Abstract:

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.

Key words: capillary electrophoresis (CE), drug screening, enzyme inhibitors, natural products