Anti-diabetic effect of amorphastilbol through PPARα/γ dual activation in db/db mice

Biochem Biophys Res Commun. 2013 Mar 1;432(1):73-9. doi: 10.1016/j.bbrc.2013.01.083. Epub 2013 Jan 29.

Abstract

Peroxisome proliferator-activated receptors (PPARs) have been considered as desirable targets for metabolic syndrome treatments, even though their specific agonists have several side effects, including body weight gain, edema, and tissue failure. The effects of amorphastilbol (APH) on glucose- and lipid metabolism were investigated with in vitro 3T3-L1 adipocyte systems and in vivo db/db mice model. APH selectively stimulates the transcriptional activities of both PPARα and PPARγ, which are able to enhance fatty acid oxidation and glucose utilization. Furthermore, APH improves glucose and lipid impairment in db/db mice. More importantly, there are no significant side effects, such as weight gain or hepatomegaly, in APH-treated animals, implying that APH do not adversely affect liver or lipid metabolism. All our data suggest that APH can be used as potential therapeutic agents against type 2 diabetes and related metabolic disorders, including obesity, by enhancing glucose and lipid metabolism.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3-L1 Cells
  • Adipocytes / drug effects
  • Adipocytes / metabolism
  • Adipogenesis / drug effects
  • Adipogenesis / genetics
  • Adipose Tissue, White / drug effects
  • Adipose Tissue, White / metabolism
  • Animals
  • Blood Glucose / drug effects
  • Cannabinoids / administration & dosage*
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Fatty Acids / metabolism
  • Gene Expression Regulation / drug effects
  • Hypoglycemic Agents / administration & dosage*
  • Liver / drug effects
  • Liver / metabolism
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Oxidation-Reduction
  • PPAR alpha / agonists*
  • PPAR gamma / agonists*

Substances

  • Blood Glucose
  • Cannabinoids
  • Fatty Acids
  • Hypoglycemic Agents
  • PPAR alpha
  • PPAR gamma
  • amorphastilbol