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

  
@article{APS4373,
	author = {Hao-shu Wu and Juan-hong Yu and Ying-yin Li and Yu-she Yang and Qiao-jun He and Yi-jia Lou and Ru-yun Ji},
	title = {Insulin-sensitizing effects of a novel α-methyl-α-phenoxylpropionate derivative in vitro},
	journal = {Acta Pharmacologica Sinica},
	volume = {28},
	number = {3},
	year = {2016},
	keywords = {},
	abstract = {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 PPARγ2, 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.},
	issn = {1745-7254},	url = {http://www.chinaphar.com/article/view/4373}
}