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New PPARγ partial agonist improves obesity-induced metabolic alterations and atherosclerosis in LDLr−/− mice

AutorSilva, Jacqueline C.; César, Fernanda A.; Heras, Beatriz de las; Boscá, Lisardo ; Rudnicki, Martina; Abdalla, Dulcineia S. P.
Palabras claveObesity
PPARγ
Thiazolidinediones
Atherosclerosis
Diabetes
Fecha de publicación2016
EditorElsevier
CitaciónPharmacological Research 104: 49-60 (2016)
ResumenPeroxisome proliferator-activated receptor gamma (PPARγ) regulates multiple pathways involved in the pathogenesis of obesity and atherosclerosis. Here, we evaluated the therapeutic potential of GQ-177, a new thiazolidinedione, on diet-induced obesity and atherosclerosis. The intermolecular interaction between PPARγ and GQ-177 was examined by virtual docking and PPAR activation was determined by reporter gene assay identifying GQ-177 as a partial and selective PPARγ agonist. For the evaluation of biological activity of GQ-177, low-density lipoprotein receptor-deficient (LDLr) C57/BL6 mice were fed either a high fat diabetogenic diet (diet-induced obesity), or a high fat atherogenic diet, and treated with vehicle, GQ-177 (20 mg/kg/day), pioglitazone (20 mg/kg/day, diet-induced obesity model) or rosiglitazone (15 mg/kg/day, atherosclerosis model) for 28 days. In diet-induced obesity mice, GQ-177 improved insulin sensitivity and lipid profile, increased plasma adiponectin and GLUT4 mRNA in adipose tissue, without affecting body weight, food consumption, fat accumulation and bone density. Moreover, GQ-177 enhanced hepatic mRNA levels of proteins involved in lipid metabolism. In the atherosclerosis mice, GQ-177 inhibited atherosclerotic lesion progression, increased plasma HDL and mRNA levels of PPARγ and ATP-binding cassette A1 in atherosclerotic lesions. GQ-177 acts as a partial PPARγ agonist that improves obesity-associated insulin resistance and dyslipidemia with atheroprotective effects in LDLr mice.
URIhttp://hdl.handle.net/10261/150975
DOI10.1016/j.phrs.2015.12.010
Identificadoresdoi: 10.1016/j.phrs.2015.12.010
e-issn: 1096-1186
issn: 1043-6618
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