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

Verfasser / Beitragende:
[Jan Rether, Gerhard Erkel, Timm Anke, Olov Sterner]
Ort, Verlag, Jahr:
2004
Enthalten in:
Biological Chemistry, 385/9(2004-09-01), 829-834
Format:
Artikel (online)
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024 7 0 |a 10.1515/BC.2004.108  |2 doi 
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245 0 0 |a Inhibition of inducible TNF-α expression by oxaspirodion, a novel spiro-compound from the ascomycete Chaetomium subspirale  |h [Elektronische Daten]  |c [Jan Rether, Gerhard Erkel, Timm Anke, Olov Sterner] 
520 3 |a In a search for compounds inhibiting the inducible TNF-αa promoter activity in T cells, a new spiro-compound, designated oxaspirodion, was isolated from fermentations of the ascomycete Chaetomium subspirale. Oxaspirodion inhibited TNF-α promoter-driven luciferase reporter gene expression with an IC50 value of 2.5 µg/ml (10 µM) in TPA/ionomycin-stimulated Jurkat T cells. Studies on the mode of action of the compound revealed that the inhibition of the TNF-α 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-κB, which is involved in the inducible expression of many proinflammatory genes. 
540 |a © Walter de Gruyter 
690 7 |a Biochemistry  |2 nationallicence 
690 7 |a Molecular biology  |2 nationallicence 
690 7 |a Cellular biology  |2 nationallicence 
690 7 |a ERK  |2 nationallicence 
690 7 |a NF-κB  |2 nationallicence 
690 7 |a oxaspirodion  |2 nationallicence 
690 7 |a TNF-α synthesis  |2 nationallicence 
700 1 |a Rether  |D Jan  |u Institut für Biotechnologie und Wirkstoff-Forschung e.V. (IBWF), Erwin-Schrödinger-Str. 56, D-67663 Kaiserslautern Germany  |4 aut 
700 1 |a Erkel  |D Gerhard  |u Institut für Biotechnologie und Wirkstoff-Forschung e.V. (IBWF), Erwin-Schrödinger-Str. 56, D-67663 Kaiserslautern Germany  |4 aut 
700 1 |a Anke  |D Timm  |u Institut für Biotechnologie und Wirkstoff-Forschung e.V. (IBWF), Erwin-Schrödinger-Str. 56, D-67663 Kaiserslautern Germany  |4 aut 
700 1 |a Sterner  |D Olov  |u Division of Organic Chemistry 2, Chemical Center, University of Lund, S-22100 Lund, Sweden  |4 aut 
773 0 |t Biological Chemistry  |d Walter de Gruyter  |g 385/9(2004-09-01), 829-834  |x 1431-6730  |q 385:9<829  |1 2004  |2 385  |o bchm 
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950 |B NATIONALLICENCE  |P 700  |E 1-  |a Erkel  |D Gerhard  |u Institut für Biotechnologie und Wirkstoff-Forschung e.V. (IBWF), Erwin-Schrödinger-Str. 56, D-67663 Kaiserslautern Germany  |4 aut 
950 |B NATIONALLICENCE  |P 700  |E 1-  |a Anke  |D Timm  |u Institut für Biotechnologie und Wirkstoff-Forschung e.V. (IBWF), Erwin-Schrödinger-Str. 56, D-67663 Kaiserslautern Germany  |4 aut 
950 |B NATIONALLICENCE  |P 700  |E 1-  |a Sterner  |D Olov  |u Division of Organic Chemistry 2, Chemical Center, University of Lund, S-22100 Lund, Sweden  |4 aut 
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