%0 Journal Article %T Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro %A Wu Hao-shu %A Yu Juan-hong %A Li Ying-yin %A Yang Yu-she %A He Qiao-jun %A Lou Yi-jia %A Ji Ru-yun %J Acta Pharmacologica Sinica %D 2016 %B 2016 %9 %! Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro %K %X 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 receptor γ (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 expression of PPARγ 2 , as well as the protein expression of insulin receptor substrate-1 (IRS-1), glucose transporter-4 (GLUT4), and adiponectin (ACRP30). The effects on GLUT4 and ACRP30 could be reversed by the PPARγ inhibitor 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 insulindependent manner. It may improve the insulin resistance associated with type 2 diabetes. %U http://www.chinaphar.com/article/view/4373 %V 28 %N 3 %P 417–422 %@ 1745-7254