In vitro inhibitory effects of palonosetron hydrochloride, bevacizumab and cyclophosphamide on purified paraoxonase-I (hPON1) from human serum

Turkes C., SÖYÜT H. , Beydemir S.

ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY, vol.42, pp.252-257, 2016 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 42
  • Publication Date: 2016
  • Doi Number: 10.1016/j.etap.2015.11.024
  • Page Numbers: pp.252-257
  • Keywords: Paraoxonase, Inhibition, Palonosetron hydrochloride, Bevacizumab, Cyclophosphamide, OXIDATIVE STRESS, PON1 ACTIVITY, POLYMORPHISMS, PURIFICATION, DRUGS, BROMOPHENOLS, CHOLESTEROL, ERYTHROCYTE, POPULATION, PLASMA


In this study, we investigated the effects of the drugs, palonosetron hydrochloride, bevacizumab and cyclophosphamide, on human serum paraoxonase-I (hPON1) enzyme activity in in vitro conditions. The enzyme was purified similar to 231-fold with 34.2% yield by using ammonium sulphate precipitation, DEAE-Sephadex A-50 ion-exchange chromatography and Sephadex G-200 gel-filtration chromatography from human serum. hPON1 exhibited a single protein band on the SDS polyacrylamide gel electrophoresis. The inhibition studies were performed on paraoxonase activity of palonosetron hydrochloride, bevacizumab and cyclophosphamide. K-i constants were found as 0.033 +/- 0.001, 0.0544 +/- 0.003 mM and 3.419 +/- 0.518 mM, respectively. Compared to the inhibition rates of the drugs, palonosetron hydrochloride has the maximum inhibition rate. However, inhibition mechanisms of the drugs were determined as noncompetitive by Lineweaver-Burk curves. (C) 2016 Elsevier B.V. All rights reserved.