降尿酸化合物的活性评价方法研究进展
Recent advances in bioactivity evaluation methods of uric acid-lowering compounds
祁丹辉 1史晓雨 1刘新泳 1展鹏1
作者信息
- 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,济南 250012
- 折叠
摘要
高尿酸血症(hyperuricemia,HUA)是由于体内尿酸升高所导致的一种代谢性疾病,与心血管疾病、代谢紊乱和肾脏并发症风险升高密切相关.活性评价是降尿酸药物研发至关重要的环节.目前,降尿酸药物的活性筛选方法大致分为体外和体内两种,体外筛选主要是基于黄嘌呤氧化酶、尿酸转运蛋白、嘌呤核苷磷酸化酶等靶点建立模型,而体内降尿酸筛选则通过啮齿类、禽类动物及类器官等模型实现.因此,从体内、体外两个方面全面综述了降尿酸化合物的活性评价方法,旨在为降尿酸药物的研发提供信息.
Abstract
Hyperuricemia is a metabolic disease caused by elevated uric acid in the body,and is closely related to the increased risk of cardiovascular disease,metabolic disorders,and renal complications.In the development process of uric acid-lowering drugs,activity evaluation is a crucial step.At present,the activity screening methods of uric acid-lowering drugs can be roughly divided into two categories:in vitro and in vivo.In vitro screening is mainly for such targets as xanthine oxidase,urate transporters,and purine nucleoside phosphorylase,etc.;while in vivo screening is achieved by rodent,poultry and organoid models.In this article,the activity evaluation methods for uric acid-lowering compounds are comprehensively summarized both in vitro and in vivo,aiming to provide some insight for the development of uric acid-lowering drugs.
关键词
高尿酸血症/痛风/降尿酸/活性评价/药物研发Key words
hyperuricemia/gout/uric acid lowering/activity evaluation/drug discovery引用本文复制引用
基金项目
山东省杰出青年科学基金(ZR2020JQ31)
出版年
2024
国家科技期刊平台
NSTL
万方数据