Department of Physiology, University of Maryland School of Medicine, Baltimore, Maryland, USA.
Antioxid Redox Signal. 2011 Jan 15;14(2):207-19. doi: 10.1089/ars.2010.3234. Epub 2010 Nov 23.
Obesity, the metabolic syndrome, and aging share several pathogenic features in both humans and non-human primates, including insulin resistance and inflammation. Since muscle and liver are considered key integrators of metabolism, we sought to determine in biopsies from lean and obese aging rhesus monkeys the nature of defects in insulin activation and, further, the potential for mitigation of such defects by an in vivo insulin sensitizer, rosiglitazone, and a thiazolidinedione activator of the peroxisome proliferator-activated receptor gamma. The peroxisome proliferator-activated receptor gamma agonist reduced hyperinsulinemia, improved insulin sensitivity, lowered plasma triglycerides and free fatty acids, and increased plasma adiponectin. In muscle of obese monkeys, previously shown to exhibit defective insulin signaling, the insulin sensitizer improved insulin activation of atypical protein kinase C (aPKC), the defective direct activation of aPKC by phosphatidylinositol (PI)-3,4,5-(PO₄)₃, and 5'-AMP-activated protein kinase and increased carnitine palmitoyltransferase-1 mRNA expression, but it did not improve insulin activation of insulin receptor substrate (IRS)-1-dependent PI 3-kinase (IRS-1/PI3K), protein kinase B, or glycogen synthase. We found that, although insulin signaling was impaired in muscle, insulin activation of IRS-1/PI3K, IRS-2/PI3K, protein kinase B, and aPKC was largely intact in liver and that rosiglitazone improved insulin signaling to aPKC in muscle by improving responsiveness to PI-3,4,5-(PO₄)₃.
肥胖、代谢综合征和衰老在人类和非人类灵长类动物中具有一些共同的发病特征,包括胰岛素抵抗和炎症。由于肌肉和肝脏被认为是代谢的关键整合器,我们试图确定在瘦猴和肥胖衰老猴的活检中,胰岛素激活的缺陷性质,以及体内胰岛素增敏剂罗格列酮和过氧化物酶体增殖物激活受体 γ 的噻唑烷二酮激活剂是否可以减轻这些缺陷。过氧化物酶体增殖物激活受体 γ 激动剂降低了高胰岛素血症,改善了胰岛素敏感性,降低了血浆甘油三酯和游离脂肪酸,增加了血浆脂联素。在先前显示存在胰岛素信号传导缺陷的肥胖猴肌肉中,胰岛素增敏剂改善了非典型蛋白激酶 C(aPKC)的胰岛素激活,PI-3,4,5-(PO₄)₃和 5'-AMP 激活蛋白激酶对 aPKC 的缺陷直接激活以及肉毒碱棕榈酰转移酶-1 mRNA 表达,但它并没有改善胰岛素受体底物(IRS)-1 依赖性 PI 3-激酶(IRS-1/PI3K)、蛋白激酶 B 或糖原合酶的胰岛素激活。我们发现,尽管肌肉中的胰岛素信号传导受损,但 IRS-1/PI3K、IRS-2/PI3K、蛋白激酶 B 和 aPKC 的胰岛素激活在肝脏中基本完整,并且罗格列酮通过改善对 PI-3,4,5-(PO₄)₃的反应性来改善肌肉中 aPKC 的胰岛素信号传导。