A role for central nervous system PPAR-γ in the regulation of energy balance

Nat Med. 2011 May;17(5):623-6. doi: 10.1038/nm.2349. Epub 2011 May 1.

Abstract

The peroxisome proliferator-activated receptor-γ (PPAR-γ) is a nuclear receptor that is activated by lipids to induce the expression of genes involved in lipid and glucose metabolism, thereby converting nutritional signals into metabolic consequences. PPAR-γ is the target of the thiazolidinedione (TZD) class of insulin-sensitizing drugs, which have been widely prescribed to treat type 2 diabetes mellitus. A common side effect of treatment with TZDs is weight gain. Here we report a previously unknown role for central nervous system (CNS) PPAR-γ in the regulation of energy balance. We found that both acute and chronic activation of CNS PPAR-γ, by either TZDs or hypothalamic overexpression of a fusion protein consisting of PPAR-γ and the viral transcriptional activator VP16 (VP16-PPAR-γ), led to positive energy balance in rats. Blocking the endogenous activation of CNS PPAR-γ with pharmacological antagonists or reducing its expression with shRNA led to negative energy balance, restored leptin sensitivity in high-fat-diet (HFD)-fed rats and blocked the hyperphagic response to oral TZD treatment. These findings have implications for the widespread clinical use of TZD drugs and for understanding the etiology of diet-induced obesity.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Blood-Brain Barrier
  • Central Nervous System / drug effects
  • Central Nervous System / physiology*
  • Energy Metabolism / physiology*
  • Gene Expression
  • Humans
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / pharmacology
  • Hypothalamus / drug effects
  • Hypothalamus / physiology
  • Male
  • PPAR gamma / agonists
  • PPAR gamma / antagonists & inhibitors
  • PPAR gamma / genetics
  • PPAR gamma / physiology*
  • RNA, Small Interfering / genetics
  • Rats
  • Rats, Long-Evans
  • Recombinant Fusion Proteins / genetics
  • Rosiglitazone
  • Thiazolidinediones / adverse effects
  • Thiazolidinediones / pharmacology
  • Weight Gain / drug effects
  • Weight Gain / physiology

Substances

  • Hypoglycemic Agents
  • PPAR gamma
  • RNA, Small Interfering
  • Recombinant Fusion Proteins
  • Thiazolidinediones
  • Rosiglitazone