Drazen J M
Harvard Medical School, Cambridge, Massachusetts, USA.
Pharmacotherapy. 1997 Jan-Feb;17(1 Pt 2):22S-30S.
The leukotrienes (LTs), a family of inflammatory mediators arising from the metabolism of arachidonic acid via the 5-lipoxygenase pathway, are prominently implicated in the pathobiology of asthma. Two classes of LTs, the cysteinyl LTs (LTC4, LTD4, and LTE4) and the dihydroxy-LT (LTB4) have been identified, with each class acting via distinct receptors. Inhibition of LT-mediated inflammation can be achieved by either interruption of 5-lipoxygenase action, thereby preventing formation of the LTs, or inhibition at specific LT receptor sites in the airway. Both the 5-lipoxygenase inhibitors and the cysLT receptor antagonists have thus far demonstrated the capacity to improve pulmonary function and reduce symptoms in clinical models of asthma, such as exercise-, aspirin-, or antigen-induced bronchoconstriction, and to improve pulmonary function in patients with mild-to-moderate, chronic stable asthma. The LTs are therefore critical effector molecules in some patients with asthma and important targets in the pharmacologic management of this disease.
白三烯（LTs）是一族通过5-脂氧合酶途径由花生四烯酸代谢产生的炎症介质，在哮喘的病理生物学中起着重要作用。已鉴定出两类白三烯，即半胱氨酰白三烯（LTC4、LTD4和LTE4）和二羟基白三烯（LTB4），每一类都通过不同的受体起作用。抑制LT介导的炎症可通过中断5-脂氧合酶的作用来实现，从而阻止白三烯的形成，或在气道中的特定LT受体位点进行抑制。到目前为止，5-脂氧合酶抑制剂和半胱氨酰白三烯受体拮抗剂在哮喘临床模型中均已显示出改善肺功能和减轻症状的能力，如运动、阿司匹林或抗原诱导的支气管收缩，并能改善轻至中度慢性稳定哮喘患者的肺功能。因此，白三烯在一些哮喘患者中是关键的效应分子，也是该疾病药物治疗的重要靶点。
