Antimalarial activity of cedronin.
Cedronin was isolated from Simaba cedron Planchon (Simaroubaceae), a species popularly believed in South America to have antimalarial properties. It was examined for in vitro and in vivo antimalarial activities and for cytotoxicity against KB cells. Experimental results showed that cedronin was active against chloroquine-sensitive and resistant strain, with an IC50 of 0.25 micrograms/ml (0.65 mumol/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 small group of quassinoids with a C19 basic skeleton and shows a rather low cytotoxicity against KB cells (IC50 = 4 micrograms/ml, 10.4 microM) as compared with C20 biologically active quassinoids; however its toxic/therapeutic ratio (10/1.8) remains lower than chloroquine (10/0.5).
Moretti
C
C
Laboratorio de Farmacognosia, ORSTRM-IBBA, La Paz, Bolivia.
Deharo
E
E
Sauvain
M
M
Jardel
C
C
David
P T
PT
Gasquet
M
M
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D002738:Chloroquine / Q000494:pharmacology; D004351:Drug Resistance; D005900:Glaucarubin / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D006801:Humans; D066298:In Vitro Techniques; D007624:KB Cells; D008288:Malaria / Q000188:drug therapy*; D008297:Male; D051379:Mice; D010936:Plant Extracts / Q000494:pharmacology* / Q000627:therapeutic use / Q000633:toxicity; D010961:Plasmodium / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000254:growth & development; D036702:Quassins
D000962:Antimalarials; D010936:Plant Extracts; D036702:Quassins; C090501:cedronolin; C090500:cedronin; D002738:Chloroquine; D005900:Glaucarubin