KR-31378 protects cardiac H9c2 cells from chemical hypoxia-induced cell death via inhibition of JNK/p38 MAPK activation

Jpn J Physiol. 2004 Dec;54(6):575-83. doi: 10.2170/jjphysiol.54.575.

Abstract

Using a metabolic inhibition buffer as an ischemic model, we show here that KR-31378, a cardioselective ATP-sensitive potassium channel opener, protects H9c2 cells from chemical hypoxia (CH)-induced cell death. Our previous study showed that CH downregulated caspase activities, but led to differential activation of mitogen-activated protein kinases (MAPKs) in H9c2 cells. The repression of CH-induced c-jun N-terminal kinase (JNK)/p38 MAPK activation resulted in partial protection against CH- induced cell death, implying JNK/p38 MAPK's causative role in CH-induced cell death. This study furthers that research and examines if KR-31378's protective effect came from modulating MAPK activity and/or caspase activity in H9c2 cells. Although KR-31378 did not restore downregulated caspase-3 activity, it did block the activation of JNK and p38 MAPK in a dose-dependent manner. Extracellular signal-regulated kinase activity was not recovered by KR-31378 treatment. CH-induced reactive oxygen species (ROS) generation was suppressed by KR-31378. Thus our results indicate that the cardioprotective effect of KR-31378 in CH is due, at least in part, to the differential inhibition of MAPKs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anthracenes / pharmacology
  • Butadienes / pharmacology
  • Cell Death / drug effects*
  • Cell Death / physiology
  • Cell Hypoxia / physiology*
  • Cell Line
  • Enzyme Activation / drug effects
  • Guanidines / chemistry
  • Guanidines / pharmacology*
  • Imidazoles / pharmacology
  • JNK Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • MAP Kinase Kinase 4
  • Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors*
  • Molecular Structure
  • Myocardium / cytology*
  • Nitriles / pharmacology
  • Pyrans / chemistry
  • Pyrans / pharmacology*
  • Pyridines / pharmacology
  • Reactive Oxygen Species
  • p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*

Substances

  • Anthracenes
  • Butadienes
  • Guanidines
  • Imidazoles
  • N''-cyano-N-(6-amino-3,4-dihydro-3-hydroxy-2-methyl-2-dimethoxymethyl-2H-benzopyran-4-yl)-N'-benzylguanidine
  • Nitriles
  • Pyrans
  • Pyridines
  • Reactive Oxygen Species
  • U 0126
  • pyrazolanthrone
  • JNK Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases
  • MAP Kinase Kinase 4
  • Mitogen-Activated Protein Kinase Kinases
  • SB 203580