Potentiation of the antimalarial agent rufigallol.

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.

authors

Winter RW,Cornell KA,Johnson LL,Ignatushchenko M,Hinrichs DJ,Riscoe MK

doi

10.1128/AAC.40.6.1408

subject

Has Abstract

pub_date

1996-06-01 00:00:00

pages

1408-11

issue

6

eissn

0066-4804

issn

1098-6596

journal_volume

40

pub_type

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