Protective mechanisms of acacetin against D-galactosamine and lipopolysaccharide-induced fulminant hepatic failure in mice

J Nat Prod. 2014 Nov 26;77(11):2497-503. doi: 10.1021/np500537x. Epub 2014 Nov 10.

Abstract

This study examined the hepatoprotective effects of acacetin (1), a flavonoid isolated from Agastache rugosa, against d-galactosamine (GalN) and lipopolysaccharide (LPS)-induced fulminant hepatic failure. Mice were given an intraperitoneal injection of 1 (25, 50, and 100 mg/kg), or the vehicle alone (5% dimethyl sulfoxide-saline), 1 h before GalN (800 mg/kg)/LPS (40 μg/kg) treatment and sacrificed at 6 h after GalN/LPS injection. GalN/LPS markedly increased mortality and serum aminotransferase activity, and these increases were attenuated by 1. GalN/LPS increased serum tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6) levels, while 1 attenuated TNF-α levels and further increased IL-6 levels. GalN/LPS increased protein expression of toll-like receptor 4, phosphorylation of extracellular signal-related kinase, and p38 and c-Jun N-terminal kinase and increased nuclear protein expression of nuclear factor κB; these increases were attenuated by 1. GalN/LPS increased Atg5 and Atg7 protein expressions, and these increases were augmented by 1. GalN/LPS activated autophagic flux as indicated by decreased microtubule-associated protein 1 light chain 3-II and sequestosome1/p62 protein expression. This activation was enhanced by 1. These findings suggest that 1 protects against GalN/LPS-induced liver injury by suppressing TLR4 signaling and enhancing autophagic flux.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Flavones / pharmacology*
  • Galactosamine / pharmacology*
  • Interleukin-6 / blood
  • Interleukin-6 / metabolism
  • JNK Mitogen-Activated Protein Kinases / metabolism
  • Lipopolysaccharides / pharmacology*
  • Liver / drug effects
  • Liver Failure, Acute / chemically induced*
  • Male
  • Mice
  • Molecular Structure
  • NF-kappa B / metabolism
  • Phosphorylation / drug effects
  • Plant Components, Aerial / chemistry
  • Republic of Korea
  • Signal Transduction / drug effects
  • Toll-Like Receptor 4 / drug effects
  • Tumor Necrosis Factor-alpha / blood
  • Tumor Necrosis Factor-alpha / drug effects

Substances

  • Flavones
  • Interleukin-6
  • Lipopolysaccharides
  • NF-kappa B
  • Toll-Like Receptor 4
  • Tumor Necrosis Factor-alpha
  • Galactosamine
  • JNK Mitogen-Activated Protein Kinases
  • acacetin