Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease
Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease
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DOI：
10.1016/j.bmcl.2012.09.056
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发表时间：
2012-12-01
影响因子：
2.7
通讯作者：
Geldenhuys, Werner J.
中科院分区：
文献类型：
--
作者：
Al-Baghdadi, Osamah B.;Prater, Natalie I.;Geldenhuys, Werner J.
用单胺氧化酶A和B法筛选了胡椒碱和抗癫痫药的一系列化合物。黑胡椒碱是一种来自黑胡椒和白色胡椒的生物碱。已显示，马槟榔碱具有广泛的活性，包括MAO抑制活性。发现两种试验筛选试验的z因子均大于0.8。值得注意的是，测试的化合物对MAO-B具有选择性，最有效的化合物具有498 nM的IC 50。为了估计血脑屏障（BBB）的渗透性，我们使用了PAMPA测定，这表明化合物可能穿透BBB。荧光牛血清白蛋白（BSA）高通量筛选（HTS）结合试验显示，胡椒碱的亲和力为8 μ M，与其他测试化合物的结合更温和。总之，这里描述的数据可能有助于深入了解缺乏MAO-A活性的选择性MAO-B抑制化合物的设计。(C)2012爱思唯尔有限公司保留所有权利。
A series of compounds related to piperine and antiepilepsirine was screened in a monoamine oxidase A and B assay. Piperine is an alkaloid from the source plant of both black and white pepper grains, Piper nigrum. Piperine has been shown to have a wide range of activity, including MAO inhibitory activity. The z-factor for the screening assay was found to be greater than 0.8 for both assays. Notably, the compounds tested were selective towards MAO-B, with the most potent compound having an IC50 of 498 nM. To estimate blood-brain barrier (BBB) permeability, we used a PAMPA assay, which suggested that the compounds are likely to penetrate the BBB. A fluorescent bovine serum albumin (BSA) high-throughput screening (HTS) binding assay showed an affinity of 8 mu M for piperine, with more modest binding for other test compounds. Taken together, the data described here may be useful in gaining insight towards the design of selective MAO-B inhibitory compounds devoid of MAO-A activity. (C) 2012 Elsevier Ltd. All rights reserved.