基于毛细管电泳的天然产物中酶抑制剂筛选研究进展

人类疾病的发生往往与体内各种酶的功能失调密切相关，因此酶一直是目前新药研发的重要靶标。天然产物是发现新药的宝贵资源，但是由于成分复杂，活性筛选一直受制于耗时费力的分离纯化过程。毛细管电泳（CE）技术由于具有样品和试剂消耗少、灵活多样的分离模式且不受样品基质干扰的特点，可以直接从粗提物开始筛选活性成分，在复杂样品活性筛选中显示出独特的优势。该文综述了近十年来CE在天然产物中酶抑制剂筛选的研究进展。其中重点介绍了CE应用于重要药物靶标，包括转移酶（激酶）、水解酶以及氧化还原酶等方面的应用，总结了用于酶抑制剂筛选的电泳分离模式和酶动力学研究，并展望了CE用于天然产物中活性成分筛选的应用前景。

Application of capillary electrophoresis in enzyme inhibitors screening from natural products

As aberrant enzyme functions are often closely associated with various diseases, enzymes represent one of the most important drug target groups. Historically, natural products have been the most productive sources for drug discovery. However, the complexity of the components leads to a bottleneck in separation and purification, thus restricting activity-based drug screening. Due to the unique advantages such as high separation efficiency and without sample matrix interference, the advantage of capillary electrophoresis (CE) directly applied to extracts without purification for activity-based drug screening is of great attractive. In this review, we have summarized the application of CE for screening enzyme inhibitors in natural products during the last decade. In particular, we discuss important examples for screening inhibitors of transferases (kinases), hydrolases, oxidoreductases, etc. We also present an overview of the technical details concerning the separation modes in CE and enzyme kinetics. Finally, we provide future prospects for the application of CE to the screening of active ingredients in natural products.