Some coumarins and benzoxazinones as potent paraoxonase 1 inhibitors

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dc.authoridKarataş, Mert Olgun/0000-0001-8500-2088
dc.authoridUSLU, HARUN/0000-0001-8827-8557
dc.authoridGençer, Nahit/0000-0001-7092-8857
dc.authoridALICI, Bulent/0000-0001-5009-3223
dc.authoridGençer, Nahit/0000-0001-7092-8857
dc.authoridGokce, Basak/0000-0001-8548-9703
dc.authorwosidKarataş, Mert Olgun/ABG-7848-2020
dc.authorwosidUSLU, HARUN/P-3681-2019
dc.authorwosidGençer, Nahit/HHD-1544-2022
dc.authorwosidALICI, Bulent/AAG-4203-2019
dc.authorwosidGençer, Nahit/AAG-4507-2019
dc.contributor.authorKaratas, Mert Olgun
dc.contributor.authorUslu, Harun
dc.contributor.authorAlici, Bulent
dc.contributor.authorGokce, Basak
dc.contributor.authorGencer, Nahit
dc.contributor.authorArslan, Oktay
dc.date.accessioned2024-08-04T20:41:31Z
dc.date.available2024-08-04T20:41:31Z
dc.date.issued2016
dc.departmentİnönü Üniversitesien_US
dc.description.abstractIn this study, we aimed to investigate the effect of some coumarin and benzoxazinone derivatives on the activity of human PON1. Human serum paraoxonase 1 was purified from fresh human serum blood by two-step procedures that are ammonium sulfate precipitation (60-80%) and then hydrophobic interaction chromatography (Sepharose 4B, L-tyrosine and 1-napthylamine). The enzyme was purified 232-fold with a final specific activity of 27.1 U/mg. In vitro effects of some previously synthesized ionic coumarin or benzoxazinone derivatives (1-21) on purified PON1 activity were investigated. Compound 14 (1-(2,3,4,5,6)-pentamethyl-benzyl-3-(6,8-dimethyl-2H-chromen-2-one-4-yl)) benzimidazolium chloride was found out as the strongest inhibitor (IC50 = 7.84 mu M) for PON1 among the compounds. Kinetic investigation and molecular docking study were evaluated for one of the most active compounds (compound 12) and obtained data showed that this compound is competitive inhibitor of PON1 and interact with Leu262 and Ser263 in the active site of PON1. Moreover, coumarin derivatives were found out as the more potent inhibitors for PON1 than benzoxazinone derivatives.en_US
dc.description.sponsorshipResearch Fund of the Balikesir University [2014-54]en_US
dc.description.sponsorshipThis work was supported by the Research Fund of the Balikesir University (project no. 2014-54).en_US
dc.identifier.doi10.3109/14756366.2016.1142982
dc.identifier.endpage1391en_US
dc.identifier.issn1475-6366
dc.identifier.issn1475-6374
dc.identifier.issue6en_US
dc.identifier.pmid26887799en_US
dc.identifier.scopus2-s2.0-84958747701en_US
dc.identifier.scopusqualityQ1en_US
dc.identifier.startpage1386en_US
dc.identifier.urihttps://doi.org/10.3109/14756366.2016.1142982
dc.identifier.urihttps://hdl.handle.net/11616/97182
dc.identifier.volume31en_US
dc.identifier.wosWOS:000385270300068en_US
dc.identifier.wosqualityQ1en_US
dc.indekslendigikaynakWeb of Scienceen_US
dc.indekslendigikaynakScopusen_US
dc.indekslendigikaynakPubMeden_US
dc.language.isoenen_US
dc.publisherTaylor & Francis Ltden_US
dc.relation.ispartofJournal of Enzyme Inhibition and Medicinal Chemistryen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/openAccessen_US
dc.subjectBenzoxazinoneen_US
dc.subjectcoumarinen_US
dc.subjectdockingen_US
dc.subjectinhibitionen_US
dc.subjectparaoxonaseen_US
dc.titleSome coumarins and benzoxazinones as potent paraoxonase 1 inhibitorsen_US
dc.typeArticleen_US

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