Evidence for protein kinase C-mediated activation of Rho-kinase in a porcine model of coronary artery spasm

Arterioscler Thromb Vasc Biol. 2003 Dec;23(12):2209-14. doi: 10.1161/01.ATV.0000104010.87348.26. Epub 2003 Oct 30.

Abstract

Objective: We have recently demonstrated that protein kinase C (PKC) and Rho-kinase play important roles in coronary vasospasm in a porcine model. However, it remains to be examined whether there is an interaction between the two molecules to cause the spasm.

Methods and results: A segment of left porcine coronary artery was chronically treated with IL-1beta-bound microbeads in vivo. Two weeks after the operation, phorbol ester caused coronary spasm in vivo and coronary hypercontractions in vitro at the IL-1beta-treated segment; both were significantly inhibited by hydroxyfasudil, a specific Rho-kinase inhibitor. Guanosine 5'-[gamma-thio]triphosphate (GTPgammaS), which activates Rho with a resultant activation of Rho-kinase, enhanced Ca2+ sensitization of permeabilized vascular smooth muscle cells, which were resistant to the blockade of PKC by calphostin C. The GTPgammaS-induced Ca2+ sensitization was greater in the spastic segment than in the control segment. Western blot analysis revealed that only PKCdelta isoform was activated during the hypercontraction.

Conclusions: These results demonstrate that PKC and Rho-kinase coexist on the same intracellular signaling pathway, with PKC located upstream on Rho-kinase, and that among the PKC isoforms, only PKCdelta may be involved. Thus, the strategy to inhibit Rho-kinase rather than PKC may be a more specific and useful treatment for coronary spasm.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / analogs & derivatives*
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / pharmacology
  • Animals
  • Blotting, Western
  • Calcium / metabolism
  • Capillary Permeability / drug effects
  • Coronary Vasospasm / enzymology*
  • Coronary Vasospasm / metabolism
  • Coronary Vessels / chemistry
  • Coronary Vessels / drug effects
  • Coronary Vessels / enzymology
  • Coronary Vessels / metabolism
  • Disease Models, Animal*
  • Enzyme Activation
  • Enzyme Inhibitors / pharmacology
  • Guanosine 5'-O-(3-Thiotriphosphate) / pharmacology
  • In Vitro Techniques
  • Intracellular Signaling Peptides and Proteins
  • Male
  • Monomeric GTP-Binding Proteins / metabolism
  • Monomeric GTP-Binding Proteins / physiology
  • Muscle Contraction / drug effects
  • Muscle Contraction / physiology
  • Muscle, Smooth, Vascular / chemistry
  • Muscle, Smooth, Vascular / cytology
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / enzymology
  • Phorbol 12,13-Dibutyrate / metabolism
  • Phorbol 12,13-Dibutyrate / pharmacology
  • Protein Kinase C / physiology*
  • Protein Serine-Threonine Kinases / antagonists & inhibitors
  • Protein Serine-Threonine Kinases / metabolism*
  • Protein Transport / drug effects
  • Protein Transport / physiology
  • Swine
  • rho-Associated Kinases

Substances

  • Enzyme Inhibitors
  • Intracellular Signaling Peptides and Proteins
  • hydroxyfasudil
  • Phorbol 12,13-Dibutyrate
  • Guanosine 5'-O-(3-Thiotriphosphate)
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • Protein Serine-Threonine Kinases
  • rho-Associated Kinases
  • Protein Kinase C
  • Monomeric GTP-Binding Proteins
  • Calcium