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 language||English (US)|
|Number of pages||4|
|Journal||Antimicrobial agents and chemotherapy|
|State||Published - Jun 1 1996|
ASJC Scopus subject areas
- Pharmacology (medical)
- Infectious Diseases