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Inhibition of TNF-alpha promoter activity and synthesis by A11-99-1, a new cyclopentenone from the ascomycete Mollisia melaleuca

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Author

Summary, in English

In a search for inhibitors of the inducible tumor necrosis factor-alpha (TNF-alpha) promoter activity and synthesis, a new chlorinated cyclopentenone was isolated from fermentations of the ascomycete Mollisia melaleuca. The structure was determined by a combination of spectroscopic techniques. The compound blocked the inducible human TNF-alpha promoter activity and synthesis with IC50-values of 2.5-5 mu g/ml (8.1-16.1 mu M). Studies on the mode of action of the compound revealed that the inhibition of TNF-alpha promoter activity is caused by an inhibition of the phosphorylation of the I kappa B protein which prevents the activation of the transcription factor NF-kappa B. No cytotoxic, antibacterial and antifungal activities could be observed up to 100 mu g/ml (323 mu m) of the compound.

Publishing year

2005

Language

English

Pages

478-484

Publication/Series

Zeitschrift fuer Naturforschung. Section C: A Journal of Biosciences

Volume

60c

Issue

5-6

Document type

Journal article

Publisher

Verlag der Zeitschrift für Naturforschung

Topic

  • Organic Chemistry

Status

Published

ISBN/ISSN/Other

  • ISSN: 0939-5075