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一些嘧啶化合物对大鼠脑单胺氧化酶-B 的体外影响。

Effect of some pyrimidine compounds on rat brain monoamine oxidase-B in vitro.

机构信息

Biochemistry Department, Faculty of Science, Alexandria University, Alexandria, Egypt.

出版信息

J Physiol Biochem. 2012 Dec;68(4):475-84. doi: 10.1007/s13105-012-0160-4. Epub 2012 Mar 31.

Abstract

The effects of some pyrimidine compounds (PCs) including barbituric acid (BA) 5,5-diethyl barbituric acid (DEBA), 2-thiobarbituric acid (TBA), violuric acid (VA), 2-thiouracil (TU), and 6-amino-2-thiouracil (ATU) on the activity of rat brain monoamine oxidase-B (MAO-B) were investigated. The results revealed that MAO-B was activated by BA, DEBA, TBA, TU, and ATU, and the activation was structural, concentration, and time dependent. However, MAO-B was inhibited by VA in a noncompetitive and irreversible manner with an enzyme-inhibitor dissociation constant (K (i) value) of 32 nM and IC(50) equals to 19 nM. All the studied PCs changed both the optimum pH and temperature of MAO-B.

摘要

研究了几种嘧啶类化合物(PCs),包括巴比妥酸(BA)、5,5-二乙基巴比妥酸(DEBA)、2-硫代巴比妥酸(TBA)、尿刊酸(VA)、2-硫代尿嘧啶(TU)和6-氨基-2-硫代尿嘧啶(ATU)对大鼠脑单胺氧化酶-B(MAO-B)活性的影响。结果表明,BA、DEBA、TBA、TU 和 ATU 可激活 MAO-B,这种激活具有结构、浓度和时间依赖性。然而,VA 以非竞争性和不可逆的方式抑制 MAO-B,其酶抑制剂解离常数(K(i)值)为 32 nM,IC(50)值等于 19 nM。所有研究的 PCs 均改变了 MAO-B 的最适 pH 值和温度。

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