Human serum paraoxonase-1 (hPON1): <i>in vitro</i> inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium


TÜRKEŞ C., SÖYÜT H., BEYDEMİR Ş.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.30, no.4, pp.622-628, 2015 (SCI-Expanded) identifier identifier identifier

Abstract

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.