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Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A
Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France
Muséum National d'Histoire Naturelle, UMR 7245 CNRS, 63 rue Buffon, Paris 75005, France
Protein Phosphorylation & Human Disease' group, CNRS, Station Biologique, Place G. Teissier, Roscoff 29680, France
ManRos Therapeutics, Centre de Perharidy, Roscoff 29680, France
* Author to whom correspondence should be addressed.
Received: 29 January 2013; in revised form: 28 February 2013 / Accepted: 1 March 2013 / Published: 6 March 2013
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.
Keywords: Oxandra asbeckii; Goniothalamus dumontetii; Siparuna spp.; aporphinoids and aristolactams; kinases inhibitors
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Marti, G.; Eparvier, V.; Morleo, B.; Ven, J.L.; Apel, C.; Bodo, B.; Amand, S.; Dumontet, V.; Lozach, O.; Meijer, L.; Guéritte, F.; Litaudon, M. Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A. Molecules 2013, 18, 3018-3027.
Marti G, Eparvier V, Morleo B, Ven JL, Apel C, Bodo B, Amand S, Dumontet V, Lozach O, Meijer L, Guéritte F, Litaudon M. Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A. Molecules. 2013; 18(3):3018-3027.
Marti, Guillaume; Eparvier, Véronique; Morleo, Barbara; Ven, Jessica L.; Apel, Cécile; Bodo, Bernard; Amand, Séverine; Dumontet, Vincent; Lozach, Olivier; Meijer, Laurent; Guéritte, Françoise; Litaudon, Marc. 2013. "Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A." Molecules 18, no. 3: 3018-3027.