1. NF-κB-Inhibiting Naphthopyrones from the Fijian Echinoderm Comanthus parvicirrus
- Author
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Folmer, Florence, T. A. Harrison, William, N. Tabudravu, Jioji, Aalbersberg, William, Feussner, Klaus, D. Wright, Anthony, Dicato, Mario, Diederich, Marc, and Jaspars, Marcel
- 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-κB, which plays an important role in cancer development and inflammation, and the mechanism of action of the two compounds was investigated. Both naphthopyrones 1and 2completely inhibit TNF-α-induced NF-κB activation at a concentration of 300 µM by inhibiting the enzymatic activity of the kinase IKKβ.
- Published
- 2008
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