Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A. - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue Molecules Année : 2013

Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A.

Guillaume Marti
Barbara Morleo
  • Fonction : Auteur
Jessica Le Ven
  • Fonction : Auteur
Bernard Bodo
  • Fonction : Auteur
Séverine Amand
  • Fonction : Auteur
  • PersonId : 1267597
Olivier Lozach
Laurent Meijer
  • Fonction : Auteur
Marc Litaudon

Résumé

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.

Domaines

Chimie organique

Dates et versions

hal-00856752 , version 1 (02-09-2013)

Identifiants

Citer

Guillaume Marti, Véronique Eparvier, Barbara Morleo, Jessica Le Ven, Cécile Apel, et al.. Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A.. Molecules, 2013, 18 (3), pp.3018-27. ⟨10.3390/molecules18033018⟩. ⟨hal-00856752⟩
55 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More