IN-VITRO ANTIOXIDANT ACTIVITY OF CALCIUM-ANTAGONISTS AGAINST LDL OXIDATION COMPARED WITH ALPHA-TOCOPHEROL

The dose-dependent (1, 5, 10, 50 mu M) antioxidative activity of calcium antagonists (verapamil, diltiazem, nifedipine, amlodipine, isradipine or lacidipine) and alpha-tocopherol against copper-induced LDL (0.25 mg/ml) oxidation was compared by measuring the diene formation and the content of TBARS. For diltiazem no antioxidant effect could be found, whereas the other calcium antagonists and a-tocopherol have demonstrated antioxidant activity at least at concentrations of 10 and 50 mu M: alpha-tocopherol > lacidipine > nifedipine > isradipine, verapamil, amlodipine. Additionally, alpha-tocopherol and lacidipine were able to attenuate LDL-oxidation significantly at 1 and 5 mu M These results indicate in vitro antioxidative activity of calcium antagonists especially from the dihydropyridine-type with greatest activity for the strongly lipophilic lacidipine. This might be one possible antiatherogenic mechanism of calcium antagonists, since oxidative modification enhances the atherogenic potential of LDL. (C) 1994 Academic Inc. Press,