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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 IC 50 values of 2.52 ± 0.18 and 2.33 ± 0.16 μM. 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 anti-inflammatory agents. [Display omitted] [ABSTRACT FROM AUTHOR]