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NF-κB Inhibiting Naphthopyrones from the Fijian Echinoderm Comanthus parvicirrus

Authors
  • Folmer, Florence
  • Harrison, William T. A.
  • Tabudravu, Jioji N.
  • Jaspars, Marcel
  • Aalbersberg, William
  • Feussner, Klaus
  • Wright, Anthony D.
  • Dicato, Mario
  • Marc Diederich
Type
Published Article
Journal
Journal of Natural Products
Publisher
American Chemical Society
Publication Date
Jun 23, 2008
Volume
71
Issue
6
Pages
1120–1120
Identifiers
DOI: 10.1021/np8002436
Source
LBMCC
Keywords
License
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Abstract

The two naphthopyrones 6-methoxycomaparvin (1) and 6-methoxycomaparvin 5-methyl ether (2) were isolated from a bioactive methanol-soluble extract of the Fijian echinoderm Comanthus parvicirrus. Their structures were assigned on the basis of spectroscopic methods. X-ray diffraction analysis was used to confirm the structure of 1. Both compounds were tested for their potential to inhibit the activation of the transcription factor NF-kappaB, which plays an important role in cancer development and inflammation, and the mechanism of action of the two compounds was investigated. Both naphthopyrones 1 and 2 completely inhibit TNF-alpha-induced NF-kappaB activation at a concentration of 300 microM by inhibiting the enzymatic activity of the kinase IKKbeta.

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