Antimalarial Activity of Axidjiferosides, New β-Galactosylceramides from the African Sponge Axinyssa djiferi

• Main Authors: Gilles Barnathan, Gaëtane Wielgosz-Collin, Emilie Genin-Seward, Jean-Michel Kornprobst, Philippe M. Loiseau, Philippe Grellier, Monique Clément, Christos Roussakis, Fereshteh Farokhi
• Format: Article
• Language: English
• Published: MDPI AG 2013-04-01
• Series: Marine Drugs
• Subjects: Axinyssa; marine sponge glycolipids; glycosphingolipids; antimalarial activity; cytotoxicity
• Online Access: http://www.mdpi.com/1660-3397/11/4/1304

The marine sponge, Axinyssa djiferi, collected on mangrove tree roots in Senegal, was investigated for glycolipids. A mixture containing new glycosphingolipids, named axidjiferoside-A, -B and -C, accounted for 0.07% of sponge biomass (dry weight) and for 2.16% of total lipids. It showed a significant antimalarial activity, with a 50% inhibitory concentration (IC50) of 0.53 ± 0.2 μM against a chloroquine-resistant strain of Plasmodium falciparum. They were identified as homologous β-galactopyranosylceramides composed of 2-amino-(6E)-octadec-6-en-1,3,4-triol, and the major one, axidjiferoside-A (around 60%), contained 2-hydroxytetracosanoic acid. Cytotoxicity was studied in vitro on human cancer cell lines (multiple myeloma, colorectal adenocarcinoma, glioblastoma and two lung cancer NSCLC-N6 and A549). Results of this investigation showed that axidjiferosides are of interest, because they proved a good antiplasmodial activity, with only a low cytotoxicity against various human cell lines and no significant antitrypanosomal and antileishmanial activity. Thus, it seems that galactosylceramides with a β anomeric configuration may be suitable in searching for new antimalarial drugs.