Effect of calcium channel blockers on paraoxonase-1 (PON1) activity and oxidative stress
Küçük Resim Yok
Tarih
2014
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier B.V.
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
Background: In 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). Methods: PON1 was purified from human serum using simple chromatographic methods, including DEAE-Sephadex anion-exchange and Sephadex G-200 gel filtration chromatography. Results: The 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. Conclusions: Our 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 0.121 mM, 0.130 mM, 0.255 mM, and 0.304 mM, respectively, and the Ki constants were calculated to be 0.222 ± 0.049 mM, 0.151 ± 0.067 mM, 0.286 ± 0.137 mM, and 0.321 ± 0.002 mM, respectively. © 2014 Institute of Pharmacology, Polish Academy of Sciences. Published by Elsevier Urban & Partner Sp. z o.o. All rights reserved.
Açıklama
Anahtar Kelimeler
Amlodipine besylate, Isradipine, Nifedipine, Nitrendipine, Paraoxonase, amlodipine besylate, ammonium sulfate, aryldialkylphosphatase 1, calcium channel blocking agent, isradipine, nifedipine, nitrendipine, amlodipine, aryldialkylphosphatase, calcium channel blocking agent, isradipine, nifedipine, PON1 protein, human, anion exchange chromatography, article, competitive inhibition, controlled study, drug binding, drug effect, drug structure, enzyme activity, enzyme inhibition, fractionation, gel filtration chromatography, human, in vitro study, oxidative stress, antagonists and inhibitors, drug effects, metabolism, oxidative stress, Amlodipine, Aryldialkylphosphatase, Calcium Channel Blockers, Humans, Isradipine, Nifedipine, Nitrendipine, Oxidative Stress, Amlodipine besylate, Isradipine, Nifedipine, Nitrendipine, Paraoxonase, amlodipine besylate, ammonium sulfate, aryldialkylphosphatase 1, calcium channel blocking agent, isradipine, nifedipine, nitrendipine, amlodipine, aryldialkylphosphatase, calcium channel blocking agent, isradipine, nifedipine, PON1 protein, human, anion exchange chromatography, article, competitive inhibition, controlled study, drug binding, drug effect, drug structure, enzyme activity, enzyme inhibition, fractionation, gel filtration chromatography, human, in vitro study, oxidative stress, antagonists and inhibitors, drug effects, metabolism, oxidative stress, Amlodipine, Aryldialkylphosphatase, Calcium Channel Blockers, Humans, Isradipine, Nifedipine, Nitrendipine, Oxidative Stress
Kaynak
Pharmacological Reports
WoS Q Değeri
Q3
Scopus Q Değeri
N/A
Cilt
66
Sayı
1
