Abstract: 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.
Keywords: Axinyssa; marine sponge glycolipids; glycosphingolipids; antimalarial activity; cytotoxicity
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Farokhi, F.; Grellier, P.; Clément, M.; Roussakis, C.; Loiseau, P.M.; Genin-Seward, E.; Kornprobst, J.-M.; Barnathan, G.; Wielgosz-Collin, G. Antimalarial Activity of Axidjiferosides, New β-Galactosylceramides from the African Sponge Axinyssa djiferi. Mar. Drugs 2013, 11, 1304-1315.
Farokhi F, Grellier P, Clément M, Roussakis C, Loiseau PM, Genin-Seward E, Kornprobst J-M, Barnathan G, Wielgosz-Collin G. Antimalarial Activity of Axidjiferosides, New β-Galactosylceramides from the African Sponge Axinyssa djiferi. Marine Drugs. 2013; 11(4):1304-1315.
Farokhi, Fereshteh; Grellier, Philippe; Clément, Monique; Roussakis, Christos; Loiseau, Philippe M.; Genin-Seward, Emilie; Kornprobst, Jean-Michel; Barnathan, Gilles; Wielgosz-Collin, Gaëtane. 2013. "Antimalarial Activity of Axidjiferosides, New β-Galactosylceramides from the African Sponge Axinyssa djiferi." Mar. Drugs 11, no. 4: 1304-1315.