Abstract
BackgroundIn this study, we investigated the in vitro effects of calcium channel blockers (nifedipine, nitrendipine, isradipine, and amlodipine besylate) on the activity of paraoxonase-1 (PON1). MethodsPON1 was purified from human serum using simple chromatographic methods, including DEAE-Sephadex anion-exchange and Sephadex G-200 gel filtration chromatography. ResultsThe calcium channel blockers decreased the in vitro PON1 activity. The inhibition mechanism of amlodipine besylate was noncompetitive, whereas nifedipine, nitrendipine, and isradipine were competitive inhibitors. ConclusionsOur results showed that calcium channel blockers exhibit inhibitory effects on PON1 at low concentrations. The IC50 values for nifedipine, nitrendipine, isradipine, and amlodipine besylate were determined to be 0.121mM, 0.130mM, 0.255mM, and 0.304mM, respectively, and the Ki constants were calculated to be 0.222±0.049mM, 0.151±0.067mM, 0.286±0.137mM, and 0.321±0.002mM, respectively.
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