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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.

A series of 5‐benzylidenethiazolidine‐2,4‐dione derivatives were synthesized and evaluated by measuring the expression of adiponectin protein in 3T3‐L1 adipocytes. Oral administration of 3V at a dosage of 25 mg/kg effectively improved the serum levels of biochemical markers in the HF/HC‐induced NAFLD rat model. 3V was identified as a potent hepatoprotective agent against NAFLD by reducing fat deposition.

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Authors:   Ma, Liang; Chen, Jinying; Liang, Xiaolin; Xie, Caifei; Deng, Chongyang; Huang, Li; Peng, Aihua; Wei, Yuanquan; Chen, Lijuan
Journal:   Archiv der Pharmazie
Year:   2012
Pages:   n/a
DOI:   10.1002/ardp.201100413
Publication date:   25-Apr-2012
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