Abstract
The hepatoprotective effects of chalcone derivatives were evaluated in D-galactosamine/ lipopolysaccharide (D-GalN/LPS)-induced fulminant hepatic failure in mouse. Thirteen chalcone derivatives were synthesized for study and their hepatoprotective effects were evaluated by assessing aspartate aminotransferase (AST) and alanine aminotransferase (ALT) levels in serum. Chalcone preparations were injected into mice at 12 h and 1 h before intraperitoneal injection of D-GalN/LPS. After abdominal administration, changes in AST and ALT between the control and treated groups were observed. Ten of the synthesized chalcone derivatives exhibited inhibitory effects on D-GalN/LPS-induced levels of AST and ALT in mice. Compounds2, 3, 8, 9, and12 markedly reduced serum AST and ALT at 8 h, inhibited hepatocyte necrosis and showed significant hepatoprotective activities. The activity of compound3 was compared with the bifendate (DDB) through oral administration. Compound3 showed much higher inhibitory effects than bifendate for decreasing AST and ALT activity. The results indicate that compound3 has strong hepatoprotective activity through suppression of tumor necrosis factoralpha (TNF-alpha) preduction, reduction of the histological change in the liver, and attenuated of hepatocyte apoptosis confirmed by DNA fragmentation assay.
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Guan, LP., Nan, JX., Jin, XJ. et al. Protective effects of chalcone derivatives for acute liver injury in mice. Arch Pharm Res 28, 81–86 (2005). https://doi.org/10.1007/BF02975140
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DOI: https://doi.org/10.1007/BF02975140