β(3)-肾上腺素能受体激动剂CL-316,243对肥胖糖尿病KKAy小鼠脂肪组织中脂联素、脂联素受体及肿瘤坏死因子-α表达的影响
The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice.
作者信息
Fu Ling, Isobe Kazumasa, Zeng Qin, Suzukawa Kazumi, Takekoshi Kazuhiro, Kawakami Yasushi
机构信息
Graduate School of Comprehensive Human Sciences, University of Tsukuba, Tsukuba, Ibaraki 305-8575, Japan.
出版信息
Eur J Pharmacol. 2008 Apr 14;584(1):202-6. doi: 10.1016/j.ejphar.2008.01.028. Epub 2008 Feb 5.
We investigated the effects of beta(3)-adrenoceptor agonist, 5-[(2R)-2-[[(2R)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benzodioxole-2,2-dicarboxylate (CL-316,243) in obese diabetic KKAy mice. Two weeks' subcutaneous administration of CL-316,243 reduced serum levels of glucose, insulin, triglyceride, free fatty acid and tumor necrosis factor-alpha (TNF-alpha), and increased adiponectin. Adiponectin, adiponectin receptors and beta(3)-adrenoceptor mRNA expressions were reduced in epididymal white adipose tissue in KKAy mice, and CL-316,243 recovered these mRNA expressions. Meanwhile, CL-316,243 suppressed the overexpressed mRNA level of TNF-alpha in both epididymal white adipose tissue and brown adipose tissue. These data suggest that the normalization of adiponectin, adiponectin receptors and TNF-alpha may result in the amelioration of obesity-induced insulin resistance.
我们研究了β(3)-肾上腺素能受体激动剂5-[(2R)-2-[[(2R)-2-(3-氯苯基)-2-羟乙基]氨基]丙基]-1,3-苯并二恶唑-2,2-二羧酸酯（CL-316,243）对肥胖糖尿病KKAy小鼠的影响。连续两周皮下注射CL-316,243可降低血清葡萄糖、胰岛素、甘油三酯、游离脂肪酸和肿瘤坏死因子-α（TNF-α）水平，并增加脂联素水平。KKAy小鼠附睾白色脂肪组织中脂联素、脂联素受体和β(3)-肾上腺素能受体mRNA表达降低，而CL-316,243可恢复这些mRNA表达。同时，CL-316,243抑制了附睾白色脂肪组织和棕色脂肪组织中TNF-α过表达的mRNA水平。这些数据表明，脂联素、脂联素受体和TNF-α的正常化可能导致肥胖诱导的胰岛素抵抗得到改善。
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