Neuroprotective effects of KR-62980, a new PPARγ agonist, against chemical ischemia-reperfusion in SK-N-SH cells

Brain Res. 2011 Feb 4:1372:103-14. doi: 10.1016/j.brainres.2010.11.062. Epub 2010 Nov 25.

Abstract

PPARγ agonists exert neuroprotective effects against various types of brain injuries. In the present study, we investigated the effects of KR-62980, a new PPARγ agonist, and rosiglitazone on the neuronal cell death induced by chemical ischemia-reperfusion in SK-N-SH cells and their underlying molecular mechanisms. Both agonists inhibited chemical ischemia-reperfusion-induced cell death, and the effects were associated with anti-apoptotic action. KR-62980 and rosiglitazone suppressed NO and ROS formation, and N-acetyl-N-acetoxy-4-chlorobenzenesulfonamide, an NO generator, reversed the protective effects of the agonists on cell viability. In the agonist-induced anti-apoptotic process, PTEN expression was suppressed in parallel with increased Akt and ERK phosphorylation, whereas PD98059 (an ERK inhibitor) or wortmannin (a PI-3K inhibitor) abolished the cell survival by KR-62980 and rosiglitazone. All of the effects of KR-62980 and rosiglitazone appeared to be PPARγ-dependent because the effects were reversed by bisphenol A diglycidyl ether, a PPARγ antagonist, or by PPARγ knockdown. Our results demonstrate that two PPARγ agonists, KR-62980 and rosiglitazone, inhibited chemical ischemia-reperfusion-induced neuronal cell death by PPARγ-mediated anti-apoptotic and anti-oxidant mechanisms related to PTEN suppression and ERK phosphorylation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Death / drug effects
  • Cell Line, Tumor
  • Dose-Response Relationship, Drug
  • Drug Interactions
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Indenes / pharmacology*
  • Morpholines / pharmacology*
  • Neuroblastoma / pathology
  • Neuroprotective Agents / pharmacology*
  • Nitric Oxide / metabolism
  • Nitric Oxide Synthase Type II / metabolism
  • Organic Chemicals / pharmacology
  • PPAR gamma / agonists*
  • Phosphorylation / drug effects
  • Reactive Oxygen Species / metabolism
  • Rosiglitazone
  • Signal Transduction / drug effects
  • Sodium Azide / pharmacology
  • Thiazolidinediones / pharmacology
  • Time Factors

Substances

  • 1-(methylimino-N-oxy)-6-(2-morpholinoethoxy)-3-phenyl-1H-indene-2-carboxylic acid ethyl ester
  • Enzyme Inhibitors
  • Indenes
  • Morpholines
  • Neuroprotective Agents
  • Organic Chemicals
  • PD 98058
  • PPAR gamma
  • Reactive Oxygen Species
  • Thiazolidinediones
  • Rosiglitazone
  • Nitric Oxide
  • Sodium Azide
  • Nitric Oxide Synthase Type II