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首页> 外文期刊>中国药理学报：英文版 >Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro
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Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro

机译：新型α-甲基-α-苯氧基丙酸酯衍生物的胰岛素增敏作用

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摘要

Aim: To examine the insulin sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative YY20 in insulin-sensitive cell lines. Methods: The peroxisome proliferator-activated receptorγ(PPARγ) agonist bioactivities of YY20 were detected by a preadipocyte differentiation assay. RT-PCR and Western blotting analysis were used to detect the expression of the target gene or protein.The effects of YY20 on insulin-mediated glucose consumption were determined in the HepG2 human hepatocellular carcinoma line. Results: YY20 could enhance the differentiation of preadipocytes to adipocytes and upregulate the gene ex-pression of PPAR),2, as well as the protein expression of insulin receptor sub-strate-1 (IRS-1), glucose transporter-4 (GLUT4), and adiponectin (ACRP30). The effects on GLUT4 and ACRP30 could be reversed by the PPARγinhibitor SR-202.Furthermore, YY20 efficiently reduced glucose consumptions in HepG2 cells after 24 h culture, and the effects were related to insulin and YY20 concentrations.Conclusion: YY20, a potential insulin-sensitizing agent like rosiglitazone, could enhance glucose consumption in HepG2 cells in a concentration- and insulin-dependent manner. It may improve the insulin resistance associated with type 2 diabetes.
机译：目的：检查新型α-甲基-α-苯氧基丙酸酯衍生物YY20在胰岛素敏感细胞系中的胰岛素敏化作用。方法：通过前脂肪细胞分化测定检测过氧化物酶体增殖物激活的受体γ（PPARγ）的YY20激动剂生物活体。 RT-PCR和Western印迹分析用于检测靶基因或蛋白质的表达。在HepG2人肝细胞癌线中测定了YY20对胰岛素介导的葡萄糖消耗的影响。结果：YY20可以增强前脂肪细胞对脂肪细胞的分化，并上调PPAR的基因，2，以及胰岛素受体亚旋转 - 1（IRS-1），葡萄糖转运蛋白-4的蛋白质表达（Glut4 ）和脂肪蛋白（ACRP30）。对Glut4和Acrp30的影响可以通过PPARγIBHIBIERSR-202来逆转。许多，YY20在24小时培养后的HepG2细胞中有效地降低了HepG2细胞的葡萄糖消耗，并且效果与胰岛素和YY20浓度有关。结论：YY20，潜在的胰岛素 - 令人敏化剂如罗格列酮，可以以浓度和胰岛素依赖的方式增强HepG2细胞中的葡萄糖消耗。它可以改善与2型糖尿病相关的胰岛素抗性。

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  • 来源
    《中国药理学报：英文版》 |2007年第3期|417-422|共6页
  • 作者

    Hao-shu WU; Juan-hong YU; Ying-yin LI; Yu-she YANG; Qiao-jun HE; Yi-jia LOU; Ru-yun JI;

  • 作者单位

    Department of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhefiang University,Hangzhou 310058,China;

    State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Graduate School of the Chinese Academy of Sciences,Shanghai 201203,China;

    Department of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhefiang University,Hangzhou 310058,China;

    State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Graduate School of the Chinese Academy of Sciences,Shanghai 201203,China;

    Department of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhefiang University,Hangzhou 310058,China;

    Department of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhefiang University,Hangzhou 310058,China;

    State Key Laboratory of Drug Research,Shanghai Institute of Materia Medica,Shanghai Institutes for Biological Sciences,Graduate School of the Chinese Academy of Sciences,Shanghai 201203,China;

  • 收录信息 中国科学引文数据库(CSCD);中国科技论文与引文数据库(CSTPCD);
  • 原文格式 PDF
  • 正文语种 chi
  • 中图分类 药学;
  • 关键词

    YY20; peroxisome proliferator-activated receptor γ; insulin sensitivity; glucose consumption;

    机译：YY20;过氧化物酶体增殖物激活受体γ;胰岛素敏感性葡萄糖消耗;
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