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...

Descripción completa

Detalles Bibliográficos
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
Materias:
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
Descripción
Sumario: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.

Ejemplares similares