人工合成白细胞介素-1阻滞剂预防晶状体蛋白、内毒素和白细胞介素-1引起的眼部炎症。

G C Chiou, Q S Yao, T Okawara
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引用次数: 21

摘要

众所周知,皮质类固醇是有效的抗炎剂,但它们会产生严重的副作用。虽然花生四烯酸代谢物阻滞剂已被开发用于治疗炎症,但它们的效力远不如皮质类固醇。此外,它们还会产生严重的副作用。为了寻找有效和安全的非甾体抗炎药(NSAIA),白细胞介素-1 (IL-1)阻滞剂已经被开发出来。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药,其抑制晶状体蛋白诱导的炎症的效力与强的松龙相当,抑制内毒素和il -1诱导的葡萄膜炎的效力是强的松龙的两倍。到目前为止,这些化合物的剂量测试没有发现严重的副作用。这些结果表明,研制强效nsaas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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Prevention of ocular inflammation induced by lens protein, endotoxin, and interleukin-1 with synthetic interleukin-1 blockers.

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.

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