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Agents and Actions

, Volume 21, Issue 3–4, pp 269–271 | Cite as

In vitro effect of N-methoxy-3-(3,5-ditert-butyl-4-hydroxybenzylidene)-2-pyrrolidone (E-5110), a novel nonsteroidal anti-inflammatory agent, on generation of some inflammatory mediators

  • K. Katayama
  • H. Shirota
  • S. Kobayashi
  • K. Terato
  • H. Ikuta
  • I. Yamatsu
Antiinflammatory/Antiarthritic Agents

Abstract

Cultured rat synovial cells generate PGE2 upon stimulation with a factor derived from rate polymorphonuclear cells (Prostaglandins27, 697, 1984). E-5110 inhibited PGE2 generation by the synovial cells. The IC50 values (μM) for inhibition of PGE2 generation were 0.026 for E-5110, 0.008 for indomethacin, 0.112 for piroxicam, 0.003 for R-830, 0.667 for BW-755C and 2.05 for benoxaprofen. Calcium ionophore A-23187-stimulated LTB4 generation by human neutrophils was inhibited by E-5110 with an IC50 value of 0.20 μM, which was similar to NDGA. The inhibition of LTB4 by E-5110 was more potent than that of R-830, BW-755C or benoxaprofen. E-5110 also inhibited superoxide generation by human neutrophils stimulated with opsonized zymosan, f-Met-Leu-Phe and phorbol myristate acetate. These results indicate that E-5110 is a potent dual inhibitor that suppresses superoxide generation.

Keywords

Indomethacin PGE2 Piroxicam Human Neutrophil Myristate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Birkhäuser Verlag 1987

Authors and Affiliations

  • K. Katayama
    • 1
  • H. Shirota
    • 1
  • S. Kobayashi
    • 1
  • K. Terato
    • 1
  • H. Ikuta
    • 1
  • I. Yamatsu
    • 1
  1. 1.Eisai Research LaboratoriesEisai Co., Ltd.IbarakiJapan

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