title: In vitro inhibitory effects of palonosetron hydrochloride, bevacizumab and cyclophosphamide on purified paraoxonase-I (hPON1) from human serum.
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.
authors.affiliation: Department of Chemistry, Faculty of Science, Atatürk University, 25240, Erzurum, Turkey.
authors.forename: Cüneyt
authors.initials: C
authors.lastname: Türkeş
authors.affiliation: Department of Primary Education, Faculty of Education, Bayburt University, 69000, Bayburt, Turkey.
authors.forename: Hakan
authors.initials: H
authors.lastname: Söyüt
authors.affiliation: Department of Chemistry, Faculty of Science, Atatürk University, 25240, Erzurum, Turkey. Electronic address: beydemir@atauni.edu.tr.
authors.forename: Şükrü
authors.initials: Ş
authors.lastname: Beydemir
mesh_terms: D043303:Aryldialkylphosphatase / Q000378:metabolism*; D000068258:Bevacizumab / Q000494:pharmacology*; D002850:Chromatography, Gel; D003520:Cyclophosphamide / Q000494:pharmacology*; D003637:DEAE-Dextran / Q000031:analogs & derivatives; D003911:Dextrans; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006801:Humans; D007546:Isoquinolines / Q000494:pharmacology*; D000077924:Palonosetron; D011812:Quinuclidines / Q000494:pharmacology*
chemical_list: D003911:Dextrans; D004791:Enzyme Inhibitors; D007546:Isoquinolines; D011812:Quinuclidines; D000068258:Bevacizumab; C027184:DEAE-Sephadex A-50; D000077924:Palonosetron; D003520:Cyclophosphamide; C025614:sephadex; D003637:DEAE-Dextran; D043303:Aryldialkylphosphatase
keywords: Bevacizumab; Cyclophosphamide; Inhibition; Palonosetron hydrochloride; Paraoxonase