Phytochemical investigation of the whole herbs of Euphorbia humifusa Willd. led to the isolation of two unde-scribed triterpenoids, (3S,5R,7R,8S,10S,13S,14S,17R,18R,21R)-7 alpha,8 alpha-epoxyfern-9(11)-en-3 beta-ol (1) and (3R, 7R,8S,9S,13S,14S,17R,18R,21R)-7 alpha,8 alpha-epoxyadian-5(10)-en-3 alpha-ol (2), along with three known compounds 3-5. Their structures were elucidated by spectroscopic analysis and optical rotation calculations. All isolates were screened for their anti-inflammatory activity by evaluating their inhibitory effect on NO production in LPS-stimulated RAW 264.7 macrophage cells. Compounds 1, 2, 4, and 5 showed potent inhibitory effects on LPS-induced NO production with IC50 values ranging from 18.88 to 31.77 mu M.