Title: Natural Aristolactams and Aporphine Alkaloids as Inhibitors of CDK1/Cyclin B and DYRK1A.
Authors: 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
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.
Subjects: APORPHINE; ALKALOIDS; PROTEIN kinases; PLANT extracts; ETHYL acetate; CYCLINS
Publication: Molecules, 2013, Vol 18, Issue 3, p3018
ISSN: 1420-3049
Publication type: Academic Journal
DOI: 10.3390/molecules18033018

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