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用合成白细胞介素-1阻滞剂预防晶状体蛋白、内毒素和白细胞介素-1诱导的眼部炎症。

Prevention of ocular inflammation induced by lens protein, endotoxin, and interleukin-1 with synthetic interleukin-1 blockers.

作者信息

Chiou G C, Yao Q S, Okawara T

机构信息

Institute of Ocular Pharmacology, Texas A&M University, College of Medicine, College Station.

出版信息

J Ocul Pharmacol. 1994 Fall;10(3):577-86. doi: 10.1089/jop.1994.10.577.

Abstract

It is well known that corticosteroids are potent anti-inflammatory agents, yet they produce serious side effects. Although arachidonate metabolite blockers have been developed for the treatment of inflammation, they are much less potent than corticosteroids. Furthermore, they still process serious side effects. In search of potent and safe non-steroidal anti-inflammatory agents (NSAIA), interleukin-1 (IL-1) blockers have been developed. Among 121 CK-analogs studied, CK-17, CK-101A and CK103A have been identified as promising anti-inflammatory agents as potent as prednisolone in inhibiting lens proteins-induced inflammation and twice as potent as prednisolone in inhibiting endotoxin-and IL-1-induced uveitis. No serious side effects could be noticed with the doses of these compounds tested to date. These results indicate that the development of potent NSAIAs is feasible. Moreover, these compounds are not related to arachidonate metabolites.

摘要

众所周知,皮质类固醇是强效抗炎剂,但它们会产生严重的副作用。尽管已经开发出花生四烯酸代谢物阻滞剂用于治疗炎症,但它们的效力远低于皮质类固醇。此外,它们仍然存在严重的副作用。为了寻找强效且安全的非甾体抗炎药(NSAIA),白细胞介素-1(IL-1)阻滞剂已被开发出来。在研究的121种CK类似物中,CK-17、CK-101A和CK103A已被确定为有前景的抗炎剂,在抑制晶状体蛋白诱导的炎症方面与泼尼松龙一样有效,在抑制内毒素和IL-1诱导的葡萄膜炎方面效力是泼尼松龙的两倍。迄今为止,在测试的这些化合物剂量下未发现严重的副作用。这些结果表明开发强效NSAIA是可行的。此外,这些化合物与花生四烯酸代谢物无关。

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