title: Synthesis and evaluation of 5-benzylidenethiazolidine-2,4-dione derivatives for the treatment of non-alcoholic fatty liver disease.
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.
authors.affiliation: State Key Laboratory of Biotherapy, West China Hospital, West China Medical School, Sichuan University, Chengdu 610041, China.
authors.forename: Liang
authors.initials: L
authors.lastname: Ma
authors.forename: Jinying
authors.initials: J
authors.lastname: Chen
authors.forename: Xiaolin
authors.initials: X
authors.lastname: Liang
authors.forename: Caifei
authors.initials: C
authors.lastname: Xie
authors.forename: Chongyang
authors.initials: C
authors.lastname: Deng
authors.forename: Li
authors.initials: L
authors.lastname: Huang
authors.forename: Aihua
authors.initials: A
authors.lastname: Peng
authors.forename: Yuanquan
authors.initials: Y
authors.lastname: Wei
authors.forename: Lijuan
authors.initials: L
authors.lastname: Chen
mesh_terms: D041721:3T3-L1 Cells; D017667:Adipocytes / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D050156:Adipogenesis / Q000187:drug effects; D052242:Adiponectin / Q000096:biosynthesis; D000284:Administration, Oral; D000818:Animals; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D015415:Biomarkers / Q000097:blood; D002454:Cell Differentiation / Q000187:drug effects; D015195:Drug Design; D005234:Fatty Liver / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D005947:Glucose / Q000378:metabolism; D056945:Hep G2 Cells; D006801:Humans; D020738:Leptin / Q000096:biosynthesis; D008297:Male; D051379:Mice; D015394:Molecular Structure; D065626:Non-alcoholic Fatty Liver Disease; D009929:Organ Size / Q000187:drug effects; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
chemical_list: D052242:Adiponectin; C499919:Adipoq protein, mouse; D001597:Benzylidene Compounds; D015415:Biomarkers; D020738:Leptin; D045162:Thiazolidinediones; D005947:Glucose