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The genus <i>Cimicifuga</i> is one of the smallest genera in the family Ranunculaceae. Cimicifugae Rhizoma originated from rhizomes of <i>Cimicifuga</i> simplex, and <i>C. dahurica</i>, <i>C. racemosa</i>, <i>C. foetida</i>, and <i>C. heracleifolia</i> have been used as anti-inflammatory, analgesic and antipyretic remedies in Chinese traditional medicine. Inflammation is related to many diseases. <i>Cimicifuga taiwanensis</i> was often used in folk therapy in Taiwan for inflammation. Phytochemical investigation and chromatographic separation of extracts from the roots of <i>Cimicifuga taiwanensis</i> has led to the isolation of six new compounds: cimicitaiwanins A–F (<b>1</b>–<b>6</b>, respectively). The structures of the new compounds were unambiguously elucidated on the basis of extensive spectroscopic data analysis (1D- and 2D-NMR, MS, and UV) and comparison with the literature data. The effect of some isolates on the inhibition of NO production in lipopolysaccharide-activated RAW 264.7 murine macrophages was evaluated. Of the isolates, <b>3</b>–<b>6</b> exhibited potent anti-NO production activity, with IC₅₀ values ranging from 6.54 to 24.58 μM, respectively, compared with that of quercetin, an iNOS inhibitor with an IC₅₀ value of 34.58 μM. This is the first report on metabolite from the endemic Taiwanese plant-<i>C. taiwanensis</i>.