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大环内酯类抗生素作为抗炎剂:罗红霉素的意外作用。

Macrolide antibiotics as antiinflammatory agents: roxithromycin in an unexpected role.

作者信息

Agen C, Danesi R, Blandizzi C, Costa M, Stacchini B, Favini P, Del Tacca M

机构信息

Istituto di Farmacologia Medica, Università di Pisa, Italy.

出版信息

Agents Actions. 1993 Jan;38(1-2):85-90. doi: 10.1007/BF02027218.

Abstract

The antiinflammatory activity of a new 14-membered macrolide antibiotic, roxithromycin, was evaluated in various rat models including carrageenan- and poly-L-arginine-induced hind-paw oedema, croton oil inflamed ear assay and polyester sponge granuloma. When administered orally to animals, roxithromycin displayed an atypical profile in the assays utilized, including: (1) marked antioedema activity similar to that of indomethacin in poly-L-arginine assay, (2) significant inhibition of lambda-carrageenan hind-paw oedema and croton-oil-induced inflammation in the ear, although indomethacin was more effective, and (3) failure to reduce the development of granuloma induced by implanted polyester sponges, while indomethacin significantly reduced the chronic inflammatory reaction. Based on these results, it is concluded that roxithromycin is active in reducing the acute inflammatory reaction in rat models through mechanisms different from conventional nonsteroidal antiinflammatory agents such as indomethacin. Therefore, roxithromycin may have a favorable impact on skin inflammatory reactions accompanying microbial infections.

摘要

在包括角叉菜胶和聚-L-精氨酸诱导的后爪水肿、巴豆油诱发的耳部炎症试验以及聚酯海绵肉芽肿等多种大鼠模型中,评估了一种新型14元大环内酯类抗生素罗红霉素的抗炎活性。当对动物口服给药时,罗红霉素在所用试验中呈现出非典型特征,包括:(1)在聚-L-精氨酸试验中具有与吲哚美辛相似的显著抗水肿活性;(2)对λ-角叉菜胶诱导的后爪水肿和巴豆油诱发的耳部炎症有明显抑制作用,尽管吲哚美辛的效果更佳;(3)不能减轻植入聚酯海绵诱导的肉芽肿的形成,而吲哚美辛能显著减轻慢性炎症反应。基于这些结果,得出结论:罗红霉素通过不同于传统非甾体抗炎药如吲哚美辛的机制,在减轻大鼠模型的急性炎症反应方面具有活性。因此,罗红霉素可能对伴随微生物感染的皮肤炎症反应产生有利影响。

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