A novel inhibitor of IL-1 generation, E5090: in vitro inhibitory effects on the generation of IL-1 by human monocytes

  • Agents Actions Suppl. 1991:32:225-9. doi: 10.1007/978-3-0348-7405-2_30.
M Goto  1 ,  K Chiba ,  R Hashida ,  H Shirota
Affiliations
  • 1. Eisai Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
PMID: 2069091 DOI: 10.1007/978-3-0348-7405-2_30
Abstract

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.

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