Anoectochilus roxburghii is a well‐known and valuable traditional Chinese herb due to various medicinal and functional benefits. In‐depth investigation is necessary to discover active ingredients and expand its application. In this study, four new compounds (1‐4) along with ten known compounds (5‐14) were isolated from the ethanol extract ofA.roxburghii. Their structures were elucidated by spectroscopic data interpretation. The isolates were screened for their inhibitory activities on the production of NO in lipopolysaccharide (LPS)‐stimulated RAW 264.7 macrophages. Among them, compounds 5, 6, 9, 10, 12, 13 and 14exhibited significant anti‐inflammatory activity through inhibiting the release of NO.