靶向NLRP3炎症小体的抗痛风小分子化合物研究进展  

Research progress of anti-gout small molecules targeting the NLRP3 inflammasome

作　　者：王振谦 张志姣 刘新泳[1] 展鹏[1] WANG Zhen-qian;ZHANG Zhi-jiao;LIU Xin-yong;ZHAN Peng(Department of Medicinal Chemistry,Key Laboratory of Chemical Biology(Ministry of Education),School of Pharmaceutical Sciences,Shandong University,Jinan 250012,China)

机构地区：[1]山东大学药学院,药物化学研究所,化学生物学教育部重点实验室,山东济南250012

出　　处：《药学学报》2024年第3期543-553,共11页Acta Pharmaceutica Sinica

基　　金：山东省杰出青年基金(ZR2020JQ31);山东省重大科技创新工程项目(2019JZZY021011).

摘　　要：目前治疗痛风炎症的临床常用药物如秋水仙碱、非甾体抗炎药及糖皮质激素仅能缓解关节炎症疼痛,并且具有严重的肝肾毒性和多器官不良反应。NOD样受体热蛋白结构域相关蛋白3(NOD-like receptor thermal protein domain associated protein 3,NLRP3)炎症小体是诱导痛风炎症发作的关键信号因子,已成为抗痛风药物研发的重要靶标。本文综述了近5年靶向NLRP3炎症小体的抗痛风小分子化合物及其活性评价方法的研究进展,以期为研发治疗痛风炎症的特异性药物提供参考。Currently,clinically used drugs for the treatment of gout inflammation,such as colchicine,nonsteroidal anti-inflammatory drugs,and glucocorticoids,can only relieve the pain of joint inflammation and have severe hepatorenal toxicity and multiple organ adverse reactions.The NOD-like receptor thermal protein domain associated protein 3(NLRP3)inflammasome is a key complex that induces the onset of gout inflammation and has become a crucial target in the development of anti-gout drugs.This article reviews the research progress of antigout small molecules targeting the NLRP3 inflammasome and their bioactivity evaluation methods in the past five years,in order to provide information for the development of specific drugs for the treatment of gout inflammation.

关 键 词：NOD样受体热蛋白结构域相关蛋白3 炎症小体 痛风 尿酸钠 小分子化合物 生物活性评价 

分 类 号：R914[医药卫生—药物化学]