Abstract
Identification of active compounds from natural products is a critical and challenging task in drug discovery pipelines. Besides commonly used bio-guided screening approaches, affinity selection strategy coupled with liquid chromatography or mass spectrometry, known as ligand fishing, has been gaining increasing interest from researchers. In this review, we summarized this emerging strategy and categorized those methods as off-line or on-line mode according to their features. The separation principles of ligand fishing were introduced based on distinct analytical techniques, including biochromatography, capillary electrophoresis, ultrafiltration, equilibrium dialysis, microdialysis, and magnetic beads. The applications of ligand fishing approaches in the discovery of lead compounds were reviewed. Most of ligand fishing methods display specificity, high efficiency, and require less sample pretreatment, which makes them especially suitable for screening active compounds from complex mixtures of natural products. We also summarized the applications of ligand fishing in the modernization of Traditional Chinese Medicine (TCM), and propose some perspectives of this remarkable technique.
Highlights
Natural products have played an indispensable role in healthcare systems throughout history, providing a huge and invaluable resource for the discovery of novel drug candidates
In the past two decades, tremendous efforts have been made for the identification of active components from Traditional Chinese Medicine (TCM), which is highlighted by artemisinin with its antimalarial effect as the most successful and impressive example and a gift from TCM to the world [2]
We focused on the ligand fishing technique, an emerging field in affinity separation techniques
Summary
Natural products have played an indispensable role in healthcare systems throughout history, providing a huge and invaluable resource for the discovery of novel drug candidates. Due to the chemical complexity of TCMs and other natural products, methods with satisfied sensitivity and efficiency for lead discovery are still in demand. Affinity-based screening assay, depending on the principle of macromolecular target-ligand binding, has been considered as one of the most convenient and efficient methods to separate potential ligands from complex mixture. These affinity-based screening assays can be applied to investigate multiple interacting pairs involved in biological systems, including antigen-antibody, receptor-ligand, enzyme-inhibitor/activator, and protein-protein interactions [4]. Taking advantage of diverse target immobilization methods and quick development of state-of-art analytical approaches, ligand fishing has emerged as a convenient and efficient technique to fish out ligands from complex mixtures. The following analysis step is generally performed by analytical instruments such as HPLC or MS
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