Abstract

The genus Cimicifuga is one of the smallest genera in the family Ranunculaceae. Cimicifugae Rhizoma originated from rhizomes of Cimicifuga simplex, and C. dahurica, C. racemosa, C. foetida, and C. heracleifolia have been used as anti-inflammatory, analgesic and antipyretic remedies in Chinese traditional medicine. Inflammation is related to many diseases. Cimicifuga taiwanensis was often used in folk therapy in Taiwan for inflammation. Phytochemical investigation and chromatographic separation of extracts from the roots of Cimicifuga taiwanensis has led to the isolation of six new compounds: cimicitaiwanins A–F (1–6, 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, 3–6 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-C. taiwanensis.

Highlights

  • Inflammation is a self-protective mechanism designed to eliminate harmful stimuli, including damaged cells, irritants, or pathogens, and initiate the wound repair process

  • In a series of studies on the anti-inflammatory constituents of Formosan endemic plants, over 500 species were screened for the inhibitory activity on LPS-induced Nitric oxide (NO) release in RAW 264.7 murine macrophages, and Cimicifuga taiwanensis was one of the active species

  • The 1H Nuclear magnetic resonance (NMR) spectrum (Table 1) showed the presence of the characteristic 9,19-cycloartane-type triterpene 7 methyl signals at δH 0.83, 0.92, 0.94, 0.99, 1.22, 1.32, and 1.08 (3H, d, J = 6.4 Hz), and 4 oxymethines appeared at δH 3.54 (1H, d, J = 4.0 Hz, H-24), 3.72 (1H, d, J = 5.6 Hz, H atoms at δH 3.81 (H-3)), 4.02 (1H, s, H-15), and 4.42 (1H, ddd, J = 9.6, 4.0, 3.2 Hz, H-23), while 1 cyclopropane methylene signal was found at δH 1.69 and 3.14

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Summary

Introduction

Inflammation is a self-protective mechanism designed to eliminate harmful stimuli, including damaged cells, irritants, or pathogens, and initiate the wound repair process. Inflammation sometimes induces further inflammation, leading to self-perpetuating chronic inflammation that can lead to severe cellular and tissue damage [1]. Chronic inflammation is associated with a variety of diseases, such as atherosclerosis [2], Alzheimer s disease [3], diabetes [4], and carcinogenesis [5]. Nitric oxide (NO) is a mediator in the inflammatory response involved in host defense. It is mainly produced by inducible nitric oxide synthase (iNOS) in inflammatory states [6] and plays a key role in every pathological process of the inflammatory process [7–10]. In a series of studies on the anti-inflammatory constituents of Formosan endemic plants, over 500 species were screened for the inhibitory activity on LPS-induced NO release in RAW 264.7 murine macrophages, and Cimicifuga taiwanensis was one of the active species

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