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目的利用经典雌激素受体(estrogenic receptor,ER)和G蛋白偶联雌激素受体(G protein-coupled estrogen receptor,GPER)阳性乳腺癌T47D细胞,探索丹参酮ⅡA(Tanshinone ⅡA)对细胞增殖活性的影响及其GPER介导与调节功能。方法以GPER激动剂G1和GPER拮抗剂G15为工具药干预,并应用GPER SiRNA转染构建GPER基因沉默的T47D细胞,利用MTT细胞增殖实验观察丹参酮ⅡA对T47D细胞增殖速率的影响及GPER的介导作用。利用Western blot方法检测丹参酮ⅡA对T47D细胞GPER表达情况的影响。结果 1×10-5mol·L-1~1×10-7mol·L-1丹参酮ⅡA能够明显抑制T47D细胞增殖,且该抑制作用可被G1拮抗,可被G15增强。丹参酮ⅡA作用于GPER基因沉默的T47D细胞,该细胞表现出更为明显的生长抑制效应。Western blot测定结果表明,1×10-5mol·L-1和1×10-6mol·L-1丹参酮ⅡA可使T47D细胞GPER蛋白表达明显降低。结论丹参酮ⅡA具有抑制乳腺癌T47D细胞增殖的作用,该抑制作用可经GPER途径介导;且丹参酮ⅡA具有对靶细胞GPER表达的调节功能。
Objective To explore the effect of Tanshinone Ⅱ A on the proliferation of human breast cancer cell line T47D using classical estrogenic receptor (ER) and G protein-coupled estrogen receptor (GPER) positive breast cancer T47D cells Effect and its GPER-mediated and regulatory functions. Methods GPER agonist G1 and GPER antagonist G15 were used as a tool to interfere GPT1 gene silencing T47D cells by GPER siRNA. The effect of Tanshinone ⅡA on the proliferation of T47D cells and GPER-mediated effect. The effect of Tanshinone ⅡA on GPER expression in T47D cells was detected by Western blot. Results Tanshinone ⅡA (1 × 10-5mol·L -1 ~1 × 10-7mol·L -1) could significantly inhibit the proliferation of T47D cells. The inhibitory effect was antagonized by G1 and could be enhanced by G15. Tanshinone IIA acts on T47D cells with GPER silencing, which shows a more pronounced growth inhibitory effect. The results of Western blot showed that the expression of GPER protein in T47D cells was significantly decreased by 1 × 10-5mol·L-1 and 1 × 10-6mol·L-1 tanshinone ⅡA. Conclusion Tanshinone Ⅱ A can inhibit the proliferation of breast cancer T47D cells. The inhibitory effect of Tanshinone ⅡA can be mediated by GPER pathway. Tanshinone Ⅱ A can regulate the GPER expression of target cells.