Inhibitory activity of Filipendula ulmaria constituents on recombinant human histidine decarboxylase
Inhibitory activity of Filipendula ulmaria constituents on recombinant human histidine decarboxylase
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DOI：
10.1016/j.foodchem.2012.10.074
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发表时间：
2013-06-01
期刊：
影响因子：
8.8
通讯作者：
Ueno, Hiroshi
中科院分区：
文献类型：
--
作者：
Nitta, Yoko;Kikuzaki, Hiroe;Ueno, Hiroshi
组氨酸脱羧酶（HDC）催化组胺（一种生物活性胺）的形成。控制HDC活性的药物有益于治疗组胺介导的症状，如过敏和胃溃疡。我们从绣线菊（Filipendula ulmaria）花瓣的乙酸乙酯提取物中寻找HDC的抑制剂。Rugosin D、Rugosin A、Rugosin A甲酯（一种新化合物）和tellimagrandin II是主要成分;这4种鞣花单宁表现出非竞争性抑制类型，Ki值约为0.35-1 μ M。这些K-i值几乎等于组氨酸甲酯（K-i = 0.46 μ M），现有的底物类似物抑制剂。我们的研究结果表明，食品中含有有效的HOC抑制剂，这些活性食品成分可能是有用的设计临床上可用的HDC抑制剂。(C)2012爱思唯尔有限公司保留所有权利。
Histidine decarboxylase (HDC) catalyses the formation of histamine, a bioactive amine. Agents that control HDC activity are beneficial for treating histamine-mediated symptoms, such as allergies and stomach ulceration. We searched for inhibitors of HDC from the ethyl acetate extract of the petal of Filipendula ulmaria, also called meadowsweet. Rugosin D, rugosin A, rugosin A methyl ester (a novel compound), and tellimagrandin II were the main components; these 4 ellagitannins exhibited a non-competitive type of inhibition, with K-i values of approximately 0.35-1 mu M. These K-i values are nearly equal to that of histidine methyl ester (K-i = 0.46 mu M), an existing substrate analogue inhibitor. Our results show that food products contain potent HOC inhibitors and that these active food constituents might be useful for designing clinically available HDC inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.