来自青花椒的单胺氧化酶抑制性香豆素。

Monoamine oxidase inhibitory coumarin from Zanthoxylum schinifolium.

作者信息

Jo Young Su, Huong Dang Thi Lan, Bae KiHwan, Lee Myung Koo, Kim Young Ho

机构信息

College of Pharmacy, Chungnam National University, Daejeon, Korea.

出版信息

Planta Med. 2002 Jan;68(1):84-5. doi: 10.1055/s-2002-20056.

DOI:10.1055/s-2002-20056

PMID:11842339

Abstract

A methanol extract of Zanthoxylum schinifolium stems at a concentration of 250 microg/ml showed potent inhibitory activity against monoamine oxidase (MAO) in a mouse brain. Activity-guided separation and purification of the extract yielded lacinartin (1) as an active coumarin compound. Lacinartin showed significant inhibitory effects on MAO in a dose-dependent manner. The IC(50) value on MAO activity was 9.2 microM. The MAO-A (IC(50) value, 5.7 microM) sensitivity to lacinartin was greater than that of MAO-B (IC(50) value, 28.6 microM). An enzyme kinetic study revealed that lacinartin inhibited MAO activity by a non-competitive mode.

摘要

花椒茎的甲醇提取物在浓度为250微克/毫升时，对小鼠脑中的单胺氧化酶（MAO）显示出强大的抑制活性。通过活性导向的提取物分离和纯化，得到了作为活性香豆素化合物的拉辛那亭（1）。拉辛那亭对MAO具有显著的剂量依赖性抑制作用。MAO活性的IC(50)值为9.2微摩尔。拉辛那亭对MAO-A（IC(50)值为5.7微摩尔）的敏感性高于MAO-B（IC(50)值为28.6微摩尔）。酶动力学研究表明，拉辛那亭以非竞争性模式抑制MAO活性。