Stable EET urea agonist and soluble epoxide hydrolase inhibitor regulate rat pulmonary arteries through TRPCs

Hypertens Res. 2011 May;34(5):630-9. doi: 10.1038/hr.2011.5. Epub 2011 Feb 10.

Abstract

Epoxyeicosatrienoic acids (EETs), cytochrome P450-derived metabolites of arachidonic acid, have been reported to increase intracellular calcium concentration in aortic vascular smooth muscle cells (SMCs). As EETs are labile, we synthesized a new stable urea EET analog with agonist and soluble epoxide hydrolase (sEH) inhibitor properties. We refer to this analog, 12-(3-hexylureido)dodec-8-enoic acid, as 8-HUDE. Measuring tension of vascular rings, intracellular calcium signaling by confocal laser scanning microscopy and gene expression by reverse-transcription-PCR and western blots, we examined the effects of 8-HUDE on pulmonary vascular tone and calcium signaling in rat pulmonary artery (PA) SMCs (PASMCs). 8-HUDE increased the tension of rat PAs to 145% baseline, whereas it had no effect on the tension of mesenteric arteries (MAs). The 8-HUDE-induced increase in vascular tone was abolished by removal of extracellular Ca(2+) or by pretreatment with either La(3+) or SKF96365, which are inhibitors of canonical transient receptor potential channels (TRPCs). Furthermore, 8-HUDE-evoked increases in [Ca(2+)](i) in PASMCs could be blunted by inhibition of TRPC with SKF96365, removal of extracellular calcium or depletion of intracellular calcium stores with caffeine, cyclopiazonic acid or 2-aminoethoxydiphenyl borate, but not by the voltage-activated calcium channel blocker nifedipine. In addition to immediate effects on calcium signaling, 8-HUDE upregulated the expression of TRPC1 and TRPC6 at both mRNA and protein levels in rat PASMCs, whereas it suppressed the expression of sEH. Our observations suggest that 8-HUDE increases PA vascular tone through increased release of calcium from intracellular stores, enhanced [Ca(2+)](i) influx in PASMCs through store-operated Ca(2+) channels and modulated the expression of TRPC and sEH proteins in a proconstrictive manner.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Boron Compounds / pharmacology
  • Caffeine / pharmacology
  • Calcium Channel Blockers / pharmacology
  • Calcium Signaling / drug effects
  • Cells, Cultured
  • Enzyme Inhibitors / pharmacology*
  • Epoxide Hydrolases / antagonists & inhibitors*
  • Fatty Acids, Monounsaturated / pharmacology*
  • Female
  • Imidazoles / pharmacology
  • Indoles / pharmacology
  • Lanthanum / pharmacology
  • Male
  • Mesenteric Arteries / drug effects
  • Muscle, Smooth, Vascular / drug effects
  • Nifedipine / pharmacology
  • Pulmonary Artery / drug effects*
  • Pulmonary Artery / enzymology
  • Rats
  • Rats, Wistar
  • Transient Receptor Potential Channels / antagonists & inhibitors*

Substances

  • 12-(3-hexylureido)dodec-8(Z)-enoic acid
  • Boron Compounds
  • Calcium Channel Blockers
  • Enzyme Inhibitors
  • Fatty Acids, Monounsaturated
  • Imidazoles
  • Indoles
  • Transient Receptor Potential Channels
  • Caffeine
  • Lanthanum
  • 2-aminoethoxydiphenyl borate
  • Epoxide Hydrolases
  • 1-(2-(3-(4-methoxyphenyl)propoxy)-4-methoxyphenylethyl)-1H-imidazole
  • Nifedipine
  • cyclopiazonic acid