In vitro inhibitory effects of palonosetron hydrochloride, bevacizumab and cyclophosphamide on purified paraoxonase-I (hPON1) from human serum
Environmental Toxicology and Pharmacology, vol.42, pp.252-257, 2016 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 42
- Publication Date: 2016
- Doi Number: 10.1016/j.etap.2015.11.024
- Journal Name: Environmental Toxicology and Pharmacology
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.252-257
- Keywords: Bevacizumab, Cyclophosphamide, Inhibition, Palonosetron hydrochloride, Paraoxonase
- Bilecik Şeyh Edebali University Affiliated: Yes
Abstract
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 ~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. Ki constants were found as 0.033 ± 0.001, 0.054 ± 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.