Olmesartan ameliorates a dietary rat model of non-alcoholic steatohepatitis through its pleiotropic effects

Eur J Pharmacol. 2008 Jul 7;588(2-3):316-24. doi: 10.1016/j.ejphar.2008.04.028. Epub 2008 Apr 16.

Abstract

Insulin resistance is a major pathological condition associated with obesity and metabolic syndrome. Insulin resistance and the renin-angiotensin system are intimately linked. We evaluated the role of the renin-angiotensin system in the pathogenesis of insulin resistance-associated, non-alcoholic steatohepatitis by using the angiotensin II type 1 receptor blocker olmesartan medoxomil in a diabetic rat model. The effects of olmesartan on methionine- and choline-deficient (MCD) diet-induced steatohepatitis were investigated in obese, diabetic Otsuka Long-Evans Tokushima Fatty (OLETF) rats and control Long-Evans Tokushima Otsuka (LETO) rats. Components of the renin-angiotensin system were up-regulated in the livers of OLETF rats, compared with LETO rats. In OLETF, but not LETO, rats, oral administration of olmesartan for 8 weeks ameliorated insulin resistance. Moreover, olmesartan suppressed MCD diet-induced hepatic steatosis and the hepatic expression of lipogenic genes (sterol regulatory element-binding protein-1c and fatty acid synthase) in OLETF, but not LETO, rats. In both OLETF and LETO rats, olmesartan inhibited hepatic oxidative stress (4-hydroxy-2-nonenal-modified protein) and expression of NADPH oxidase. Olmesartan also inhibited hepatic fibrosis, stellate cell activation, and expression of fibrogenic genes (transforming growth factor-beta, alpha 1 [I] procollagen, plasminogen activator inhibitor-1) in both OLETF and LETO rats. In conclusion, pharmacological blockade of the angiotensin II type 1 receptor slows the development of steatohepatitis in the OLETF rat model. This angiotensin II type 1 receptor blocker may exert insulin resistance-associated effects against hepatic steatosis and inflammation as well as direct effects against the generation of reactive oxygen species and fibrogenesis.

MeSH terms

  • Angiotensin II Type 1 Receptor Blockers / therapeutic use*
  • Animals
  • Choline Deficiency / complications
  • Disease Models, Animal
  • Fatty Acids / biosynthesis
  • Fatty Liver / drug therapy*
  • Imidazoles / pharmacology
  • Imidazoles / therapeutic use*
  • Insulin Resistance
  • Liver Cirrhosis, Experimental / prevention & control
  • Male
  • Methionine / deficiency
  • Oxidative Stress
  • RNA, Messenger / analysis
  • Rats
  • Rats, Long-Evans
  • Sterol Regulatory Element Binding Protein 1 / genetics
  • Tetrazoles / pharmacology
  • Tetrazoles / therapeutic use*
  • Transforming Growth Factor beta / genetics
  • Tumor Necrosis Factor-alpha / blood

Substances

  • Angiotensin II Type 1 Receptor Blockers
  • Fatty Acids
  • Imidazoles
  • RNA, Messenger
  • Srebf1 protein, rat
  • Sterol Regulatory Element Binding Protein 1
  • Tetrazoles
  • Transforming Growth Factor beta
  • Tumor Necrosis Factor-alpha
  • olmesartan
  • Methionine