Plants as a source of antimalarial drugs 5. Activities of <i>Ailanthus altissima</i> stem constituents and of some related quassinoids

Abstract

Abstract Extracts from Ailanthus altissima (Mill.) Swingle Simaroubaceae have been tested for activity against Plasmodium falciparum in vitro and against P. berghei infections in mice. The activity of the chloroformic extract in vitro (IC 50 5 μg ml‐1) and in vivo (ED 50 82.94 mg kg −1 d −1 after oral administration) is due principally to the presence of the quassinoid ailanthone (IC 50 in vitro 0.015μg ml −1 ED 50 in vivo 0.76 mg kg −1 d −1 ). The constituent alkaloids canthin‐6‐one and 1‐methoxycanthin‐6‐one are inactive in vitro . The in vitro and in vivo antimalarial activities of five related quassinoids, viz., ailanthinone, chaparrin, glaucarubol, glaucarubin, glaucarubinone are also reported.