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

Küçük Resim Yok

Tarih

2016

Dergi Başlığı

Dergi ISSN

Cilt Başlığı

Yayıncı

Taylor & Francis Ltd

Erişim Hakkı

info:eu-repo/semantics/openAccess

Özet

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 mu M) for PON1, respectively. The present study has demonstrated that PON1 activity is very highly sensitive to studied coumarin derivatives.

Açıklama

Anahtar Kelimeler

Coumarin derivatives, in vitro inhibition, paraoxonase

Kaynak

Journal of Enzyme Inhibition and Medicinal Chemistry

WoS Q Değeri

Q1

Scopus Q Değeri

Q1

Cilt

31

Sayı

4

Künye