In vitro inhibition effect of some dihydroxy coumarin compounds on purified human serum paraoxonase 1 (PON1)

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dc.authoridBasaran, Ismet -- 0000-0001-7641-8938
dc.contributor.authorErzengin, Mahmut
dc.contributor.authorBaşaran, İsmet
dc.contributor.authorÇakır, Umit
dc.contributor.authorAybey, Aynur
dc.contributor.authorSinan, Selma
dc.date.accessioned13.07.201910:50:10
dc.date.accessioned2019-07-29T19:28:08Z
dc.date.available13.07.201910:50:10
dc.date.available2019-07-29T19:28:08Z
dc.date.issued2012
dc.departmentSabire Yazıcı Fen Edebiyat Fakültesi
dc.description.abstractHuman serum paraoxonase 1 (PON1; EC 3.1.8.1) is a high-density lipoprotein associated, calcium-dependent enzyme that hydrolyses aromatic esters, organophosphates and lactones and can protect the low-density lipoprotein against oxidation. In this study, in vitro inhibition effect of some dihydroxy coumarin compounds namely 6,7-dihydroxy-3-(2-methylphenyl)-2H-chromen-2-one (A), 6,7-dihydroxy-3-(3-methylphenyl)-2H-chromen-2-one (B) and 6,7-dihydroxy-3-(4-methylphenyl)-2H-chromen-2-one (C) on purified PON1 were investigated by using paraoxon as a substrate. PON1 was purified using two-step procedures, namely ammonium sulphate precipitation and Sepharose-4B-l-tyrosine-1-naphthylamine hydrophobic interaction chromatography. The purified enzyme had a specific activity of 11.76 U/mg. The dihydroxy coumarin derivatives of A and B compounds inhibited PON1 enzyme activity in a noncompetitive inhibition manner with K (i) of 0.0080 +/- 0.256 and 0.0003 +/- 0.018 mM values, respectively. C compound exerted an uncompetitive inhibition of PON1 enzyme activity with K (i) of 0.0010 +/- 0.173 mM. Moreover, dihydroxy coumarin derivatives of A, B and C compounds were effective inhibitors on purified human serum PON1 activity with IC50 of 0.012, 0.022 and 0.003 mM values, respectively. IC50 value of unsubstituted 6,7 dihydroxy coumarin was found as 0.178 mM. The present study has demonstrated that PON1 activity is very highly sensitive to studied coumarin derivatives.
dc.identifier.doi10.1007/s12010-012-9876-4
dc.identifier.endpage1548en_US
dc.identifier.issn0273-2289
dc.identifier.issue6en_US
dc.identifier.pmid22971832
dc.identifier.scopusqualityQ2
dc.identifier.startpage1540en_US
dc.identifier.urihttps://doi.org/10.1007/s12010-012-9876-4
dc.identifier.urihttps://hdl.handle.net/20.500.12451/5992
dc.identifier.volume168en_US
dc.identifier.wosWOS:000311310400015
dc.identifier.wosqualityN/A
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.indekslendigikaynakPubMed
dc.language.isoen
dc.publisherHumana Press
dc.relation.ispartofApplied Biochemistry and Biotechnology
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectParaoxonase 1
dc.subjectIn Vitro Inhibition
dc.subjectCoumarin Derivatives
dc.titleIn vitro inhibition effect of some dihydroxy coumarin compounds on purified human serum paraoxonase 1 (PON1)
dc.typeArticle

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