Folli F, Kahn C R, Hansen H, Bouchie J L, Feener E P
Department of Medicine I, I.R.C.C.S.H. San Raffaele, Milano, Italy.
J Clin Invest. 1997 Nov 1;100(9):2158-69. doi: 10.1172/JCI119752.
To investigate potential interactions between angiotensin II (AII) and the insulin signaling system in the vasculature, insulin and AII regulation of insulin receptor substrate-1 (IRS-1) phosphorylation and phosphatidylinositol (PI) 3-kinase activation were examined in rat aortic smooth muscle cells. Pretreatment of cells with AII inhibited insulin-stimulated PI 3-kinase activity associated with IRS-1 by 60%. While AII did not impair insulin-stimulated tyrosine phosphorylation of the insulin receptor (IR) beta-subunit, it decreased insulin-stimulated tyrosine phosphorylation of IRS-1 by 50%. AII inhibited the insulin-stimulated association between IRS-1 and the p85 subunit of PI 3-kinase by 30-50% in a dose-dependent manner. This inhibitory effect of AII on IRS-1/PI 3-kinase association was blocked by the AII receptor antagonist saralasin, but not by AT1 antagonist losartan or AT2 antagonist PD123319. AII increased the serine phosphorylation of both the IR beta-subunit and IRS-1. In vitro binding experiments showed that autophosphorylation increased IR binding to IRS-1 from control cells by 2.5-fold versus 1.2-fold for IRS-1 from AII-stimulated cells, suggesting that AII stimulation reduces IRS-1's ability to associate with activated IR. In addition, AII increased p85 serine phosphorylation, inhibited the total pool of p85 associated PI 3-kinase activity, and decreased levels of the p50/p55 regulatory subunit of PI 3-kinase. These results suggest that activation of the renin-angiotensin system may lead to insulin resistance in the vasculature.
为研究血管中血管紧张素II(AII)与胰岛素信号系统之间的潜在相互作用,我们检测了大鼠主动脉平滑肌细胞中胰岛素和AII对胰岛素受体底物-1(IRS-1)磷酸化及磷脂酰肌醇(PI)3-激酶激活的调节作用。用AII预处理细胞可使与IRS-1相关的胰岛素刺激的PI 3-激酶活性降低60%。虽然AII并不损害胰岛素刺激的胰岛素受体(IR)β亚基的酪氨酸磷酸化,但它使胰岛素刺激的IRS-1酪氨酸磷酸化降低了50%。AII以剂量依赖的方式使胰岛素刺激的IRS-1与PI 3-激酶p85亚基之间的结合减少30%-50%。AII对IRS-1/PI 3-激酶结合的这种抑制作用可被AII受体拮抗剂沙拉新阻断,但不能被AT1拮抗剂氯沙坦或AT2拮抗剂PD123319阻断。AII增加了IRβ亚基和IRS-1的丝氨酸磷酸化。体外结合实验表明,自磷酸化使对照细胞中IR与IRS-1的结合增加了2.5倍,而AII刺激细胞中IRS-1与IR的结合仅增加了1.2倍,这表明AII刺激降低了IRS-1与活化IR结合的能力。此外,AII增加了p85丝氨酸磷酸化,抑制了与p85相关的PI 3-激酶的总活性池,并降低了PI 3-激酶p50/p55调节亚基的水平。这些结果表明,肾素-血管紧张素系统的激活可能导致血管中的胰岛素抵抗。