人参皂苷Rb3(ginsenoside Rb3,GRb3)是西洋参茎叶总皂苷(Panax quinquefolius Saponin of stem and leaf,PQS)的主要入血成分之一,既往研究显示其具有雌激素受体激动效应。本研究观察GRb3对ox-LDL诱导人脐静脉内皮细胞氧化应激与功能障碍的保护作用。药物干预后检测细胞内SOD、NOS活性与MDA含量,ELISA法进行细胞培养上清液ET-1与NO含量的测定,real time RT-PCR方法检测细胞中eNOS和iNOS的转录水平,Western blotting方法测定丝氨酸/苏氨酸蛋白激酶Akt的磷酸化水平。与ox-LDL损伤模型组相比,GRb3增高细胞内SOD活力,降低细胞内MDA含量与总NOS活性,减少细胞ET-1和NO合成,升高eNOS的转录水平及降低iNOS的转录水平,且能调节Akt的磷酸化水平,从而发挥保护作用,给予雌激素受体抑制剂ICI182780预处理后上述保护作用消失。结果提示,GRb3可通过雌激素受体的介导发挥抗ox-LDL对内皮细胞的损伤作用,其作用效应与17β-雌二醇相似。
Ginsenoside Rb3 (GRb3) is one of the main components in plasma of Panax quinquefolius Saponin of stem and leaf (PQS), which can be into human plasma. Previous studies have found PQS has estrogen-like vascular protective effects. In the present study, we investigated the estrogen-like protective effect of GRb3 on oxidative stress and dysfunction of endothelial cells induced by oxidized low-density lipoprotein. The activities of SOD, NOS and the contents of MDA in the cell lysate were examined by enzyme method or spectrophotometry. The NO and ET-1 concentrations in the cell culture supernatant were measured by ELISA method. The iNOS and eNOS mRNA expression were measured by real time RT-PCR, while the phosphorylation levels of Akt was measured by Western blotting. The results showed that GRb3 could enhance the activity of SOD, reduce the content of MDA, increase the level of NOS, NO, ET-1 and iNOS mRNA expression while decrease the eNOS mRNA expression and the phosphorylation level of Akt. These effects were blocked by estrogen receptor antagonist ICI182780. GRb3 can play a role in protecting vascular endothelial cells by estrogen receptors, the protective mechanism is similar to 17-β estrodiol.