Three new indole alkaloid derivatives, fissindoalkas A -C (1-3) together with one known biogenetically related polysubstituted indole alkaloid (4) were isolated from the roots of Fissistigma oldhamii (Hemsl.) Merr. The structures of compounds 1-4 were elucidated using comprehensive spectroscopic methods. The inhibitory activities of compounds 1-4 against nitric oxide (NO) production induced by lipopolysaccharide (LPS) were evaluated in vitro using mouse macrophage RAW264.7 cells. Compounds 2 and 3 showed potent inhibitory activities on NO production with IC50 values of 2.52 +/- 0.18 and 2.33 +/- 0.16 mu M. These results indicate that the discovery of indole alkaloid derivatives, from the roots of F. oldhamii, which show significant anti-inflammatory properties, could be of great importance to the research and for the development of novel natural antiinflammatory agents.