Norris Andrew W, Chen Lihong, Fisher Simon J, Szanto Ildiko, Ristow Michael, Jozsi Alison C, Hirshman Michael F, Rosen Evan D, Goodyear Laurie J, Gonzalez Frank J, Spiegelman Bruce M, Kahn C Ronald
Research Division, Joslin Diabetes Center, One Joslin Place, Boston, Massachusetts 02215, USA.
J Clin Invest. 2003 Aug;112(4):608-18. doi: 10.1172/JCI17305.
Activation of peroxisome proliferator-activated receptor gamma (PPARgamma) by thiazolidinediones (TZDs) improves insulin resistance by increasing insulin-stimulated glucose disposal in skeletal muscle. It remains debatable whether the effect of TZDs on muscle is direct or indirect via adipose tissue. We therefore generated mice with muscle-specific PPARgamma knockout (MuPPARgammaKO) using Cre/loxP recombination. Interestingly, MuPPARgammaKO mice developed excess adiposity despite reduced dietary intake. Although insulin-stimulated glucose uptake in muscle was not impaired, MuPPARgammaKO mice had whole-body insulin resistance with a 36% reduction (P < 0.05) in the glucose infusion rate required to maintain euglycemia during hyperinsulinemic clamp, primarily due to dramatic impairment in hepatic insulin action. When placed on a high-fat diet, MuPPARgammaKO mice developed hyperinsulinemia and impaired glucose homeostasis identical to controls. Simultaneous treatment with TZD ameliorated these high fat-induced defects in MuPPARgammaKO mice to a degree identical to controls. There was also altered expression of several lipid metabolism genes in the muscle of MuPPARgammaKO mice. Thus, muscle PPARgamma is not required for the antidiabetic effects of TZDs, but has a hitherto unsuspected role for maintenance of normal adiposity, whole-body insulin sensitivity, and hepatic insulin action. The tissue crosstalk mediating these effects is perhaps due to altered lipid metabolism in muscle.
噻唑烷二酮类药物(TZDs)激活过氧化物酶体增殖物激活受体γ(PPARγ),通过增加胰岛素刺激的骨骼肌葡萄糖代谢来改善胰岛素抵抗。TZDs对肌肉的作用是直接的还是通过脂肪组织间接发挥作用,目前仍存在争议。因此,我们利用Cre/loxP重组技术构建了肌肉特异性PPARγ基因敲除(MuPPARγKO)小鼠。有趣的是,尽管饮食摄入量减少,但MuPPARγKO小鼠仍出现了肥胖。虽然胰岛素刺激的肌肉葡萄糖摄取没有受损,但MuPPARγKO小鼠存在全身胰岛素抵抗,在高胰岛素钳夹试验中维持正常血糖所需的葡萄糖输注速率降低了36%(P<0.05),这主要是由于肝脏胰岛素作用显著受损。当给予高脂饮食时,MuPPARγKO小鼠出现了与对照组相同的高胰岛素血症和葡萄糖稳态受损。同时给予TZDs治疗可在一定程度上改善MuPPARγKO小鼠中这些由高脂饮食诱导的缺陷,改善程度与对照组相同。MuPPARγKO小鼠肌肉中几种脂质代谢基因的表达也发生了改变。因此,肌肉PPARγ对于TZDs的抗糖尿病作用并非必需,但在维持正常肥胖、全身胰岛素敏感性和肝脏胰岛素作用方面具有迄今未被认识的作用。介导这些作用的组织间相互作用可能是由于肌肉中脂质代谢的改变。