In vitro inhibitory effects of palonosetron hydrochloride, bevacizumab and cyclophosphamide on purified paraoxonase-I (hPON1) from human serum
Küçük Resim Yok
Tarih
2016
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Elsevier B.V.
Erişim Hakkı
info:eu-repo/semantics/closedAccess
Özet
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. © 2016 Elsevier B.V.
Açıklama
Anahtar Kelimeler
Bevacizumab, Cyclophosphamide, Inhibition, Palonosetron hydrochloride, Paraoxonase, aryldialkylphosphatase, aryldialkylphosphatase 1, bevacizumab, cyclophosphamide, messenger RNA, palonosetron, aryldialkylphosphatase, bevacizumab, cyclophosphamide, DEAE-Sephadex A-50, dextran, diethylaminoethyldextran, enzyme inhibitor, isoquinoline derivative, palonosetron, quinuclidine derivative, sephadex, Article, blood level, controlled study, drug mechanism, enzyme activity, enzyme assay, enzyme inhibition, enzyme purification, gel filtration chromatography, gene expression, human, IC50, in vitro study, ion exchange chromatography, molecular dynamics, polyacrylamide gel electrophoresis, priority journal, analogs and derivatives, metabolism, size exclusion chromatography, Aryldialkylphosphatase, Bevacizumab, Chromatography, Gel, Cyclophosphamide, DEAE-Dextran, Dextrans, Enzyme Inhibitors, Humans, Isoquinolines, Quinuclidines, Bevacizumab, Cyclophosphamide, Inhibition, Palonosetron hydrochloride, Paraoxonase, aryldialkylphosphatase, aryldialkylphosphatase 1, bevacizumab, cyclophosphamide, messenger RNA, palonosetron, aryldialkylphosphatase, bevacizumab, cyclophosphamide, DEAE-Sephadex A-50, dextran, diethylaminoethyldextran, enzyme inhibitor, isoquinoline derivative, palonosetron, quinuclidine derivative, sephadex, Article, blood level, controlled study, drug mechanism, enzyme activity, enzyme assay, enzyme inhibition, enzyme purification, gel filtration chromatography, gene expression, human, IC50, in vitro study, ion exchange chromatography, molecular dynamics, polyacrylamide gel electrophoresis, priority journal, analogs and derivatives, metabolism, size exclusion chromatography, Aryldialkylphosphatase, Bevacizumab, Chromatography, Gel, Cyclophosphamide, DEAE-Dextran, Dextrans, Enzyme Inhibitors, Humans, Isoquinolines, Quinuclidines
Kaynak
Environmental Toxicology and Pharmacology
WoS Q Değeri
Q2
Scopus Q Değeri
Q1
Cilt
42
