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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

  • 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.

     

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