Chiba K, Goto M, Shirota H
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
Agents Actions Suppl. 1991;32:231-5. doi: 10.1007/978-3-0348-7405-2_31.
The in vivo production of IL-1-like activity was investigated in the exudate of a rat air-pouch inflammatory model. An inflammatory reaction was induced by LPS injection into the air-pouch. IL-1 activity in the exudate reached the maximum level at 4 h and then rapidly decreased until 8 h after the injection of LPS. Orally administered E5090 and prednisolone dose-dependently inhibited the generation of IL-1 activity. Both compounds also suppressed chronic granuloma formation in parallel with the IL-1 inhibition. On the other hand, indomethacin had no effect on either IL-1 generation or granuloma formation in spite of the complete inhibition of PGE2 generation. These results suggest that E5090 inhibits the production of IL-1-like activity in the exudate and exhibits steroid-like antiinflammatory effects.
在大鼠气囊炎症模型的渗出液中研究了白细胞介素-1样活性的体内产生情况。通过向气囊内注射脂多糖诱导炎症反应。注射脂多糖后4小时，渗出液中的白细胞介素-1活性达到最高水平，然后迅速下降，直至8小时。口服给予的E5090和泼尼松龙剂量依赖性地抑制白细胞介素-1活性的产生。这两种化合物还与白细胞介素-1抑制作用平行地抑制慢性肉芽肿的形成。另一方面，尽管吲哚美辛完全抑制了前列腺素E2的产生，但对白细胞介素-1的产生或肉芽肿的形成均无影响。这些结果表明，E5090抑制渗出液中白细胞介素-1样活性的产生，并表现出类类固醇的抗炎作用。
