Isolation of bioactive aporphinoid alkaloids in Oxandra asbecki (Annonaceae)

• Published in: Planta Medica
• Main Authors: Le Ven, J, Eparvier, V, Litaudon, M, Gueritte, F
• Format: Conference Proceeding
• Language: English
• Published: 24.08.2010
• ISSN: 0032-0943; 1439-0221
• DOI: 10.1055/s-0030-1264677

Since prehistoric times, humans beneficially used natural resources for their daylife needs. Plants are able to synthesize complex molecules and consequently have a unique chemical diversity. This is a source of inspiration for new drugs discovery. Dyrk1A kinase is a target used in research on Alzheimer's disease. Inhibition of this kinase is associated with treating symptoms of this disease [1,2]. In France, the annual number of new cases is 230 000. The prevalence is expected to double in industrialized countries and quadruple in developing countries in the coming decades. The development of a better diagnosis and treatment is essential. The Annonaceae is a large family of tropical plants that have been investigated intensively. There exist 38 species in Oxandra genus and Oxandra asbecki species in Venezuela and in primary forests of French Guiana. To the aim of discovering new bioactive plants from French Guiana, Oxandra asbecki was selected for phytochemical study because of its potent inhibition of DyrK1A kinase. Bioassay-directed fractionation of the ethyl acetate extract provided three bioactive alkaloids. We isolated three aporphinoid alkaloids and show for the first time an strong activity (with micromolar IC50) of Velutamin under two kinase: CDK1 and DyrK1A, and activity of Aristolactam AII on DyrK1A kinase. References: 1. Lee, V.M-Y., et al. (2004). Trends in neurosciences 27. 2. Nam Doo Kim, N.D., et al. (2006) Biol. Med. Chem. Lett. 16, 3772–3776.