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. 1996 Jun;40(6):1408–1411. doi: 10.1128/aac.40.6.1408

Potentiation of the antimalarial agent rufigallol.

R W Winter 1, K A Cornell 1, L L Johnson 1, M Ignatushchenko 1, D J Hinrichs 1, M K Riscoe 1
PMCID: PMC163340  PMID: 8726010

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 approximately 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.

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Selected References

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