title: Antioxidant effect of a new calcium antagonist, azelnidipine, in cultured human arterial endothelial cells.
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.
authors.affiliation: Second Department of Internal Medicine, Kagawa Medical University, Kagawa, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Shinomiya
authors.forename: K
authors.initials: K
authors.lastname: Mizushige
authors.forename: M
authors.initials: M
authors.lastname: Fukunaga
authors.forename: H
authors.initials: H
authors.lastname: Masugata
authors.forename: K
authors.initials: K
authors.lastname: Ohmori
authors.forename: M
authors.initials: M
authors.lastname: Kohno
authors.forename: S
authors.initials: S
authors.lastname: Senda
mesh_terms: 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
chemical_list: D000975:Antioxidants; D002121:Calcium Channel Blockers; D004095:Dihydropyridines; C075750:8-epi-prostaglandin F2alpha; D001383:Azetidinecarboxylic Acid; D015237:Dinoprost; C061679:azelnidipine