[Mechanism related to docosahexaenoic acid induced large conductance calcium-activated potassium channel currents increase in coronary smooth muscle cells]

Zhonghua Xin Xue Guan Bing Za Zhi. 2011 Apr;39(4):348-52. doi: 10.3760/cma.j.issn.0253-3758.2011.04.014.
[Article in Chinese]

Abstract

Objective: To investigate the mechanism of enhanced large conductance calcium-activated potassium channel currents (BK) in coronary smooth muscle cells (SMCs) by docosahexaenoic acid (DHA).

Methods: Coronary SMCs were isolated by enzyme digestion. Potassium channels in coronary SMCs were identified by applications of different potassium blockers. Effects of DHA and its metabolite 16, 17-epoxydocosapentaenoic acid (16, 17-EDP) on BK channels in the absence and presence of cytochrome P450 epoxygenase inhibitor SKF525A were studied by patch clamp in whole-cell configuration.

Results: BK channels were widely distributed in SMCs, and BK currents in normal SMCs accounted for (64.2 ± 2.7)% of total potassium currents (n = 20). DHA could activate BK channels, and its 50% effective concentration (EC(50)) was (0.23 ± 0.03) µmol/L, however, the effect of DHA on BK channels was abolished after SMCs were incubated with cytochrome P450 epoxygenase inhibitor SKF525A. 16, 17-EDP, a metabolite of DHA, could reproduce the effects of DHA on BK channels, and its EC(50) was (19.7 ± 2.8) nmol/L.

Conclusion: DHA and metabolites can activate BK channels and dilate coronary arteries through activating cytochrome P450 epoxygenase pathway.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Coronary Vessels / cytology*
  • Coronary Vessels / drug effects
  • Coronary Vessels / metabolism
  • Cytochrome P-450 Enzyme Inhibitors
  • Docosahexaenoic Acids / pharmacology*
  • Fatty Acids, Unsaturated / pharmacology
  • Large-Conductance Calcium-Activated Potassium Channels / metabolism*
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Myocytes, Smooth Muscle / drug effects*
  • Myocytes, Smooth Muscle / metabolism*
  • Proadifen / pharmacology
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Cytochrome P-450 Enzyme Inhibitors
  • Fatty Acids, Unsaturated
  • Large-Conductance Calcium-Activated Potassium Channels
  • Docosahexaenoic Acids
  • Proadifen
  • docosapentaenoic acid