New sesquiterpene dimers from Inula britannica inhibit NF-κB activation and NO and TNF-α production in LPS-stimulated RAW264.7 cells

Hui Zi Jin, Dongho Lee, Jeong Hyung Lee, Kyeong Lee, Young Soo Hong, Dong Ho Choung, Young Ho Kim, Jung Joon Lee

Research output: Contribution to journalArticle

50 Citations (Scopus)

Abstract

A bioassay-guided isolation of an ethyl acetate-soluble extract of the aerial parts of Inula britannica van chinensis (Rupr.) Regel, using an in vitro NF-κB reporter gene assay, led to the isolation of four new sesquiterpene dimers bearing a norbornene moiety, inulanolides A - D (1 - 4), and three known sesquiterpenes, 1,6α-dihydroxyeriolanolide (5), 1-acetoxy-6α- hydroxyeriolanolide (6), and eupatolide (7). The structures of the new compounds were elucidated by spectroscopic methods. Among these compounds, inulanolides B and D (2 and 4) and eupatolide (7), exhibited potent inhibitory activity on the LPS-induced NF-κB activation with IC50 values of 0.49 μM, 0.48 μM, and 1.54 μM, respectively. Consistent with their inhibitory effect on NF-κB activation, compounds 2,4, and 7 also strongly inhibited the production of NO and TNF-α in the LPS-stimulated RAW264.7 cells with IC50 values in the range of 2 μM.

Original languageEnglish
Pages (from-to)40-45
Number of pages6
JournalPlanta Medica
Volume72
Issue number1
DOIs
Publication statusPublished - 2006 Jan 1
Externally publishedYes

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Keywords

  • Compositae
  • Inula britannica
  • NF-κB
  • NO
  • Sesquiterpene dimer
  • TNF-α

ASJC Scopus subject areas

  • Plant Science
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

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