摘要
传统的非甾体抗炎药(NSAIDs)是一类广泛用于抗炎、解热、镇痛的药物,但由于胃肠道毒副作用和肾毒性使它的应用受到很大限制。而近年研究开发的新一代NSAIDs选择性/特异性COX-2抑制剂出现了增加心血管疾病的发病率(包括心脏病和中风)等安全性问题。随着对COX-1生理、病理机制的深入研究,发现其与多种疾病之间有密切的关系,如疼痛、血栓症、动脉粥样硬化、神经炎症和癌症等,而选择性地抑制COX-1为治疗上述多种疾病提供了新的思路。因此,COX-1及选择性COX-1抑制剂成为现代研究的热点。本文对COX-1的结构、生理病理功能及选择性COX-1抑制剂的发展现状和构效关系进行了综述。
Non-steroidal anti-inflammatory drugs （NSAIDs） are among the most commonly used drugs in the world due to their anti-inflammatory, analgesic and antipyretic properties. However, its application is largely limited by gastrointestinal and kidney toxicity. In recent years, the new generation of NSAIDs, selective/specific COX-2 inhibitors, appeared to increase the incidence of cardiovascular disease （heart attack and stroke） and other security issues. There are many intensive studies on physiological and pathological mechanism of COX-1, which has been found that it has a close relationship with many kinds of disease, such as pain, thrombosis, atherogenesis, neuroinflammation and cancer. Inhibiting COX-1 selectively provides new ideas for treating those diseases. Therefore, COX-1 and its selective inhibitors become a hot spot of modem research. In this article, the role of COX-1, including physiological pathology function, structure-activity relationship as well as the progress of selective COX-1 inhibitors were reviewed.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2016年第10期727-734,750,共9页
Chinese Journal of Antibiotics
基金
国家自然科学基金(No.81502944)
关键词
COX-1
选择性COX-1抑制剂
炎症
癌症
构效关系
COX- 1
Selective COX- 1 inhibitors
Inflammation
Cancer
Structure-activity relationships
