Planta Med 1998; 64(7): 594-597
DOI: 10.1055/s-2006-957528
© Georg Thieme Verlag Stuttgart · New York

Inhibitory Effect of Sesquiterpene Lactones from Saussurea lappa on Tumor Necrosis Factor-α Production in Murine Macrophage-Like Cells

Jae Youl Cho1 , Jisoo Park1 , Eun Sook Yoo1 , Kyong Up Baik1 , Jee Hyung Jung2 , Jongsoo Lee1 , Myung Hwan Park1
  • 1Department of Inflammation, Allergy and Autoimmune Diseases, R & D Center, Daewoong Pharmaceutical Co. Ltd., Sungnam, Korea
  • 2College of Pharmacy, Pusan National University, Pusan, Korea
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Publication History



Publication Date:
04 January 2007 (online)


Total methanol extract of Saussurea lappa radix (Compositae) showed potent inhibitory effect on the production of tumor necrosis factor-α (TNF-α), a proinflammatory cytokine, in murine macrophage-like cell (RAW264.7 cells) in our previous screening studies on 120 Korean medicinal plants. The activity-guided purification of the plant resulted in the isolation of three components. The chemical structures of the components isolated were established by spectroscopic analyses as sesquiterpene lactones [cynaropicrin (1), reynosin (2), and santamarine (3)]. These three compounds inhibited TNF-α production in a dose-dependent manner. The molar concentrations of cynaropicrin, reynosin, and santamarine producing 50% inhibition (IC50) of TNF-α production were 2.86 µg/ml (8.24 µM), 21.7 µg/ml (87.4 µM), and 26.2 µg/ml (105 µM), respectively. However, treatment with sulphydryl (SH) compounds such as L-cysteine, dithiothreitol, and 2-mercaptoethanol abrogated the inhibitory effect of cynaropicrin on TNF-α production. Therefore, we conclude that the principal inhibitory component of Saussurea lappa is cynaropicrin and its inhibitory effect is mediated through conjugation with SH-groups of target proteins.