Stelmach Iwona, Grzelewski Tomasz
Department of Pediatrics and Allergy, N Copernicus Hospital, Lodz, Poland.
Recent Pat Inflamm Allergy Drug Discov. 2008 Nov;2(3):202-11. doi: 10.2174/187221308786241938.
Leukotrienes, and especially cysteinyl leukotrienes have been shown to be involved in many processes that play a role in asthma pathophysiology: eosinophil recruitment, the most characteristic processes of asthma pathogenesis, increased mucosal secretion, which impairs the normal process of airway clearance and favors the development of mucus plugs, mucosal edema, caused by increased vascular permeability and bronchoconstriction, leading to smooth muscle hypertrophy. Latest progress in the understanding of chronic asthma pathology events underline the leukotriene synthesis pathway enzymes and different leukotriene receptors as potential targets of asthma treatment in children. Agents inhibiting the production of leukotrienes or agents antagonising their receptor's action, attract attention. Studies on molecular mechanisms of leukotrienes action have led to the development and patents of potential drugs including new 5-lipoxygenase inhibitors, 5-lipoxygenase-activating protein (FLAP) inhibitors, leukotriene B4 receptor antagonists, or nanoparticulate leukotriene receptor antagonist formulations.
白三烯，尤其是半胱氨酰白三烯，已被证明参与了许多在哮喘病理生理学中起作用的过程：嗜酸性粒细胞募集，这是哮喘发病最具特征性的过程；黏膜分泌增加，这会损害气道正常的清除过程并促进黏液栓的形成；黏膜水肿，由血管通透性增加和支气管收缩引起，导致平滑肌肥大。对慢性哮喘病理事件认识的最新进展强调了白三烯合成途径酶和不同的白三烯受体作为儿童哮喘治疗潜在靶点的重要性。抑制白三烯产生的药物或拮抗其受体作用的药物引起了关注。对白三烯作用分子机制的研究已促成了包括新型5-脂氧合酶抑制剂、5-脂氧合酶激活蛋白（FLAP）抑制剂、白三烯B4受体拮抗剂或纳米颗粒白三烯受体拮抗剂制剂等潜在药物的开发并获得专利。
