液相色谱-酶亲和检测联用技术研究进展

发布时间：2018-03-05 13:38

本文选题：液相色谱　切入点：酶亲和检测(EAD)　出处：《药物分析杂志》2017年06期 　论文类型：期刊论文

【摘要】：液相色谱-酶亲和检测(high performance liquid chromatography-enzyme affinity detection,HPLC-EAD)联用技术是近年来逐渐建立的,根据酶对具有某一相同立体结构的底物具有亲和性,进而出现竞争性抑制现象的原理,用于筛选复杂体系中对某种酶具有亲和性的底物的一种新技术。本文调研了与该联用技术相关的大量文献,并从该技术的概述、应用和展望这3个方面进行综述。经过分析与总结发现这种技术虽然起步较晚,但是发展迅速,目前多用于药物代谢酶的抑制剂,中药活性成分的筛选和药物筛选。细胞色素P450酶、黄嘌呤氧化酶、α-葡萄糖苷酶等生物酶都在人体内发挥着十分重要的作用,通过筛选能够与这些酶高效结合的底物,进而研究其具体结合模型以及在体内的作用机制,是药物研发的重要手段。由于酶亲和技术本身存在的一些还未解决的缺陷,比如安全性与有效性、渗漏与变性、成本较高的问题,因而在一定程度上限制了它的发展与大规模应用。但是由于它的亲和特性,这一技术仍然在体内重要的代谢酶抑制剂的筛选、复方中药产生临床疗效的主要活性成分群的筛选等方面具有重要的理论意义和应用价值。
[Abstract]:High performance liquid chromatography-enzyme affinity detection HPLC-EAD has been developed in recent years. According to the principle of enzyme affinity to a substrate with the same stereoscopic structure, competitive inhibition occurs. A new technique for screening substrates with affinity for an enzyme in a complex system. The application and prospect of these three aspects were reviewed. After analysis and summary, it was found that although this technology started relatively late, it was developing rapidly. At present, it is mostly used as inhibitor of drug metabolizing enzyme. Biological enzymes such as cytochrome P450 enzyme, xanthine oxidase, 伪 -glucosidase play a very important role in human body. It is an important means of drug development to study the specific binding model and the mechanism of its action in vivo. Due to some unsolved defects of enzyme affinity technology itself, such as safety and effectiveness, leakage and denaturation, The problem of high cost limits its development and large-scale application to a certain extent. However, due to its affinity, this technique is still used in the screening of important metabolic enzyme inhibitors in vivo. The screening of the main active component groups which produce clinical curative effect of compound Chinese medicine has important theoretical significance and application value.
【作者单位】：中南大学湘雅医院临床药理研究所;中南大学临床药理研究所遗传药理学湖南省重点实验室;
【基金】：国家自然科学基金(81403086):基于HPLC-TPMT EAD-MS联用技术的天芪降糖胶囊中TPMT酶亲和活性成分研究
【分类号】：O657.72;R917

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