Antiplasmodial activity of Aspidosperma indole alkaloids

  • Mitaine-Offer A
  • Sauvain M
  • Valentin A
 et al. 
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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 IC50after 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.

Author-supplied keywords

  • A. megalocarpon
  • Antiplasmodial activity
  • Aspidosperma pyrifolium
  • Aspidospermane alkaloids
  • Plasmodium falciparum

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Authors

  • A. C. Mitaine-Offer

  • M. Sauvain

  • A. Valentin

  • J. Callapa

  • M. Mallié

  • M. Zches-Hanrot

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