Three triterpenes were isolated from Diospyros leucomelas and identified as betulin, betulinic acid, and ursolic acid. They showed anti-inflammatory activity in the carrageenan and serotonin paw edema tests and TPA and EPP ear edema tests. The blockade of their effects by progesterone, actinomycin D, and cycloheximide has served to determine the mechanism of action in relationship with that of glucocorticoids. Betulinic acid was the most affected and therefore a mode of action similar to these drugs may be postulated for it.