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Arch Pharm (Weinheim) ; 345(7): 517-24, 2012 Jul.
Article in English | MEDLINE | ID: mdl-22532295

ABSTRACT

Twenty-two 5-benzylidenethiazolidine-2,4-dione derivatives (TZDs) were synthesized and evaluated for their potency on adipogenesis of 3T3-L1 adipocytes by measuring the expression of adiponectin protein. Among them, compared to rosiglitazone, 3V was found to upregulate the adiponectin protein expression and downregulate the secretion of leptin protein in 3T3-L1 adipocytes at a respective concentration of 10 µM. With respect to high-fat/high-calorie (HF/HC) diet-induced non-alcoholic fatty liver disease (NAFLD) in Wistar rats, oral administration of 3V could reduce liver weight, visceral fat, and improve serum levels of biochemical markers. H&E staining of liver sections validated 3V as a potent hepatoprotective agent for reducing fat deposition against NAFLD.


Subject(s)
Benzylidene Compounds/chemical synthesis , Fatty Liver/drug therapy , Thiazolidinediones/chemical synthesis , 3T3-L1 Cells , Adipocytes/cytology , Adipocytes/drug effects , Adipocytes/metabolism , Adipogenesis/drug effects , Adiponectin/biosynthesis , Administration, Oral , Animals , Benzylidene Compounds/chemistry , Benzylidene Compounds/therapeutic use , Biomarkers/blood , Cell Differentiation/drug effects , Drug Design , Fatty Liver/metabolism , Fatty Liver/pathology , Glucose/metabolism , Hep G2 Cells , Humans , Leptin/biosynthesis , Male , Mice , Molecular Structure , Non-alcoholic Fatty Liver Disease , Organ Size/drug effects , Rats , Rats, Wistar , Structure-Activity Relationship , Thiazolidinediones/chemistry , Thiazolidinediones/therapeutic use
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