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Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A.
Marti, Guillaume; Eparvier, Véronique; Morleo, Barbara; Le Ven, Jessica; Apel, Cécile; Bodo, Bernard; Amand, Séverine; Dumontet, Vincent; Lozach, Olivier; Meijer, Laurent; Guéritte, Françoise; Litaudon, Marc.
Afiliação
  • Marti G; Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France. Guillaume.Marti@icsn.cnrs-gif.fr
Molecules ; 18(3): 3018-27, 2013 Mar 06.
Article em En | MEDLINE | ID: mdl-23467012
ABSTRACT
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 IC50 values on DYRK1A.
Assuntos

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Aporfinas / Proteínas Tirosina Quinases / Extratos Vegetais / Proteína Quinase CDC2 / Proteínas Serina-Treonina Quinases / Ciclina B / Alcaloides Indólicos / Lactamas Idioma: En Ano de publicação: 2013 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Aporfinas / Proteínas Tirosina Quinases / Extratos Vegetais / Proteína Quinase CDC2 / Proteínas Serina-Treonina Quinases / Ciclina B / Alcaloides Indólicos / Lactamas Idioma: En Ano de publicação: 2013 Tipo de documento: Article