ABSTRACT Reactive oxygen species and granule proteases produced by neutrophils contribute to the pathogenesis of inflammatory diseases. The extracts of the roots and the leaves of Salvia nipponica var. formosana were showed potent inhibitory effects on superoxide anion production in fMLP/CB-activated human neutrophils as well as other anti-inflammatory effects, and led to the isolation of 25 compounds. Among them, compounds 8, 12, 13, 14, 15, 17 and 20 were exhibited more potent inhibitory effect on superoxide anion generation and elastase release by human neutrophils in response to fMLP/CB. Moreover, those isolated compounds also showed significant anticholinesterase and antioxidative activities. To the best of our knowledge, this is the first report of phytochemical and biological activity study on S. nipponica var. formosana.