BW-B 70C

BW-B 70C是一种强效的和选择性的5-脂氧合酶抑制剂[1].

5-脂氧合酶是一种将必需脂肪酸(EFAs)转换成白三烯,并且由5-脂氧合酶激活蛋白(FLAP)活化的酶.

BW-B 70C是一种强效的和选择性的5-脂氧合酶抑制剂.BW-B 70C在体内具有较高的效力和较长的持续时间,被认为是潜在的抗哮喘药物[1].在致敏豚鼠中,BW B70C (2-50 mg/kg)剂量依赖性地抑制过敏原诱导的支气管收缩,这与BW B70C对5-脂氧合酶的抑制活性相一致.另外,BW B70C (20 mg/kg)抑制嗜酸性细胞浸润达67%[2].在豚鼠中,5-脂氧合酶抑制剂BW B70C (30 mg/kg)抑制白细胞迁徙至气道管腔\由肺泡巨噬细胞合成白三烯C4以及内毒素诱导的白蛋白微血管渗漏.然而,BW B70C不影响血管白细胞着边以及分泌磷脂酶A2和TNF-α的血液水平[3].在局灶性脑缺血大鼠模型中,BW-B 70C改善神经功能缺损评分并降低梗死.此外,BW-B 70C减少5-脂氧合酶(5-LOX),并通过NF-κB的下调抑制诱导型一氧化氮合酶(iNOS)的表达[4].

参考文献：
[1].  Payne AN, Jackson WP, Salmon JA, et al. Hydroxamic acids and hydroxyureas as novel, selective 5-lipoxygenase inhibitors for possible use in asthma. Agents Actions Suppl, 1991, 34: 189-199.
[2].  Yeadon M, Dougan FL, Petrovic A, et al. Effect of BW B70C, a novel inhibitor of arachidonic acid 5-lipoxygenase, on allergen-induced bronchoconstriction and late-phase lung eosinophil accumulation in sensitised guinea-pigs. Agents Actions, 1993, 38(1-2): 8-18.
[3].  Bureau MF, De Castro CM, Cortese C, et al. 5-Lipoxygenase and endotoxin-induced microvascular albumin exchanges and leucocyte recruitment in guinea-pig lungs. Eur J Pharmacol, 1997, 324(1): 89-98.
[4].  Jatana M, Giri S, Ansari MA, et al. Inhibition of NF-kappaB activation by 5-lipoxygenase inhibitors protects brain against injury in a rat model of focal cerebral ischemia. J Neuroinflammation, 2006, 3: 12.