摘要
目的探讨槲皮素(quercetin,Que)和补骨脂素(psor-alen,Pso)对人类乳腺癌细胞株增殖的影响。方法采用流式细胞术和蛋白印迹法检测槲皮素和补骨脂素对雌激素依赖性乳腺癌细胞MCF-7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和补骨脂素发挥雌激素样作用与雌激素受体的关系。结果①槲皮素、补骨脂素在10μmol.L-1可使MCF-7细胞增殖指数明显升高,增加S期细胞的比例,与10-3μmon.L-1E2阳性对照组的变化趋势一致。当ICI182,780分别与E2、金雀异黄素、槲皮素、补骨脂素共孵育48 h后,E2、金雀异黄素、槲皮素、补骨脂素的增殖效应被抑制,细胞周期S期细胞数比例下降,G0/G1期细胞数比例上升。②10μmol.L-1槲皮素和10μmol.L-1补骨脂素均上调MCF-7细胞ERα蛋白水平,而对ERβ蛋白表达没有影响;当分别与ICI182,780共孵育MCF-7细胞ERα蛋白表达被拮抗。结论槲皮素和补骨脂素具有雌激素活性,此作用是通过雌激素受体(ER)介导的;产生的类似金雀异黄素促进MCF-7细胞增殖的作用是通过增加ERα表达实现的。
Aim To investigate the effects of quercetin and psoralen on the proliferation of human breast carcinoma cells in vitro. Methods Effects of quercetin and psoralen on the cell proliferation was tested in ER-positire MCF-7 cells by flow cytometer and Western blot.And the estrogen-like effect of psoralen and its relation with the estrogen-receptor were evaluated by pure estrogen receptor antagonist ICI182,780 as a tool. Resuits ① Psoralen （ 10 μmon·L^-1） and quercetin （ 10μmon·L^-1） stimulated proliferation of MCF - 7 cells compared with vehicle control, and the cell cycle was impulsed from G1 to S, DNA synthesizing was enhanced. It was also found the above function on boosting MCF-7 cell proliferation could be inhibited by adding estrogen receptor antagonism ICI182,780. ② Psoralen（ 10μmon·L^-1） and quercetin （10μmon·L^-1） up-regulated ERα protein levels without altering ERβ levels. The above up-regulation on ERα protein could be inhibited by adding estrogen receptor antagonism ICI182,780. Conclusions Psoralen and quercetin have the estrogen-like activities through the estrogen response pathway. And they exert estrogenic activity to MCF-7 cell proliferation through interaction with ERα expression.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2009年第5期601-605,共5页
Chinese Pharmacological Bulletin
基金
国家自然科学基金资助项目(No30371775,30510403202,30540420032)
教育部长江学者和创新团队发展计划资助项目(NoIRT0413)
教育部博士点科研基金资助项目(No20050026012)
