title: Natural aristolactams and aporphine alkaloids as inhibitors of CDK1/cyclin B and DYRK1A.
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.
authors: Centre de Recherche de Gif, Institut de Chimie des Substances Naturelles, CNRS, 1 avenue de la Terrasse, 91198 Gif-sur-Yvette Cedex, France. Guillaume.Marti@icsn.cnrs-gif.fr
authors: Guillaume
authors: G
authors: Marti
authors: Véronique
authors: V
authors: Eparvier
authors: Barbara
authors: B
authors: Morleo
authors: Jessica
authors: J
authors: Le Ven
authors: Cécile
authors: C
authors: Apel
authors: Bernard
authors: B
authors: Bodo
authors: Séverine
authors: S
authors: Amand
authors: Vincent
authors: V
authors: Dumontet
authors: Olivier
authors: O
authors: Lozach
authors: Laurent
authors: L
authors: Meijer
authors: Françoise
authors: F
authors: Guéritte
authors: Marc
authors: M
authors: Litaudon
mesh_terms: D001060:Aporphines / Q000737:chemistry / Q000494:pharmacology*; D016203:CDC2 Protein Kinase / Q000037:antagonists & inhibitors*; D019926:Cyclin B / Q000037:antagonists & inhibitors*; D026121:Indole Alkaloids / Q000737:chemistry / Q000494:pharmacology*; D007769:Lactams / Q000737:chemistry / Q000494:pharmacology*; D019906:Nuclear Magnetic Resonance, Biomolecular; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors*; D000097603:Dyrk Kinases
chemical_list: D001060:Aporphines; D016203:CDC2 Protein Kinase; D019926:Cyclin B; D026121:Indole Alkaloids; D007769:Lactams; D010936:Plant Extracts; D017346:Protein Serine-Threonine Kinases; D011505:Protein-Tyrosine Kinases; D000097603:Dyrk Kinases; C457228:aristolactam A; C487927:aristolactam BII