Potentiation of the antimalarial activity of qinghaosu by methoxylated flavones.
Interaction between the flavones casticin and artemetin and the antimalarial activity of chloroquine and qinghaosu (QHS) was examined using an in vitro growth assay based on [3H]hypoxanthine incorporation in synchronized cultures of a cloned line of Plasmodium falciparum. Casticin, and to a lesser extent artemetin, selectively enhanced the inhibition of growth by QHS, but had little effect on the activity of chloroquine. The findings suggest that flavones indigenous to Artemisia annua, from which QHS is isolated, might significantly alter the clinical potential of this novel antimalarial drug in the treatment of chloroquine-resistant malaria.
Elford
B C
BC
Clinical Research Centre, Harrow, Middlesex, UK.
Roberts
M F
MF
Phillipson
J D
JD
Wilson
R J
RJ
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins; D002999:Clone Cells; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D005419:Flavonoids / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development; D012717:Sesquiterpenes / Q000494:pharmacology*
D000962:Antimalarials; D037621:Artemisinins; D005419:Flavonoids; D012717:Sesquiterpenes; C054132:artemetin; C054133:casticin; C031327:artemisinin