环氧合酶／5-脂氧合酶双重抑制剂的研究进展

非甾体类抗炎药(NSAID)广泛用于各种炎症的治疗。长期使用经典的NSAID会产生严重的副作用,尤其是胃肠道副作用。为避免经典的NSAID的副作用,开发出了选择性COX-2抑制剂,但长期使用选择性COX-2抑制剂对心血管系统有副作用。COX/5-LOX双重抑制剂通过同时阻断炎症介质前列腺素和白三烯的形成,产生协同的抗炎作用,有望提高疗效,同时避免COX抑制剂引发的副作用。本文对COX/5-LOX双重抑制剂的抗炎镇痛作用机制,以及研究现状进行综述。

Development of dual cyclooxygenase/5-1ipoxygenase inhibitors

Non steroidal anti-inflammatory drugs(NSAID) are among the most widely used medications for inflammatory diseases,but classical NSAID produce serious adverse effects,especially gastrointestinal adverse events.In order to avoid the side-effects of NSAID therapy,COX-2 inhibitors have been deve-loped.However,long-term use of COX-2 inhibitors may result in cardiovascular adverse events.Dual inhibitors of COX and 5-LOX may have synergistic anti-inflammatory effects and reduce the undesirable side-effects of COX inhibitors by blocking the formation of both prostaglandins and leucotrienes.In this review,the mechanisms of dual inhibitors of COX/5-LOX are described and various structural families of dual inhibitors are illustrated.