By means of activity-directed chromatographic fractionation using the 12-O-tetradecanoylphorbol acetate (TPA)-induced edema test, two saikosaponins were isolated from the MeOH extract of Heteromorpha trifoliata leaves. They were identified as 16 beta, 23-dihydroxy-13,28-epoxyolean-11-en-3 beta-yl-[beta-D-glucopyranosyl (1-->2)]-[beta-D-glucopyranosyl (1-->3)]-beta-D-fucopyranoside [1] and 16 beta, 23,28-trihydroxy-11 alpha-methoxyolean-12-en-3 beta-yl-[beta-D-glucopyranosyl (1-->2)]-[beta-D-glucopyranosyl (1-->3) [beta-D-fucopyranoside [2]. Compound 1 showed activity in the TPA and ethylphenylpropiolate (EPP) mouse ear edema and the serotonin paw edema tests, whereas compound 2 was active only in the mouse ear edema model. Both substances had only a slight effect against a carrageenan paw edema model. The anti-inflammatory action of compound 1 was notably decreased by the mRNA and protein synthesis inhibitors actinomycin D and cycloheximide.