Planta Med 2006; 72(1): 40-45
DOI: 10.1055/s-2005-873189
Original Paper
Biochemistry and Molecular Biology
© Georg Thieme Verlag KG Stuttgart · New York

New Sesquiterpene Dimers from Inula britannica Inhibit NF-κB Activation and NO and TNF-α Production in LPS-Stimulated RAW264.7 Cells

Hui Zi Jin1 , 2 , Dongho Lee1 , Jeong Hyung Lee1 , Kyeong Lee1 , Young-Soo Hong1 , Dong-Ho Choung1 , Young Ho Kim2 , Jung Joon Lee1
  • 1Anticancer Research Laboratory, Korea Research Institute of Bioscience and Biotechnology, Daejeon, Korea
  • 2College of Pharmacy, Chungnam National University, Daejeon, Korea
Further Information

Publication History

Received: April 5, 2005

Accepted: June 8, 2005

Publication Date:
10 November 2005 (online)

Abstract

A bioassay-guided isolation of an ethyl acetate-soluble extract of the aerial parts of Inula britannica var. 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.

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Dr. Jung Joon Lee

Anticancer Research Laboratory

Korea Research Institute of Bioscience and Biotechnology

P.O. Box 115

Yuseong

Daejeon 305-600

Korea

Fax: +82-42-860-4585

Email: jjlee@kribb.re.kr