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Molecules 2013, 18(3), 3018-3027; doi:10.3390/molecules18033018
Article

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

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Received: 29 January 2013 / Revised: 28 February 2013 / Accepted: 1 March 2013 / Published: 6 March 2013
(This article belongs to the Section Metabolites)
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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 Oxandra asbeckii; Goniothalamus dumontetii; Siparuna spp.; aporphinoids and aristolactams; kinases inhibitors
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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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.

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