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

Molecules

Guillaume Marti²  Véronique Eparvier²  Barbara Morleo²  Jessica Le Ven²  Cຜile Apel²  Bernard Bodo³  Séverine Amand³  Vincent Dumontet²  Olivier Lozach¹  Laurent Meijer¹  Françoise Guéritte² 

[1] Protein Phosphorylation & Human Disease’ group, CNRS, Station Biologique, Place G. Teissier, Roscoff 29680, France; E-Mails:;Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France; E-Mails:;Muséum National d’Histoire Naturelle, UMR 7245 CNRS, 63 rue Buffon, Paris 75005, France; E-Mails:

关键词: Oxandra asbeckii;    Goniothalamus dumontetii;    Siparuna spp.;    aporphinoids and aristolactams;    kinases inhibitors;   

DOI  :  10.3390/molecules18033018

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.