Plants as sources of antimalarial drugs, Part 4: Activity of Brucea javanica fruits against chloroquine-resistant Plasmodium falciparum in vitro and against Plasmodium berghei in vivo.
Extracts of Brucea javanica fruit have been prepared and monitored for their in vitro and in vivo antiplasmodial activities. The antimalarial activity of the fruit was found to be attributable to its quassinoid constituents. Nine of the quassinoids possessed in vitro IC50 values between 0.046-0.0008 microgram/ml against the chloroquine resistant Plasmodium falciparum strain (Kl) tested. The two quassinoid glycosides tested were considerably less active in vitro than the aglycones. Four quassinoids were found to possess activity in vivo against Plasmodium berghei infections in mice after oral dosing. All five quassinoids tested in vivo showed some toxicity.
O'Neill
M J
MJ
Bray
D H
DH
Boardman
P
P
Chan
K L
KL
Phillipson
J D
JD
Warhurst
D C
DC
Peters
W
W
D000818:Animals; D000962:Antimalarials / Q000302:isolation & purification / Q000494:pharmacology* / Q000627:therapeutic use; D000440:Butanols; D002725:Chloroform; D002738:Chloroquine / Q000494:pharmacology*; D004351:Drug Resistance; D005900:Glaucarubin / Q000031:analogs & derivatives / Q000302:isolation & purification / Q000494:pharmacology; D008288:Malaria / Q000188:drug therapy*; D008297:Male; D051379:Mice; D010936:Plant Extracts / Q000302:isolation & purification / Q000494:pharmacology / Q000627:therapeutic use; D010946:Plants, Medicinal / Q000032:analysis*; D010962:Plasmodium berghei; D010963:Plasmodium falciparum / Q000187:drug effects*
D000962:Antimalarials; D000440:Butanols; D010936:Plant Extracts; D002725:Chloroform; D002738:Chloroquine; D005900:Glaucarubin