The antiplasmodial activity of twelve alkaloids with an aspidospermane skeleton was estimated in vitro on chloroquine-resistant and sensitive strains of Plasmodium falciparum. Seven tetracyclic alkaloids possessing a free ethyl chain such aspidospermine, showed IC50 after incubation for 72 h between 3.2 and 15.4 μM. Moreover, four pentacyclic alkaloids with ethyl chain included in a tetrahydrofuran, such haplocine, showed a reduced activity, with IC50, after 72 h, between 22.6 and 52.6 μM. According to these results, a chloroquine-potentiating experiment was also performed with two of the most active compounds. Isobolograms were obtained and demonstrated a synergic effect of N-formyl-aspidospermidine and aspidospermine when associated with chloroquine. The cytotoxicity and the selectivity index of some alkaloids were also estimated.
CITATION STYLE
Mitaine-Offer, A. C., Sauvain, M., Valentin, A., Callapa, J., Mallié, M., & Zches-Hanrot, M. (2002). Antiplasmodial activity of Aspidosperma indole alkaloids. Phytomedicine, 9(2), 142–145. https://doi.org/10.1078/0944-7113-00094
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