HUMAN RECOMBINANT LIPOCORTIN-1 HAS ACUTE LOCAL ANTI-INFLAMMATORY PROPERTIES IN THE RAT PAW EDEMA TEST
HUMAN RECOMBINANT LIPOCORTIN-1 HAS ACUTE LOCAL ANTI-INFLAMMATORY PROPERTIES IN THE RAT PAW EDEMA TEST
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DOI：
10.1073/pnas.86.9.3428
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发表时间：
1989-05-01
影响因子：
11.1
通讯作者：
PEPINSKY, RB
中科院分区：
文献类型：
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作者：
CIRINO, G;PEERS, SH;PEPINSKY, RB
人重组脂皮质素1已经在常规急性炎症模型中测试了抗炎活性。当通过足底注射角叉菜胶诱导时，局部施用微克量的蛋白质抑制大鼠爪的水肿：ED 50为10-20 μ g/爪，并且抑制（最大60-70%）不依赖于完整的肾上腺皮质。脂皮质素产生约角叉菜胶试验中50%的抑制作用对缓激肽、5-羟色胺、血小板活化因子-乙酸酯或葡聚糖引起的水肿无活性，而脂皮质素强烈抑制了眼镜蛇毒磷脂酶A2引起的水肿。蛋白质抑制水肿时，大鼠进行了预处理的代理人，耗尽肥大细胞胺，激肽原，或多形核白细胞开始角叉菜胶水肿，但没有抑制作用时，大鼠进行预处理的双重环氧合酶/脂氧合酶抑制剂BW 755 C。这些结果表明，人重组脂皮质素可能通过选择性干扰类花生酸的产生而具有有效的局部抑制活性。脂皮质素对肥大细胞脱颗粒或激肽引起的水肿相对无效，但磷脂酶A2引起的脱颗粒除外。
Human recombinant lipocortin 1 has been tested for anti-inflammatory activity in a conventional model of acute inflammation. Microgram amounts of the protein, locally administered, inhibited edema of the rat paw when induced by subplantar injections of carrageenin: the ED50 was 10-20 .mu.g per paw, and inhibition (maximum of 60-70%) was not dependent upon an intact adrenal cortex. Doses of lipocortin that produced .apprxeq. 50% inhibition in the carrageenin test were inactive against edema elicited by bradykinin, serotonin, platelet-activating factor-acether, or dextran, whereas edema caused by Naja mocambique venom phospholipase A2 was strongly inhibited by lipocortin. The protein inhibited edema when rats were pretreated with agents that depleted mast-cell amines, kininogen, or polymorphonuclear leukocytes prior to initiation of the carrageenin edema but had no inhibitory action when rats were pretreated with the dual cyclooxygenase/lipoxygenase inhibitor BW 755C. These results demonstrate that human recombinant lipocortin has potent local antiinflammatory activity, probably through selectively interfering with eicosanoid generation. Lipocortin is relatively ineffective against edema caused by mast-cell degranulation or kinins, except when degranulation is caused by phospholipase A2.