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与吗氯贝胺和临床使用的参考药物相比,黄酮类化合物芦丁和槲皮素的大鼠电药理学图谱表明其具有抗抑郁和/或神经保护作用。

Rat electropharmacograms of the flavonoids rutin and quercetin in comparison to those of moclobemide and clinically used reference drugs suggest antidepressive and/or neuroprotective action.

作者信息

Dimpfel Wilfried

机构信息

Justus-Liebig-University Giessen, c/o NeuroCode AG, Sportparkstr. 9, D 35578 Wetzlar, Germany.

出版信息

Phytomedicine. 2009 Apr;16(4):287-94. doi: 10.1016/j.phymed.2009.02.005.

DOI:10.1016/j.phymed.2009.02.005
PMID:19303757
Abstract

In order to be able to test single constituents of herbal plant extracts with respect to possible clinical usefulness, the model of local field potential analysis leading to the so-called electropharmacogram has been successfully used in rats to classify the effects of theanine and theogallin in the past. The present investigation aims at the prediction of efficacy and possible mechanisms of action of rutin and quercetin. Adult rats (day-night converted) were instrumented with four bipolar concentric electrodes into the frontal cortex, hippocampus, striatum and reticular formation. Field potentials were recorded during a pre-drug reference period of 45 min followed by oral administration of the particular test compound and 4h recording thereafter. Data were transmitted wirelessly to the computer for spectral frequency analysis. Rutin (5-80 mg/kg) as well as quercetin (5-40 mg/kg orally) produced similar electropharmacograms with dose dependent decreases of spectral alpha2 and beta1 frequencies within all brain areas. Peak effects were reached 4h after administration. The pattern of changes approached that obtained after 2.5mg/kg of moclobemide during the first hour as revealed by discriminant analysis in comparison to a large matrix of other drugs with known clinical indications. Data suggest antidepressant capabilities for rutin and quercetin with inhibition of monoamino oxidase at least as part of the mechanism of action. Both compounds should be tested clinically in patients with symptoms of depression.

摘要

为了能够测试草药植物提取物的单一成分的潜在临床效用,过去在大鼠中成功使用了导致所谓电药理图的局部场电位分析模型来对茶氨酸和没食子儿茶素的作用进行分类。本研究旨在预测芦丁和槲皮素的疗效及可能的作用机制。成年大鼠(昼夜颠倒)在额叶皮质、海马体、纹状体和网状结构中植入四个双极同心电极。在给药前45分钟的参考期内记录场电位,随后口服特定测试化合物,并在之后4小时进行记录。数据通过无线传输至计算机进行频谱频率分析。芦丁(5 - 80毫克/千克)以及槲皮素(口服5 - 40毫克/千克)产生了相似的电药理图,所有脑区的频谱α2和β1频率均呈剂量依赖性降低。给药后4小时达到峰值效应。与大量具有已知临床适应症的其他药物的矩阵进行判别分析显示,变化模式接近在第一小时给予2.5毫克/千克吗氯贝胺后所获得的模式。数据表明芦丁和槲皮素具有抗抑郁能力,至少部分作用机制是抑制单胺氧化酶。这两种化合物均应在有抑郁症状的患者中进行临床测试。

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