Leung Kar Wah, Cheng Yuen-Kit, Mak Nai Ki, Chan Kelvin K C, Fan T P David, Wong Ricky N S
Department of Biology, Hong Kong Baptist University, Hong Kong.
FEBS Lett. 2006 May 29;580(13):3211-6. doi: 10.1016/j.febslet.2006.04.080. Epub 2006 May 4.
We here provide definitive evidence that ginsenoside-Rg1, the pharmacologically active component of ginseng, is a functional ligand of the glucocorticoid receptor (GR) as determined by fluorescence polarization assay. Rg1 increased the phosphorylation of GR, phosphatidylinositol-3 kinase (PI3K), Akt/PKB and endothelial nitric oxide synthase (eNOS) leading to increase nitric oxide (NO) production in human umbilical vein endothelial cell. Rg1-induced eNOS phosphorylation and NO production were significantly reduced by RU486, LY294,002, or SH-6. Also, knockdown of GR completely eliminated the Rg1-induced NO production. This study revealed that Rg1 can indeed serve as an agonist ligand for GR and the activated GR can induce rapid NO production from eNOS via the non-transcriptional PI3K/Akt pathway.
我们在此提供确凿证据，通过荧光偏振测定法确定，人参的药理活性成分人参皂苷-Rg1是糖皮质激素受体（GR）的功能性配体。Rg1增加了GR、磷脂酰肌醇-3激酶（PI3K）、Akt/PKB和内皮型一氧化氮合酶（eNOS）的磷酸化，从而导致人脐静脉内皮细胞中一氧化氮（NO）生成增加。RU486、LY294,002或SH-6显著降低了Rg1诱导的eNOS磷酸化和NO生成。此外，GR的敲低完全消除了Rg1诱导的NO生成。本研究表明，Rg1确实可作为GR的激动剂配体，并且活化的GR可通过非转录性PI3K/Akt途径诱导eNOS快速生成NO。
