A new triterpenoid glycoside (1) and 15 known compounds (2-16) were isolated from the whole plants of Gueldenstaedtia verna. The new compound (1) was identified as complogenin 22-O--d-glucopyranoside by extensive spectroscopic techniques including 1D (H-1 and C-13) and 2D NMR experiments (HSQC, HMBC and NOESY), HR-DART-MS and chemical methods. Most of the isolates were evaluated for their inhibitory activities on LPS-induced NO production in RAW 264.7 cells. The inhibitory effects of the active compounds, sulphuretin (8) and (22E,24S)-5,8-epidioxy-24-methyl-cholesta-6,9(11),22-trien-3-ol (13), on the production of pro-inflammatory mediators (including IL-6, IL1 and PGE(2)) were further estimated in vitro by ELISA in RAW 264.7 macrophages. [GRAPHICS] .