CONCLUSION Quercetin has the estrogen-like activities which are induced by affecting expression of ERαprotein.