title: In vitro inhibition effect of some coumarin compounds on purified human serum paraoxonase 1 (PON1).
abstract: Human 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 effect of some hydroxy and dihydroxy ionic coumarin derivatives (1-20) on purified PON1 activity was investigated. Among these compounds, derivatives 11-20 are water soluble. In investigated compounds, compounds 6 and 13 were found the most active (IC50 = 35 and 34 µM) for PON1, respectively. The present study has demonstrated that PON1 activity is very highly sensitive to studied coumarin derivatives.
authors.affiliation: a Department of Biochemistry, Faculty of Pharmacy , Suleyman Demirel University , Isparta , Turkey .
authors.forename: Basak
authors.initials: B
authors.lastname: Gokce
authors.affiliation: b Department of Chemistry, Faculty of Art and Sciences , Balikesir University , Balikesir , Turkey , and.
authors.forename: Nahit
authors.initials: N
authors.lastname: Gencer
authors.affiliation: b Department of Chemistry, Faculty of Art and Sciences , Balikesir University , Balikesir , Turkey , and.
authors.forename: Oktay
authors.initials: O
authors.lastname: Arslan
authors.affiliation: c Department of Chemistry, Faculty of Arts and Sciences , Inonu University , Malatya , Turkey.
authors.forename: Mert Olgun
authors.initials: MO
authors.lastname: Karatas
authors.affiliation: c Department of Chemistry, Faculty of Arts and Sciences , Inonu University , Malatya , Turkey.
authors.forename: Bulent
authors.initials: B
authors.lastname: Alici
mesh_terms: D043303:Aryldialkylphosphatase / Q000037:antagonists & inhibitors* / Q000302:isolation & purification / Q000378:metabolism; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D003374:Coumarins; D004791:Enzyme Inhibitors; D043303:Aryldialkylphosphatase; C468406:PON1 protein, human
keywords: Coumarin derivatives; in vitro inhibition; paraoxonase