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Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro

Acta Pharmacologica Sinica 2007年第3期28卷 417-422页

作者： Hao-shu WU~(2,4) Juan-hong YU~(3,4) Ying-yin LI~2 Yu-she YANG~3 Qiao-jun HE~2 Yi-jia LOU~(2,5) Ru-yun JI~3 ~2Department of Pharmacology and Toxicology,College of Pharmaceutical Sciences,Zhejiang University,Hangzhou 310058,China ~3State 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 Zhejiang University Hangzhou China Department of 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 China

Aim:To examine the insulin sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative yy20 in insulin-sensitive cell ***:Theperoxisome proliferator-activated receptor γ（PPARγ）agonist bioactivities of yy20were detected by a preadipocyte differentiation ***-PCR and Westernblotting analysis were used to detect the expression of the target gene or *** effects of yy20 on insulin-mediated glucose consumption were determined inthe HepG2 human hepatocellular carcinoma ***:yy20 could enhancethe differentiation of preadipocytes to adipocytes and upregulate the gene ex-pression of PPARγ2,as well as the protein expression of insulin receptor sub-strate-1（IRS-1）,glucose transporter-4（GLUT4）,and adiponectin（ACRP30）.Theeffects on GLUT4 and ACRP30 could be reversed by the PPARγ inhibitor ***,yy20 efficiently reduced glucose consumptions in HepG2 cells after24 h culture,and the effects were related to insulin and yy20 ***:yy20,a potential insulin-sensitizing agent like rosiglitazone,couldenhance glucose consumption in HepG2 cells in a concentration-and insulin-dependent *** may improve the insulin resistance associated with type 2diabetes.

关键词： yy20 peroxisome proliferator-activated receptor y insulin sensitivity glucose consumption

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