Cholesterol-lowering drugs cause dissolution of cholesterol crystals and disperse Kupffer cell crown-like structures during resolution of NASH

J Lipid Res. 2015 Feb;56(2):277-85. doi: 10.1194/jlr.M053785. Epub 2014 Dec 17.

Abstract

Cholesterol crystals form within hepatocyte lipid droplets in human and experimental nonalcoholic steatohepatitis (NASH) and are the focus of crown-like structures (CLSs) of activated Kupffer cells (KCs). Obese, diabetic Alms1 mutant (foz/foz) mice were a fed high-fat (23%) diet containing 0.2% cholesterol for 16 weeks and then assigned to four intervention groups for 8 weeks: a) vehicle control, b) ezetimibe (5 mg/kg/day), c) atorvastatin (20 mg/kg/day), or d) ezetimibe and atorvastatin. Livers of vehicle-treated mice developed fibrosing NASH with abundant cholesterol crystallization within lipid droplets calculated to extend over 3.3% (SD, 2.2%) of liver surface area. Hepatocyte lipid droplets with prominent cholesterol crystallization were surrounded by TNFα-positive (activated) KCs forming CLSs (≥ 3 per high-power field). KCs that formed CLSs stained positive for NLRP3, implicating activation of the NLRP3 inflammasome in response to cholesterol crystals. In contrast, foz/foz mice treated with ezetimibe and atorvastatin showed near-complete resolution of cholesterol crystals [0.01% (SD, 0.02%) of surface area] and CLSs (0 per high-power field), with amelioration of fibrotic NASH. Ezetimibe or atorvastatin alone had intermediate effects on cholesterol crystallization, CLSs, and NASH. These findings are consistent with a causative link between exposure of hepatocytes and KCs to cholesterol crystals and with the development of NASH possibly mediated by NLRP3 activation.

Keywords: caspase 1; crown-like structure; lipotoxicity; nonalcoholic steatohepatitis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticholesteremic Agents / pharmacology
  • Anticholesteremic Agents / therapeutic use*
  • Atorvastatin
  • Azetidines / pharmacology
  • Azetidines / therapeutic use
  • Cholesterol / metabolism*
  • Ezetimibe
  • Female
  • Heptanoic Acids / pharmacology
  • Heptanoic Acids / therapeutic use
  • Inflammasomes / drug effects
  • Inflammasomes / metabolism
  • Kupffer Cells / drug effects*
  • Kupffer Cells / metabolism*
  • Liver / drug effects
  • Liver / metabolism
  • Mice
  • Mice, Mutant Strains
  • Non-alcoholic Fatty Liver Disease / drug therapy
  • Pyrroles / pharmacology
  • Pyrroles / therapeutic use

Substances

  • Anticholesteremic Agents
  • Azetidines
  • Heptanoic Acids
  • Inflammasomes
  • Pyrroles
  • Cholesterol
  • Atorvastatin
  • Ezetimibe