Antioxidant effect of a new calcium antagonist, azelnidipine, in cultured human arterial endothelial cells

J Int Med Res. 2004 Mar-Apr;32(2):170-5. doi: 10.1177/147323000403200210.

Abstract

Azelnidipine is a novel dihydropyridine-type calcium antagonist with long-acting anti-hypertensive action and a low reported incidence of tachycardia. We aimed to evaluate its antioxidant activity in cultured human arterial endothelial cells under oxidative stress. Endothelial cells were exposed to 1 mM H2O2 and treated with 100 microM alpha-tocopherol, 1 nM, 10 nM or 100 nM azelnidipine, 100 nM nifedipine or 100 nM amlodipine. After 3 h, the cell number and level of lipid peroxidation were evaluated by measuring the total protein and 8-iso-PGF2 alpha concentrations, respectively. The total protein concentration was similar with each treatment. Inhibition of 8-iso-PGF2 alpha was greatest with 10 nM azelnidipine (compared with the other drugs); the difference between 10 nM and 100 nM azelnidipine was not significant. We conclude that azelnidipine has a potent antioxidative effect that could be of significant clinical benefit when combined with its long-lasting anti-hypertensive action and low incidence of tachycardia.

MeSH terms

  • Antioxidants / pharmacology*
  • Azetidinecarboxylic Acid / analogs & derivatives*
  • Azetidinecarboxylic Acid / pharmacology*
  • Calcium Channel Blockers / pharmacology*
  • Cells, Cultured
  • Dihydropyridines / pharmacology*
  • Dinoprost / analogs & derivatives*
  • Dinoprost / metabolism
  • Endothelium, Vascular / cytology
  • Endothelium, Vascular / drug effects*
  • Endothelium, Vascular / metabolism
  • Humans

Substances

  • Antioxidants
  • Calcium Channel Blockers
  • Dihydropyridines
  • 8-epi-prostaglandin F2alpha
  • Azetidinecarboxylic Acid
  • Dinoprost
  • azelnidipine