A novel inhibitor of IL-1 generation, E5090: in vitro inhibitory effects on the generation of IL-1 by human monocytes.
E5090 is an orally active inhibitor of IL-1 generation, being converted in vivo into the pharmacologically active deacetylated form (DA-E5090). In vitro effects of DA-E5090 on the generation of IL-1 by human monocytes stimulated with LPS were examined. DA-E5090 inhibited both IL-1 alpha and IL-1 beta generation by human monocytes stimulated with 1 microgram/ml of LPS in a dose dependent-manner (1-10 microM), as determined by LAF assay and ELISA. Northern blotting analysis indicated that DA-E5090 inhibits transcription of IL-1 alpha and IL-1 beta m-RNAs.
Goto
M
M
Eisai Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
Chiba
K
K
Hashida
R
R
Shirota
H
H
D000179:Acrylates / Q000494:pharmacology*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology*; D015152:Blotting, Northern; D015870:Gene Expression / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007375:Interleukin-1 / Q000096:biosynthesis* / Q000235:genetics; D008070:Lipopolysaccharides / Q000494:pharmacology; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism*; D009284:Naphthols / Q000494:pharmacology*; D012333:RNA, Messenger / Q000378:metabolism
D000179:Acrylates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007375:Interleukin-1; D008070:Lipopolysaccharides; D009284:Naphthols; D012333:RNA, Messenger; C069679:DA-E 5090; C069676:E 5090