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

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Abstract

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.

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  • Organic Chemistry
Original languageEnglish
Pages (from-to)478-484
JournalZeitschrift fuer Naturforschung. Section C: A Journal of Biosciences
Volume60c
Issue number5-6
Publication statusPublished - 2005
Publication categoryResearch
Peer-reviewedYes

Bibliographic note

The information about affiliations in this record was updated in December 2015. The record was previously connected to the following departments: Organic chemistry (S/LTH) (011001240)