Endothelin-1 activates p38 mitogen-activated protein kinase via endothelin-A receptor in rat myocardial cells

Mol Cell Biochem. 1999 Sep;199(1-2):119-24. doi: 10.1023/a:1006918901356.

Abstract

In myocardial cells (MCs), endothelin-1 (ET-1) exerts various effects such as hypertrophy, and causes cellular injury. Long-term treatment with an endothelin-A (ET(A)) receptor antagonist improves the survival of rats with heart failure, suggesting that myocardial endothelin system contributes to the progression of heart failure. p38 mitogen-activated kinase (MAPK) is a member of the MAPK family and activated by several forms of environmental stresses. We show here the effect of ET-1 on p38 MAPK activation and the role of ET-1-activated p38 MAPK on morphological changes in MCs. ET-1-stimulated p38 MAPK phosphorylation was detectable within 2 min and maximal at 5 min and was concentration dependent. The maximum effect was obtained at 10 nM. An ET(A) receptor antagonist, BQ-123, but not an endothelin-B receptor antagonist, BQ-788, inhibited these reactions. A p38 MAPK inhibitor, SB203580, failed to inhibit the morphological changes associated with ET-1-induced myocardial cell hypertrophy. These results indicate that p38 MAPK is activated by ET-1 but does not contribute to the development of ET-1-induced myocardial cell hypertrophy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Cardiomegaly / metabolism
  • Cells, Cultured
  • Dose-Response Relationship, Drug
  • Endothelin-1 / metabolism*
  • Endothelin-1 / pharmacology
  • Enzyme Activation
  • Enzyme Inhibitors / pharmacology
  • Imidazoles / pharmacology
  • Leucine / metabolism
  • Mitogen-Activated Protein Kinases / antagonists & inhibitors
  • Mitogen-Activated Protein Kinases / drug effects
  • Mitogen-Activated Protein Kinases / metabolism*
  • Myocardium / cytology
  • Myocardium / metabolism*
  • Oligopeptides / pharmacology
  • Peptides, Cyclic / pharmacology
  • Phosphorylation
  • Piperidines / pharmacology
  • Pyridines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Endothelin A
  • Receptors, Endothelin / metabolism*
  • Sarcomeres / drug effects
  • p38 Mitogen-Activated Protein Kinases

Substances

  • Endothelin-1
  • Enzyme Inhibitors
  • Imidazoles
  • Oligopeptides
  • Peptides, Cyclic
  • Piperidines
  • Pyridines
  • Receptor, Endothelin A
  • Receptors, Endothelin
  • BQ 788
  • Mitogen-Activated Protein Kinases
  • p38 Mitogen-Activated Protein Kinases
  • Leucine
  • SB 203580
  • cyclo(Trp-Asp-Pro-Val-Leu)