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目的探讨法尼酯X受体(FXR)的激活是否抑制结肠癌细胞的生长。方法对人结肠癌HCT-116细胞进行体外培养,用四唑氮蓝还原法(MTT)和流式细胞仪测定FXR特异性激动剂GW4064对结肠癌HCT-116细胞生长的抑制作用,同时应用RT-PCR方法检测其FXR mRNA及VEGF mRNA的表达。结果 FXR特异性激动剂GW4064可上调结肠癌HCT-116细胞的FXR mRNA表达,下调VEGF mRNA的表达;对结肠癌HCT-116细胞的生长具有明显的抑制作用,并促进结肠癌HCT116细胞的凋亡,且均呈剂量及时间依赖关系。结论 FXR特异性激动剂GW4064可以显著抑制结肠癌HCT116细胞的生长,激活FXR受体可能为结肠癌的治疗提供一种潜在的靶点。
Objective To investigate whether the activation of farnesol X receptor (FXR) inhibits the growth of colon cancer cells. Methods Human colon cancer HCT-116 cells were cultured in vitro. The inhibitory effect of FXR-specific agonist GW4064 on the growth of human colon cancer HCT-116 cells was determined by MTT assay and flow cytometry. RT- -PCR method to detect the expression of FXR mRNA and VEGF mRNA. Results FXR-specific agonist GW4064 upregulated FXR mRNA expression and down-regulated the expression of VEGF mRNA in colon cancer HCT-116 cells, significantly inhibited the growth of HCT-116 colon cancer cells and promoted the apoptosis of colon cancer HCT116 cells , And were dose-and time-dependent. Conclusion FX40-specific agonist GW4064 can significantly inhibit the growth of human colon cancer HCT116 cells. Activation of FXR receptor may provide a potential target for the treatment of colon cancer.