Cedronin was isolated from Simaba cedron Planchon (Simaroubaceae), a s
pecies popularly believed in South America to have antimalarial proper
ties. It was examined for in vitro and in vivo antimalarial activities
and for cytotoxicity against KB cells. Experimental results showed th
at cedronin was active against chloroquine-sensitive and resistant str
ain, with an IC50 of 0.25 mu g/ml (0.65 mu mol/ml). It was also found
to be active in vivo against Plasmodium vinkei with an IC50 of 1.8 mg/
kg (4.7 nM/kg) in the classic 4-day test. Cedronin belongs to the smal
l group of quassinoids with a C-19 basic skeleton and shows a rather l
ow cytotoxicity against KB cells (IC50 = 4 mu g/ml, 10.4 mu M) as comp
ared with C-20 biologically active quassinoids; however its toxic/ther
apeutic ratio (10/1.8) remains lower than chloroquine (10/0.5).