20,10-olide (4a), have been isolated from the leaves of Croton gratissimus. The acetyl derivatives of 8 and 4a were evaluated against a chloroquine-sensitive strain of Plasmodium falciparum (D10).Croton gratissimus Burch. (C. zambesicus Mull. Arg.; C. microbotryus Pax.) (Euphorbiaceae) grows on stony hillsides as a semideciduous tree species throughout much of the warmer and drier regions from South Africa, northeastwards, to the horn of Africa. The leaves of this plant are ground with goat fat and those of two other Croton species, the resulting paste is heated on coals, and the fumes are inhaled as a cure for insomnia. 1 A tea made from the leaves is taken for coughs in Botswana. 2 Watt and Breyer-Brandwijk 3 documented C. gratissimus as a remedy for fever, for treating bleeding gums and eye disorders, and as an ingredient used to "smoke" rheumatic patients. In South Africa, the leaves are dried and smoked for influenza, colds, and fevers. 4 The traditional use of this species for treating fevers, intermittent or otherwise, indicates its likely application as an antimalarial, since it is employed as such within the malaria endemic region of southern Africa. In Nigeria, bark infusions of the species (as C. zambesicus) are reported to treat malaria. 5 Accordingly, crude dichloromethane extracts of South African leaves of C. gratissimus have previously been investigated for antiplasmodial activity in vitro and shown to have an IC 50 value of 3.5 μg/mL; 6 the constituent(s) responsible were not identified. The stem bark of C. gratissimus has been reported to yield four cembranoids, namely, (+)-(1R*,2S*,7S*,8S*,12R*)-7,8-epoxy-2,12-cyclocembra-3E,10Z-dien-20,10-olide, (+)-(1R*,10R*)c e m b r a -2 E , 4 E , 7 E , 1 1 Z -t e t r a e n -2 0 , 1 0 -o l i d e , (+)-(1R*,4S*,10R*)-4-hydroxycembra-2E,7E,11Z-trien-20,10-olide (4a), and (−)-(1R*,4R*,10R*)-4-hydroxycembra-2E,7E,11Z-trien-20,10-olide, in addition to lupeol, 4(15)eudesmene-1β,6α-diol, and α-glutinol.7