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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium
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Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium

机译：人血清对氧磷酶-1（hPON1）：盐酸莫西沙星，左氧氟沙星半水合物，盐酸头孢吡肟，头孢噻肟钠和头孢唑肟钠的体外抑制作用

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摘要

In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. K-i constants were calculated to be 2.641 +/- 0.040 mM, 5.525 +/- 0.817 mM, 35.092 +/- 1.093 mM, 252.762 +/- 5.749 mM and 499.244 +/- 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.
机译：在这项研究中，我们研究了抗菌药物（盐酸莫西沙星，盐酸左氧氟沙星，盐酸头孢吡肟，头孢噻肟钠和头孢唑肟钠）对人血清体外对氧磷酶-1（hPON1）酶活性的影响。为此，使用简单的色谱方法从人血清中纯化了hPON1酶。抗菌药物在低浓度下对hPON1表现出抑制作用。计算出的K-i常数分别为2.641 +/- 0.040mM，5.525 +/- 0.817mM，35.092 +/- 1.093mM，252.762 +/- 5.749mM和499.244 +/- 10.149mM。盐酸莫西沙星的抑制机理是竞争性的，而左氧氟沙星半水合物，盐酸头孢吡肟，头孢噻肟钠和头孢唑肟钠是非竞争性抑制剂。

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