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

49 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

Fingerprint

Inula
Sesquiterpenes
Dimers
sesquiterpenoids
Inhibitory Concentration 50
inhibitory concentration 50
Bearings (structural)
Chemical activation
Bioassay
Reporter Genes
reporter genes
Biological Assay
aerial parts
Assays
bioassays
Genes
cells
Antennas
extracts
assays

Keywords

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

ASJC Scopus subject areas

  • Plant Science
  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

New sesquiterpene dimers from Inula britannica inhibit NF-κB activation and NO and TNF-α production in LPS-stimulated RAW264.7 cells. / Jin, Hui Zi; Lee, Dongho; Lee, Jeong Hyung; Lee, Kyeong; Hong, Young Soo; Choung, Dong Ho; Kim, Young Ho; Lee, Jung Joon.

In: Planta Medica, Vol. 72, No. 1, 01.01.2006, p. 40-45.

Research output: Contribution to journalArticle

Jin, Hui Zi ; Lee, Dongho ; Lee, Jeong Hyung ; Lee, Kyeong ; Hong, Young Soo ; Choung, Dong Ho ; Kim, Young Ho ; Lee, Jung Joon. / New sesquiterpene dimers from Inula britannica inhibit NF-κB activation and NO and TNF-α production in LPS-stimulated RAW264.7 cells. In: Planta Medica. 2006 ; Vol. 72, No. 1. pp. 40-45.
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