Antioxidant effect of a new calcium antagonist, azelnidipine, in cultured human arterial endothelial cells.
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.
Shinomiya
K
K
Second Department of Internal Medicine, Kagawa Medical University, Kagawa, Japan.
Mizushige
K
K
Fukunaga
M
M
Masugata
H
H
Ohmori
K
K
Kohno
M
M
Senda
S
S
D000975:Antioxidants / Q000494:pharmacology*; D001383:Azetidinecarboxylic Acid / Q000031:analogs & derivatives* / Q000494:pharmacology*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002478:Cells, Cultured; D004095:Dihydropyridines / Q000494:pharmacology*; D015237:Dinoprost / Q000031:analogs & derivatives* / Q000378:metabolism; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D006801:Humans
D000975:Antioxidants; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C075750:8-epi-prostaglandin F2alpha; D001383:Azetidinecarboxylic Acid; D015237:Dinoprost; C061679:azelnidipine