1-methyl-2-undecyl-4(1H)-quinolone as an irreversible and selective inhibitor of type B monoamine oxidase

被引：37

作者：

Lee, MK

Hwang, BY

Lee, SA

Oh, GJ

Choi, WH

Hong, SS

Lee, KS

Ro, JS ^{[1
]}

机构：

[1] Chungbuk Natl Univ, Coll Pharm, Cheongju 361763, South Korea

[2] Chungbuk Natl Univ, Res Ctr Bioresource & Hlth, Cheonju 361763, South Korea

[3] Univ Illinois, Coll Pharm, Program Collaborat Res Pharmaceut Sci, Chicago, IL 60612 USA

[4] Univ Illinois, Coll Pharm, Dept Med Chem & Pharmacognosy, Chicago, IL 60612 USA

[5] Samjin Pharm Co Ltd, Hwasung 445920, South Korea

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2003年 / 51卷 / 04期

关键词：

1-methyl-2-undecyl-4(1H)-quinolone; Evodia rutaecarpa; monoamine oxidase inhibitor;

D O I：

10.1248/cpb.51.409

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The inhibitory compound of monoamine oxidase (MAO) activity was isolated from the CH2Cl2 fraction of the fructus of Evodia rutaecarpa and identified as 1-methyl-2-undecyl-4(1H)-quinolone (1). Compound 1 showed a selective inhibition of type B MAO (MAO-B) activity with the IC50 value of 15.3 mum using a substrate kynuramine, but did not inhibit type A MAO (MAO-A) activity. The kinetic analysis using Lineweaver-Burk plots indicated that compound 1 competitively inhibited MAO-B activity with the K-i value of 9.9 mum. The inhibition of MAO-B by compound 1 was found to be irreversible by dialysis of the incubation mixture. These results suggest that compound 1 is a potent irreversible inhibitor of MAO-B, and may regulate catecholamine content in the neurons.

引用

页码：409 / 411

页数：3

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