抗炎脂皮质素衍生肽。

M Perretti, R J Flower
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引用次数: 7

摘要

肽Ac2-26,从人脂皮质蛋白1序列中提取,以浓度依赖的方式抑制人中性粒细胞胞质颗粒中弹性酶活性的释放,以及中性粒细胞对内皮细胞单层的粘附(IC50约为100微克/毫升,33微米)。肽Ac2-26的作用不局限于特定的中性粒细胞激活剂,对甲酰基met - leu - phe (FMLP),白三烯B4 (LTB4)和血小板活化因子(PAF)有效。肽Ac2-26不改变FMLP与其受体的结合。这些体外观察补充了用这种肽获得的体内数据,并可能使我们更好地了解其药理学,也许也可以了解脂皮质素1的药理学。
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Anti-inflammatory lipocortin-derived peptides.

Peptide Ac2-26, drawn from the sequence of human lipocortin 1, inhibited the release of elastase activity from cytoplasmic granules of human neutrophils, and neutrophil adhesion to monolayers of endothelial cells, in a concentration-dependent manner (approximate IC50 of 100 micrograms/ml, 33 microM). The effect of peptide Ac2-26 was not restricted to a specific neutrophil activator, being effective against formyl-Met-Leu-Phe (FMLP), leukotriene B4 (LTB4) and platelet-activating factor (PAF). Peptide Ac2-26 did not alter FMLP binding to its receptor. These in vitro observations complement in vivo data obtained with this peptide and may enable a better understanding of its pharmacology and, perhaps, that of of lipocortin 1 too.

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