In our continuing search for biologically active natural product(s) of plant origin, Buddleja saligna, a South African medicinal plant, was screened in line with its traditional use for antidiabetic (yeast alpha glucosidase inhibitory) and antiplasmodial (against a chloroquine sensitive strain of Plasmodium falciparum (NF54)) activities. The hexane fraction showed the most promising activity with regards to its antidiabetic (IC50 ¼ 260 ± 0.112 mg/ml) and antiplasmodial (IC50 ¼ 8.5 ± 1.6 mg/ml) activities. Using activity guided fractionation three known terpenoids (betulonic acid, betulone and spinasterol) were isolated from this species for the first time. The compounds displayed varying levels of biological activities (antidiabetic: 27.31 mg/ml - IC50 - 5.6 mg/ml; antiplasmodial: 14 mg/ml - IC50 - 2 mg/ml) with very minimal toxicity.