Potentiation of the antimalarial agent rufigallol

R. W. Winter, Kenneth A. Cornell, Linda L. Johnson, Marina Ignatushchenko, David J. Hinrichs, Michael K. Riscoe

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Abstract

We have discovered a remarkable synergistic antimalarial interaction between rufigallol and the structurally similar compound exifone. The synergistic effects were produced in chloroquine-susceptible and chloroquine- resistant clones of Plasmodium falciparum. The degree of potentiation as estimated by standard isobolar analysis was ~60-fold for experiments initiated with asynchronous parasites. The most pronounced synergism was observed in experiments with synchronized trophozoite-infected erythrocytes, in which the degree of synergy was at least 300-fold. While the mechanism underlying this drug potentiation remains unresolved, it is hypothesized that rufigallol acts in pro-oxidant fashion to produce oxygen radicals inside parasitized erythrocytes. These radicals would attack exifone, thereby initiating its transformation into a more potent compound, a xanthone.

Original languageEnglish (US)
Pages (from-to)1408-1411
Number of pages4
JournalAntimicrobial agents and chemotherapy
Volume40
Issue number6
StatePublished - Jun 1 1996

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ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Infectious Diseases

Cite this

Winter, R. W., Cornell, K. A., Johnson, L. L., Ignatushchenko, M., Hinrichs, D. J., & Riscoe, M. K. (1996). Potentiation of the antimalarial agent rufigallol. Antimicrobial agents and chemotherapy, 40(6), 1408-1411.