title: Insulin-sensitizing effects of a novel alpha-methyl- alpha -phenoxylpropionate derivative in vitro.
abstract: OBJECTIVE
  To examine the insulin sensitizing effects of a novel alpha-methyl-alpha- phenoxylpropionate derivative YY20 in insulin-sensitive cell lines.
  
  
  METHODS
  The peroxisome proliferator-activated receptor gamma (PPAR gamma) 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 PPAR gamma 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 PPAR gamma 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Department of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
authors.forename: Hao-Shu
authors.initials: HS
authors.lastname: Wu
authors.forename: Juan-Hong
authors.initials: JH
authors.lastname: Yu
authors.forename: Ying-Yin
authors.initials: YY
authors.lastname: Li
authors.forename: Yu-She
authors.initials: YS
authors.lastname: Yang
authors.forename: Qiao-Jun
authors.initials: QJ
authors.lastname: He
authors.forename: Yi-Jia
authors.initials: YJ
authors.lastname: Lou
authors.forename: Ru-Yun
authors.initials: RY
authors.lastname: Ji
mesh_terms: D016475:3T3 Cells; D017667:Adipocytes / Q000187:drug effects; D052242:Adiponectin / Q000096:biosynthesis / Q000235:genetics; D000818:Animals; D045744:Cell Line, Tumor; D005947:Glucose / Q000378:metabolism; D051275:Glucose Transporter Type 4 / Q000096:biosynthesis / Q000235:genetics; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology*; D007328:Insulin / Q000494:pharmacology*; D055504:Insulin Receptor Substrate Proteins / Q000096:biosynthesis / Q000235:genetics; D007333:Insulin Resistance / Q000502:physiology*; D051379:Mice; D047495:PPAR gamma / Q000037:antagonists & inhibitors / Q000096:biosynthesis / Q000235:genetics; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D052242:Adiponectin; D051275:Glucose Transporter Type 4; D007004:Hypoglycemic Agents; C526292:IRS1 protein, human; D007328:Insulin; D055504:Insulin Receptor Substrate Proteins; D047495:PPAR gamma; D010666:Phenylpropionates; D005947:Glucose