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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >In vitro inhibition effect of some coumarin compounds on purified human serum paraoxonase 1 (PON1)
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In vitro inhibition effect of some coumarin compounds on purified human serum paraoxonase 1 (PON1)

机译:某些香豆素类化合物对体外纯化人血清对氧磷酶1(PON1)的抑制作用

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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.
机译:摘要人血清对氧磷酶1(PON1; EC 3.1.8.1)是一种高密度脂蛋白相关,钙依赖性酶,可水解芳香族酯,有机磷酸酯和内酯,可保护低密度脂蛋白免于氧化。在这项研究中,研究了一些羟基和二羟基离子香豆素衍生物(1-20)对纯化的PON1活性的体外作用。在这些化合物中,衍生物11 – 20是水溶性的。在研究的化合物中,发现化合物6和13分别对PON1最具活性(IC 50 α=?35和34?μM)。本研究表明,PON1活性对研究的香豆素衍生物非常敏感。

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