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Text
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URL Address
<a href="http://doi.org/10.1016/j.bmcl.2012.09.056" target="_blank" rel="noreferrer noopener">http://doi.org/10.1016/j.bmcl.2012.09.056</a>
Pages
7183–7188
Issue
23
Volume
22
Dublin Core
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Title
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Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease.
Publisher
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Bioorganic & medicinal chemistry letters
Date
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2012
2012-12
Subject
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Alkaloids/*chemistry/isolation & purification/pharmacology; Animals; Benzodioxoles/*chemistry/isolation & purification/pharmacology; Binding Sites; Blood-Brain Barrier/drug effects; Bovine/metabolism; Cattle; Humans; Hydrogen Bonding; Molecular Docking Simulation; Monoamine Oxidase Inhibitors/*chemistry/isolation & purification/pharmacology; Monoamine Oxidase/*chemistry/metabolism; Parkinson Disease/metabolism/pathology; Piper nigrum/*chemistry; Piperidines/*chemistry/isolation & purification/pharmacology; Polyunsaturated Alkamides/*chemistry/isolation & purification/pharmacology; Protein Binding; Protein Structure; Serum Albumin; Tertiary
Creator
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Al-Baghdadi Osamah B; Prater Natalie I; Van der Schyf Cornelis J; Geldenhuys Werner J
Description
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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 muM 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.
Identifier
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<a href="http://doi.org/10.1016/j.bmcl.2012.09.056" target="_blank" rel="noreferrer noopener">10.1016/j.bmcl.2012.09.056</a>
Rights
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Article information provided for research and reference use only. All rights are retained by the journal listed under publisher and/or the creator(s).
2012
Al-Baghdadi Osamah B
Alkaloids/*chemistry/isolation & purification/pharmacology
Animals
Benzodioxoles/*chemistry/isolation & purification/pharmacology
Binding Sites
Bioorganic & medicinal chemistry letters
Blood-Brain Barrier/drug effects
Bovine/metabolism
Cattle
Geldenhuys Werner J
Humans
Hydrogen Bonding
Molecular Docking Simulation
Monoamine Oxidase Inhibitors/*chemistry/isolation & purification/pharmacology
Monoamine Oxidase/*chemistry/metabolism
Parkinson Disease/metabolism/pathology
Piper nigrum/*chemistry
Piperidines/*chemistry/isolation & purification/pharmacology
Polyunsaturated Alkamides/*chemistry/isolation & purification/pharmacology
Prater Natalie I
Protein Binding
Protein Structure
Serum Albumin
Tertiary
Van der Schyf Cornelis J