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目的探讨槲皮素抑制前列腺癌的作用机制。方法应用蛋白印迹技术检查槲皮素(quercetin)对雄激素受体(androgen receptor,AR)的辅调节因子c-Jun和cAMP应答元件结合蛋白的结合蛋白[cAMP response elem entb ind ing prote in(CREB)-b ind ing prote in,CBP]蛋白表达的影响;利用细胞转染技术检测c-Jun和CBP对AR功能的影响;免疫沉淀技术检验c-Jun与AR的蛋白-蛋白相互作用。结果槲皮素能够明显诱导c-Jun的高表达,高表达的c-Jun能够抑制AR的功能。槲皮素对CBP的蛋白表达水平无明显影响,而增加CBP的表达并不能逆转槲皮素对AR功能的抑制作用。免疫沉淀结果表明,c-Jun与AR存在蛋白-蛋白相互作用。结论槲皮素抑制前列腺癌的机制可能是通过c-Jun与AR的蛋白相互作用,而不是通过c-Jun竞争结合AR的辅激活因子CBP来实现的。
Objective To investigate the mechanism of quercetin inhibiting prostate cancer. METHODS: Western blotting was used to examine the effect of quercetin on the cAMP response eleme entb ing ing prote in (CREB), a co-regulator of the androgen receptor (AR), c-Jun and cAMP response element binding protein ) -b ing ing prote in, CBP] protein expression; the use of cell transfection technology to detect c-Jun and CBP on AR function; immunoprecipitation assay c-Jun and AR protein-protein interaction. Results Quercetin obviously induced high expression of c-Jun, and high expression of c-Jun could inhibit the function of AR. Quercetin had no significant effect on CBP protein expression, while increasing CBP expression did not reverse the inhibitory effect of quercetin on AR function. Immunoprecipitation results show that there is protein-protein interaction between c-Jun and AR. Conclusions The mechanism of quercetin inhibiting prostate cancer may be through protein interaction between c-Jun and AR rather than c-Jun competing for binding to AR co-activator CBP.