A potent anti-inflammatory activity was detected from methanol extracts prepared from roots of Rhodiola sacra. In the preliminary test, methanol extracts from the roots of R. sacra could potently attenuate histological change in the lung tissue after lipopolysaccharide (LPS)-treated inflammatory stimulation. The active compound has been identified as 3-(3,4-dihydroxy-phenyl)-acrylic acid phenethyl ester (caffeic acid phenethyl ester, CAPE). In vivo study on protective effect of R. sacra CAPE against inflammatory response by endotoxin shock in the LPS-induced inflammatory mice showed significantly attenuated the intravenous LPS-induced increase in plasma TNF-alpha and IL-1 beta concentration. R. sacra CAPE significantly inhibited LPS-induced nuclear transcription factor-kappa B (NF-kappa B) activation. It also down-regulates enhanced matrix metalloproteinase-9 (MMP-9) activity triggered by LPS in mouse lung. In the present study, the results indicate that the intake of R sacra CAPE could provide health benefits, reducing the magnitude of the inflammatory process triggered by endotoxin shock and the production of inflammatory mediators. (C) 2008 Elsevier Ltd. All rights reserved.