Antiplasmodial activity of aspidosperma indole alkaloids. |
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Authors: | A C Mitaine-Offer M Sauvain A Valentin J Callapa M Mallié M Zèches-Hanrot |
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Institution: | Laboratoire de Pharmacognosie, Faculté de Pharmacie, Université de Reims Champagne-Ardenne, France. acoffer@u-bourgogne.fr |
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Abstract: | 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 microM. 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 microM. 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. |
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