Department of Experimental Pharmacology University of Naples Federico II via Domenico Montesano 49 Naples 80131 Italy.
Mediators Inflamm. 1992;1(4):251-4. doi: 10.1155/S0962935192000383.
Antiflammin-2 (AF2) is a nonapeptide corresponding to the amino acid residues 246-254 of lipocortin-1 showing anti-inflammatory activity both in vitro and in vivo. The effect of AF2 on the thromboxane B(2) (TXB(2)) and histamine release from isolated and perfused guinea-pig lungs has been studied. AF-2 (10-100 nM) inhibited leukotriene C(4)- (LTC(4)) (3 ng) and antigen-induced (ovalbumin, 1 mg) TXB(2) release in normal and sensitized lungs, respectively. In contrast AF-2 (100 nM) did not modify TXB(2) release induced by histamine (5 mug) or bradykinin (5 mug) in normal lungs. Antigen-induced histamine release was not affected by 100 nM AF-2 infusion. When tested in chopped lung fragments AF-2 (0.1-25 muM) did not modify the release of histamine and TXB(2) induced by antigen (ovalbumin, 10 mug ml(-1)) or calcium ionophore A 23187 (1 muM). Our results show that the inhibitory effect of AF-2 on TXB(2) release is selective and depends on the stimulus applied. In this respect AF-2 mimics, at least in part, the actions of both glucocorticoids and lipocortin-1.
抗弗拉明-2（AF2）是一种九肽，对应于脂皮质素-1 的氨基酸残基 246-254，具有体外和体内抗炎活性。研究了 AF2 对分离和灌注豚鼠肺中血栓素 B2（TXB2）和组胺释放的影响。AF-2（10-100 nM）抑制白细胞三烯 C4-（LTC4）（3 ng）和抗原（卵清蛋白，1 mg）诱导的 TXB2 释放正常和致敏肺，分别。相比之下，AF-2（100 nM）不改变正常肺中组胺（5 mug）或缓激肽（5 mug）诱导的 TXB2 释放。100 nM AF-2 输注不影响抗原诱导的组胺释放。在切碎的肺片段中测试时，AF-2（0.1-25 μM）不改变抗原（卵清蛋白，10 μg ml-1）或钙离子载体 A23187（1 μM）诱导的组胺和 TXB2 的释放。我们的结果表明，AF-2 对 TXB2 释放的抑制作用是选择性的，取决于所应用的刺激物。在这方面，AF-2 至少部分模拟了糖皮质激素和脂皮质素-1 的作用。
