目的 探讨人参皂苷Rg₁(ginsenoside Rg₁,G-Rg₁)对人肝HL-7702细胞糖皮质激素受体(GR)的调节作用。方法 将含有糖皮质激素受体反应元件(GRE)的荧光素酶报告基因的表达质粒载体pGRE-tk-LUC与内参照基因载体质粒pRL-SV40,通过脂质体介导瞬时转染至人肝HL-7702细胞中,利用双荧光素酶报告基因检测系统,观察报告基因的表达变化;利用Western blotting方法 检测药物对细胞GR蛋白表达的影响。结果 G-Rg₁与地塞米松均可诱导pGRF-tk-LUC报告基因表达,且呈剂量依赖性,而且这种诱导作用可以被糖皮质激素受体阻断剂RU486(Mifepristone)所阻断,G-Rg₁对细胞GR蛋白表达有显著的抑制作用。结论 G-Rg₁在体外能够表现出一些类似糖皮质激素样的生物活性,可能是GR的配体。

Objective To investigate the effect of ginsenoside Rg,(G-Rg₁)on regulation of glucocorticoid receptor (GR) in HL-7702 cells. Methods HL-7702 Cells were transiently cotransfected by Lipofect AMINE^TE 2000 with pGRE-tk-LLTC reporter plasmid and pRL-SV40 plasmid. The effects of G-Rg₁, and Dexamethasone on luciferase activity expression were detected by Dual-Luciferase Reporter Assays，the protein expression of GR in HL-7702 cells was analyzed by Western blotting assay，respectively. Results A dose-dependent induction of the reporter gene was observed in response to Dex or G-Rg₁，and the inductive effect was blocked by treatment with the antiglucocorticoid RU486(Mifepristone).G-Rg, also down-regulated the GR protein expression in HL-7702 cells.Conclusion These Results strongly indicate that G-Rg₁，which may be a ligand of GR，has some glucocorticoid-like effect in vitro.

国家自然科学基金资助项目(30472271)