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

Türkeş C., Söyüt H., Beydemir Ş.

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

  • Publication Type: Article / Article
  • Volume: 42
  • Publication Date: 2016
  • Doi Number: 10.1016/j.etap.2015.11.024
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.252-257
  • Keywords: Paraoxonase, Inhibition, Palonosetron hydrochloride, Bevacizumab, Cyclophosphamide, OXIDATIVE STRESS, PON1 ACTIVITY, POLYMORPHISMS, PURIFICATION, DRUGS, BROMOPHENOLS, CHOLESTEROL, ERYTHROCYTE, POPULATION, PLASMA
  • Erzincan Binali Yildirim University Affiliated: Yes


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.