Lee YoungJoo, Jin YoungRan, Lim WonChung, Ji SangMi, Choi Songho, Jang Siyoul, Lee SeungKi
Department of Bioscience and Biotechnology, College of Engineering, Institute of Biotechnology, Sejong University, Seoul, South Korea.
J Steroid Biochem Mol Biol. 2003 Mar;84(4):463-8. doi: 10.1016/s0960-0760(03)00067-0.
We have examined the possibility that a component of Panax ginseng, ginsenoside-Rh1, acts by binding to steroid hormone receptors such as receptors for estrogen, glucocorticoid, androgen, and retinoic acid. Ginsenoside-Rh1 activated the transcription of the estrogen-responsive luciferase reporter gene in MCF-7 breast cancer cells at a concentration of 50 microM. Activation was inhibited by the specific estrogen receptor antagonist ICI 182,780, indicating that the estrogenic effect of ginsenoside-Rh1 is estrogen receptor dependent. Ginsenoside-Rh1 induction of luciferase activity was dose-dependent in CV-1 cells transiently transfected with estrogen receptor and reporter plasmids. Next, we evaluated the ability of ginsenoside-Rh1 to induce the estrogen-responsive genes in MCF-7 cells. Ginsenoside-Rh1 increased c-fos and pS2 at the mRNA levels at 24h after treatment, although the effects were not as prominent as 17beta-estradiol. Western blot analysis showed that progesterone receptor protein was induced at 24h of treatment of ginsenoside-Rh1. However, ginsenoside-Rh1 failed to activate the glucocorticoid receptor, the androgen receptor, or the retinoic acid receptor in CV-1 cells transiently transfected with the corresponding steroid hormone receptors and hormone responsive reporter plasmids. These data support our hypothesis that ginsenoside-Rh1 acts as a weak phytoestrogen, presumably by binding and activating the estrogen receptor.
我们研究了人参的一种成分人参皂苷-Rh1是否通过与类固醇激素受体（如雌激素、糖皮质激素、雄激素和视黄酸受体）结合来发挥作用。人参皂苷-Rh1在浓度为50微摩尔时可激活MCF-7乳腺癌细胞中雌激素反应性荧光素酶报告基因的转录。特异性雌激素受体拮抗剂ICI 182,780可抑制这种激活，表明人参皂苷-Rh1的雌激素作用依赖于雌激素受体。在用雌激素受体和报告质粒瞬时转染的CV-1细胞中，人参皂苷-Rh1诱导荧光素酶活性呈剂量依赖性。接下来，我们评估了人参皂苷-Rh1在MCF-7细胞中诱导雌激素反应基因的能力。处理24小时后，人参皂苷-Rh1在mRNA水平上增加了c-fos和pS2，尽管其作用不如17β-雌二醇显著。蛋白质印迹分析表明，人参皂苷-Rh1处理24小时可诱导孕激素受体蛋白。然而，在用相应类固醇激素受体和激素反应性报告质粒瞬时转染的CV-1细胞中，人参皂苷-Rh1未能激活糖皮质激素受体、雄激素受体或视黄酸受体。这些数据支持了我们的假设，即人参皂苷-Rh1作为一种弱植物雌激素，可能是通过结合并激活雌激素受体来发挥作用的。
