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

作者：Farokhi Fereshteh; Grellier Philippe; Clement Monique; Roussakis Christos; Loiseau Philippe M; Genin Seward Emilie; Kornprobst Jean Michel; Barnathan Gilles^*; Wielgosz Collin Gaetane

来源：Marine Drugs, 2013, 11(4): 1304-1315.

DOI：10.3390/md11041304

• Axinyssa
• marine sponge glycolipids
• glycosphingolipids
• antimalarial activity
• cytotoxicity

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 mu M against a chloroquine-resistant strain of Plasmodium falciparum. They were identified as homologous beta-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 beta anomeric configuration may be suitable in searching for new antimalarial drugs.

• 出版日期2013-4