1 40 1 Text A resource consisting primarily of words for reading. Examples include books, letters, dissertations, poems, newspapers, articles, archives of mailing lists. Note that facsimiles or images of texts are still of the genre Text. 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 The Dublin Core metadata element set is common to all Omeka records, including items, files, and collections. For more information see, http://dublincore.org/documents/dces/. Title A name given to the resource Inhibition of monoamine oxidase by derivatives of piperine, an alkaloid from the pepper plant Piper nigrum, for possible use in Parkinson's disease. Publisher An entity responsible for making the resource available Bioorganic & medicinal chemistry letters Date A point or period of time associated with an event in the lifecycle of the resource 2012 2012-12 Subject The topic of the resource 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 An entity primarily responsible for making the resource Al-Baghdadi Osamah B; Prater Natalie I; Van der Schyf Cornelis J; Geldenhuys Werner J Description An account of the resource 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 An unambiguous reference to the resource within a given context <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 Information about rights held in and over the resource 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