Eight lignans (1-8) and two macrolides (9-10) were isolated from the CHCl 3 -soluble fraction of Houttuynia cordata Thumb (Saururaceae). Structures of isolates were elucidated by extensive spectroscopic methods. Fatty acid-derived macrolides (9-10) have rarely been reported from nature. All the isolates were tested for their inhibitory activities against NO production in RAW 264.7 cells stimulated by LPS. It was found that compounds 3 and 9 remarkably down-regulated LPS-induced NO production with IC 50 values, 5.4 and 40.3 μM, respectively, without cytotoxicity.