Additive action of 11beta-HSD1 inhibition and PPAR-gamma agonism on hepatic steatosis and triglyceridemia in diet-induced obese rats

Int J Obes (Lond). 2009 May;33(5):601-4. doi: 10.1038/ijo.2009.33. Epub 2009 Feb 17.

Abstract

Both 11beta-hydroxysteroid dehydrogenase (11beta-HSD1) inhibition and peroxisome proliferator-activated receptor-gamma (PPAR-gamma) agonism reduce liver and plasma lipids in rodents through partly distinct mechanisms. This study aimed to assess their additivity of action on liver and plasma lipids in a model of diet-induced steatosis. Rats were fed an obesogenic diet and were treated either with an 11beta-HSD1 inhibitor (Compound A, 3 mg kg(-1) day(-1)) or rosiglitazone (RSG, 5 mg kg(-1) day(-1)) or both for 6 weeks. Compound A and RSG reduced liver steatosis and triglyceridemia, and did so additively when given in combination. The 11beta-HSD1 inhibitor had no effect on serum adiponectin, but increased liver adiponectin receptor type 2 (Adipo-R2) mRNA levels. Conversely, RSG increased serum adiponectin, a likely mediator of its antisteatotic action, but had no effect per se on the Adipo-R2 expression. mRNA levels of representative genes of fatty acid oxidation tended to be increased by both compounds. The study shows that combined 11beta-HSD1 inhibition and PPAR-gamma agonism additively reduce liver steatosis and triglyceridemia, which may eventually prove therapeutically useful.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
  • Adiponectin / blood
  • Animals
  • Disease Models, Animal
  • Fatty Liver / metabolism*
  • Fatty Liver / prevention & control
  • Male
  • Obesity / metabolism
  • PPAR gamma / agonists*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Adiponectin / blood
  • Rosiglitazone
  • Thiazolidinediones / pharmacology
  • Triazoles / pharmacology
  • Triglycerides / metabolism*

Substances

  • Adiponectin
  • PPAR gamma
  • Receptors, Adiponectin
  • Thiazolidinediones
  • Triazoles
  • Triglycerides
  • compound A (octyltriazole)
  • Rosiglitazone
  • 11-beta-Hydroxysteroid Dehydrogenase Type 1