Inhibition of inducible TNF-alpha expression by oxaspirodion, a novel spiro-compound from the ascomycete Chaetomium subspirale
Författare
Summary, in English
In a search for compounds inhibiting the inducible TNF-alpha promoter activity in T cells, a new spirocompound, designated oxaspirodion, was isolated from fermentations of the ascomycete Chaetomium subspirale. Oxaspirodion inhibited TNF-alpha promoterdriven luciferase reporter gene expression with an IC50 value of 2.5 mug/ml (10 muM) in TPA/ionomycinstimulated Jurkat T cells. Studies on the mode of action of the compound revealed that the inhibition of the TNF-alpha promoter activity is caused by an inhibition of the phosphorylation of the ERK1/2 kinases. In addition, oxaspirodion inhibited the activation of the transcription factor NF-kappaB, which is involved in the inducible expression of many proinflammatory genes.
Avdelning/ar
Publiceringsår
2004
Språk
Engelska
Sidor
829-834
Publikation/Tidskrift/Serie
Biological Chemistry
Volym
385
Issue
9
Dokumenttyp
Artikel i tidskrift
Förlag
De Gruyter
Ämne
- Organic Chemistry
Status
Published
ISBN/ISSN/Övrigt
- ISSN: 1437-4315