Ferreira S H, Lorenzetti B B, Bristow A F, Poole S
Faculty of Medicine, São Paulo, Brazil.
Nature. 1988 Aug 25;334(6184):698-700. doi: 10.1038/334698a0.
Interleukin-1 (IL-1) describes two inflammatory proteins, IL-1 alpha and IL-1 beta, produced by activated macrophages and other cell types and encoded by two genes. Their amino acid sequences have only 26% similarity, but their biological activities are comparable, with a few exceptions; indeed, both molecules appear to act at the same receptor. As IL-1 release prostaglandins which sensitize nociceptors in man and in experimental animals, we tested IL-1 alpha and IL-1 beta in rats for hyperalgesic (nociceptive) activity. Our results show that IL-1 beta given systemically is an extremely potent hyperalgesic agent with a probable peripheral site of action; IL-1 alpha is approximately 3,000 times less active than IL-1 beta. We have delineated the region of IL-1 beta mediating the hyperalgesic effect and developed an analgesic tripeptide analogue of IL-1 beta which antagonizes hyperalgesia evoked by IL-1 beta and by the inflammatory agent carrageenan.
白细胞介素-1（IL-1）指的是两种炎症蛋白，即IL-1α和IL-1β，由活化的巨噬细胞及其他细胞类型产生，由两个基因编码。它们的氨基酸序列仅有26%的相似性，但其生物学活性相当，仅有少数例外情况；实际上，这两种分子似乎作用于同一受体。由于IL-1可释放使人类和实验动物中的伤害感受器敏感化的前列腺素，我们在大鼠中测试了IL-1α和IL-1β的痛觉过敏（伤害感受）活性。我们的结果表明，全身给予IL-1β是一种极其强效的痛觉过敏剂，其作用部位可能在周围；IL-1α的活性比IL-1β低约3000倍。我们已经确定了IL-1β介导痛觉过敏效应的区域，并开发了一种IL-1β的镇痛三肽类似物，它可拮抗IL-1β和炎症剂角叉菜胶诱发的痛觉过敏。
