Inhibition of TNF-alpha promoter activity and synthesis by A11-99-1, a new cyclopentenone from the ascomycete Mollisia melaleuca
Författare
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.
Avdelning/ar
Publiceringsår
2005
Språk
Engelska
Sidor
478-484
Publikation/Tidskrift/Serie
Zeitschrift fuer Naturforschung. Section C: A Journal of Biosciences
Volym
60c
Issue
5-6
Länkar
Dokumenttyp
Artikel i tidskrift
Förlag
Verlag der Zeitschrift für Naturforschung
Ämne
- Organic Chemistry
Status
Published
ISBN/ISSN/Övrigt
- ISSN: 0939-5075