Some indazoles reduced the activity of human serum paraoxonase 1, an antioxidant enzyme: in vitro inhibition and molecular modeling studies

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dc.contributor.authorAlım, Zuhal
dc.contributor.authorKılıç, Deryanur
dc.contributor.authorDemir, Yeliz
dc.date.accessioned13.07.201910:50:10
dc.date.accessioned2019-07-16T08:25:55Z
dc.date.available13.07.201910:50:10
dc.date.available2019-07-16T08:25:55Z
dc.date.issued2019
dc.departmentFen Edebiyat Fakültesi
dc.description.abstractBackground: Paraoxonase 1 (PON1: EC 3.1.8.1) is a vital antioxidant enzyme against mainly atherosclerosis and many other diseases associated with oxidative stress. Thus, studies related to PON1 have an important place in the pharmacology. In this study, we aimed to evaluate the in vitro inhibition effects of some indazoles on the activity of human PON1. Methods: PON1 was purified from human serum with a specific activity of 5000?U/mg and 13.50% yield by using simple chromatographic methods. Results: The indazoles showed K i values in a range of 26.0?±?3.00–111?±?31.0?µM against hPON1. All these indazoles exhibited competitive inhibition. In addition, molecular docking studies were performed in order to assess the probable binding mechanisms into the active site of hPON1. Molecular modeling studies confirmed our results. Conclusions: Inhibition of PON1 by indazoles supplies a verification to further consideration of limitation dosage of indazole molecule groups as drug. © 2018 Informa UK Limited, trading as Taylor & Francis Group
dc.identifier.doi10.1080/13813455.2018.1470646
dc.identifier.endpage9en_US
dc.identifier.issn1381-3455
dc.identifier.scopusqualityQ1
dc.identifier.startpage1en_US
dc.identifier.urihttps://dx.doi.org/10.1080/13813455.2018.1470646
dc.identifier.urihttps://hdl.handle.net/20.500.12451/3103
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherTaylor and Francis Ltd
dc.relation.ispartofArchives of Physiology and Biochemistry
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectEnzyme İnhibition
dc.subjectİndazole
dc.subjectMolecular Modeling
dc.subjectParaoxonase 1
dc.subjectPurification
dc.titleSome indazoles reduced the activity of human serum paraoxonase 1, an antioxidant enzyme: in vitro inhibition and molecular modeling studies
dc.typeArticle

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