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Br J Clin Pharmacol. 1990 Aug;30(2):287-91. doi: 10.1111/j.1365-2125.1990.tb03777.x.
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A metabolite of paludrine with high antimalarial activity.具有高抗疟活性的百乐君代谢物。
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THE CARBON MONOXIDE-BINDING PIGMENT OF LIVER MICROSOMES. I. EVIDENCE FOR ITS HEMOPROTEIN NATURE.肝微粒体的一氧化碳结合色素。I. 其血红蛋白性质的证据。
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双胍类抗疟药在人肝微粒体中的体外代谢：美芬妥英羟化酶（P450 MP）酶作用的证据。

In vitro metabolism of the biguanide antimalarials in human liver microsomes: evidence for a role of the mephenytoin hydroxylase (P450 MP) enzyme.

作者信息

Helsby N A, Ward S A, Howells R E, Breckenridge A M

机构信息

Department of Parasitology, Liverpool School of Tropical Medicine.

出版信息

Br J Clin Pharmacol. 1990 Aug;30(2):287-91. doi: 10.1111/j.1365-2125.1990.tb03777.x.

DOI:10.1111/j.1365-2125.1990.tb03777.x
PMID:2206791
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1368230/
Abstract

The metabolic activation of the arylbiguanide antimalarials proguanil (PG) and chlorproguanil (CPG) has been investigated in liver microsomes from three human livers. All three microsomal preparations activated the biguanides. The kinetic parameters for PG metabolism to cycloguanil (CG) were Km 21.8, 29.6 and 26.4 microM and Vmax 1.5, 5.9, and 8.2 pmol min-1 mg-1. The values for CPG conversion to chlorcycloguanil (CCG) were Km 12.9, 19.7 and 26.1 microM and Vmax 5.7, 4.8 and 3.6 pmol min-1 mg-1. The metabolic activation of both biguanides was competitively inhibited by the anticonvulsant mephenytoin. Sparteine and tolbutamide had no effect on biguanide metabolism. These data suggest an involvement of the mephenytoin hydroxylase enzyme, which exhibits a genetic polymorphism in man, in the metabolic activation of the biguanide antimalarials.

摘要

在来自三个人类肝脏的肝微粒体中，研究了芳基双胍类抗疟药氯胍（PG）和氯丙胍（CPG）的代谢活化情况。所有三种微粒体制剂均能活化双胍类药物。PG代谢为环氯胍（CG）的动力学参数为：米氏常数（Km）分别为21.8、29.6和26.4微摩尔，最大反应速度（Vmax）分别为1.5、5.9和8.2皮摩尔每分钟每毫克。CPG转化为氯环氯胍（CCG）的值为：Km分别为12.9、19.7和26.1微摩尔，Vmax分别为5.7、4.8和3.6皮摩尔每分钟每毫克。两种双胍类药物的代谢活化均受到抗惊厥药美芬妥英的竞争性抑制。司巴丁和甲苯磺丁脲对双胍类药物代谢无影响。这些数据表明，在人类中表现出遗传多态性的美芬妥英羟化酶参与了双胍类抗疟药的代谢活化过程。