Inhibition of inducible TNF-alpha expression by oxaspirodion, a novel spiro-compound from the ascomycete Chaetomium subspirale

J Rether, G Erkel, T Anke, Olov Sterner

Forskningsoutput: TidskriftsbidragArtikel i vetenskaplig tidskriftPeer review

Sammanfattning

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.
Originalspråkengelska
Sidor (från-till)829-834
TidskriftBiological Chemistry
Volym385
Nummer9
DOI
StatusPublished - 2004

Bibliografisk information

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)

Ämnesklassifikation (UKÄ)

  • Organisk kemi

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