Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A

In an effort to find potent inhibitors of the protein kinases DYRK1A and CDK1/Cyclin B, a systematic in vitro evaluation of 2,500 plant extracts from New Caledonia and French Guyana was performed. Some extracts were found to strongly inhibit the activity of these kinases. Four aristolactams and one...

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Autores principales: Marti, Guillaume, Eparvier, Véronique, Morleo, Barbara, Ven, Jessica Le, Apel, Cécile, Bodo, Bernard, Amand, Séverine, Dumontet, Vincent, Lozach, Olivier, Meijer, Laurent, Guéritte, Françoise, Litaudon, Marc
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269938/
https://www.ncbi.nlm.nih.gov/pubmed/23467012
http://dx.doi.org/10.3390/molecules18033018
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author Marti, Guillaume
Eparvier, Véronique
Morleo, Barbara
Ven, Jessica Le
Apel, Cécile
Bodo, Bernard
Amand, Séverine
Dumontet, Vincent
Lozach, Olivier
Meijer, Laurent
Guéritte, Françoise
Litaudon, Marc
author_facet Marti, Guillaume
Eparvier, Véronique
Morleo, Barbara
Ven, Jessica Le
Apel, Cécile
Bodo, Bernard
Amand, Séverine
Dumontet, Vincent
Lozach, Olivier
Meijer, Laurent
Guéritte, Françoise
Litaudon, Marc
author_sort Marti, Guillaume
collection PubMed
description In an effort to find potent inhibitors of the protein kinases DYRK1A and CDK1/Cyclin B, a systematic in vitro evaluation of 2,500 plant extracts from New Caledonia and French Guyana was performed. Some extracts were found to strongly inhibit the activity of these kinases. Four aristolactams and one lignan were purified from the ethyl acetate extracts of Oxandra asbeckii and Goniothalamus dumontetii, and eleven aporphine alkaloids were isolated from the alkaloid extracts of Siparuna pachyantha, S. decipiens, S. guianensis and S. poeppigii. Among these compounds, velutinam, aristolactam AIIIA and medioresinol showed submicromolar IC(50) values on DYRK1A.
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spelling pubmed-62699382018-12-20 Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A Marti, Guillaume Eparvier, Véronique Morleo, Barbara Ven, Jessica Le Apel, Cécile Bodo, Bernard Amand, Séverine Dumontet, Vincent Lozach, Olivier Meijer, Laurent Guéritte, Françoise Litaudon, Marc Molecules Article In an effort to find potent inhibitors of the protein kinases DYRK1A and CDK1/Cyclin B, a systematic in vitro evaluation of 2,500 plant extracts from New Caledonia and French Guyana was performed. Some extracts were found to strongly inhibit the activity of these kinases. Four aristolactams and one lignan were purified from the ethyl acetate extracts of Oxandra asbeckii and Goniothalamus dumontetii, and eleven aporphine alkaloids were isolated from the alkaloid extracts of Siparuna pachyantha, S. decipiens, S. guianensis and S. poeppigii. Among these compounds, velutinam, aristolactam AIIIA and medioresinol showed submicromolar IC(50) values on DYRK1A. MDPI 2013-03-06 /pmc/articles/PMC6269938/ /pubmed/23467012 http://dx.doi.org/10.3390/molecules18033018 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Marti, Guillaume
Eparvier, Véronique
Morleo, Barbara
Ven, Jessica Le
Apel, Cécile
Bodo, Bernard
Amand, Séverine
Dumontet, Vincent
Lozach, Olivier
Meijer, Laurent
Guéritte, Françoise
Litaudon, Marc
Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title_full Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title_fullStr Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title_full_unstemmed Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title_short Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
title_sort natural aristolactams and aporphine alkaloids as inhibitors of cdk1/cyclin b and dyrk1a
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269938/
https://www.ncbi.nlm.nih.gov/pubmed/23467012
http://dx.doi.org/10.3390/molecules18033018
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