Assessment of the inhibitory effects and molecular docking of some sulfonamides on human serum paraoxonase 1

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dc.authoridKılıç, Deryanur -- 0000-0002-9115-136X
dc.contributor.authorAlım, Zuhal
dc.contributor.authorKılıç, Deryanur
dc.contributor.authorKöksal, Zeynep
dc.contributor.authorBeydemir, Şükrü
dc.contributor.authorÖzdemir, Hasan
dc.date.accessioned13.07.201910:50:10
dc.date.accessioned2019-07-29T19:28:44Z
dc.date.available13.07.201910:50:10
dc.date.available2019-07-29T19:28:44Z
dc.date.issued2017
dc.departmentSabire Yazıcı Fen Edebiyat Fakültesi
dc.description.abstractParaoxonase-1 (PON1) is an organophosphate hydrolyzer and antiatherogenic enzyme. Due to the PON1's crucial functions, inhibitors and activators of PON1 must be known for pharmacological applications. In this study, we investigated the in vitro effects of some sulfonamides compounds on human serum PON1 (hPON1). For this aim, we purified the hPON1 from human serum with high specific activity by using simple chromatographic methods, and after the purification processes, we investigated in vitro interactions between the enzyme and some sulfonamides (2-amino-5-methyl-1,3-benzenedisulfonamide, 2-chloro-4-sulfamoilaniline, 4-amino-3-methylbenzenesulfanilamide, sulfisoxazole, sulfisomidine, and 5-amino-2-methylbenzenesulfonamide). IC50, K-i values, and inhibition types were calculated for each sulfonamide. 2-amino-5-methyl-1,3-benzenedisulfonamide and 2-chloro-4-sulfamoilaniline exhibited noncompetitive inhibition effect, whereas 4-amino-3-methylbenzenesulfanilamide, sulfisoxazole, and sulfisomidine exhibited mixed type inhibition. On the other hand, 5-amino-2-methylbenzenesulfonamide showed competitive inhibition and so molecular docking studies were performed for this compound in order to assess the probable binding mechanism into the active site of hPON1.
dc.identifier.doi10.1002/jbt.21950
dc.identifier.issn1095-6670
dc.identifier.issn1099-0461
dc.identifier.issue10en_US
dc.identifier.scopusqualityQ2
dc.identifier.urihttps://doi.org/10.1002/jbt.21950
dc.identifier.urihttps://hdl.handle.net/20.500.12451/6078
dc.identifier.volume31en_US
dc.identifier.wosWOS:000412328200009
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherWiley
dc.relation.ispartofJournal of Biochemical and Molecular Toxicology
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/closedAccess
dc.subjectAtherosclerosis
dc.subjectInhibition
dc.subjectMolecular Docking
dc.subjectParaoxonase-1
dc.subjectSulfonamide
dc.titleAssessment of the inhibitory effects and molecular docking of some sulfonamides on human serum paraoxonase 1
dc.typeArticle

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