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Bioorg Med Chem Lett. 2012 Dec 1;22(23):7183-8. doi: 10.1016/j.bmcl.2012.09.056. Epub 2012 Sep 23.

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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1
Neurotherapeutics Emphasis Group, Department of Pharmaceutical Sciences, Northeast Ohio Medical University, College of Pharmacy, Rootstown, OH 44272, USA.

Abstract

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 IC(50) 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 μM 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.

PMID:
23102654
DOI:
10.1016/j.bmcl.2012.09.056
[Indexed for MEDLINE]

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