Faculty of Pharmacy, Iryo Sosei (former Iwaki Meisei) University, Fukushima, Japan.
J Pept Sci. 2019 Aug;25(8):e3197. doi: 10.1002/psc.3197. Epub 2019 Jul 1.
Platelet-activating factor (PAF) is known as an important mediator of anaphylaxis and, therefore, may possibly serve as a direct target for anti-anaphylactic drugs. We recently reported that a synthetic N-terminally biotinylated peptide, BP21, alleviates hypothermia and vascular hyperpermeability during anaphylactic reactions in a mouse model of anaphylaxis via the direct binding of a Tyr-Lys-Asp-Gly sequence in the peptide to PAF. In this study, we investigated the effect of BP21 on in vivo anaphylactic hypotension. Results showed that BP21 significantly inhibited anaphylactic hypotension in a dose-dependent manner, with peak severity being reached within 20 minutes. Adrenaline, which is the recommended first line treatment for anaphylactic patients, did not inhibit anaphylactic hypothermia. The combined administration of BP21 with adrenaline inhibited both hypotension and hypothermia, even at both low doses, more effectively compared with solo administration of BP21 or adrenaline. These results suggested that BP21 could potentially be a novel anti-anaphylactic agent for targeting PAF in vivo.
血小板激活因子（PAF）是过敏反应的重要介质，因此可能成为抗过敏药物的直接靶点。我们最近报道，一种合成的 N 端生物素化肽 BP21 通过肽中的 Tyr-Lys-Asp-Gly 序列与 PAF 的直接结合，在过敏反应的小鼠模型中缓解过敏反应期间的体温过低和血管高通透性。在这项研究中，我们研究了 BP21 对体内过敏性低血压的影响。结果表明，BP21 以剂量依赖性方式显著抑制过敏性低血压，在 20 分钟内达到峰值严重程度。肾上腺素是推荐用于治疗过敏患者的一线药物，但不能抑制过敏性低体温。BP21 与肾上腺素联合给药可更有效地抑制低血压和低体温，即使在低剂量下也是如此，比单独使用 BP21 或肾上腺素更有效。这些结果表明，BP21 可能是一种针对体内 PAF 的新型抗过敏药物。
