Dual-target screening of bioactive components from traditional Chinese medicines by hollow fiber-based ligand fishing combined with liquid chromatography-mass spectrometry

作者：Chen, Liang; Wang, Xin; Liu, Youping; Di, Xin^*

来源：Journal of Pharmaceutical and Biomedical Analysis, 2017, 143: 269-276.

DOI：10.1016/j.jpba.2017.06.001

• Hollow fiber
• Ligand fishing
• Liquid chromatography-mass spectrometry
• alpha-Glucosidase inhibitors
• Angiotensin-converting enzyme inhibitors
• Traditional Chinese medicines

A novel strategy was developed for dual-target screening of bioactive components from traditional Chinese medicines (TCMs). This strategy was based on the use of low-cost microporous hollow fibers filled with target enzymes as baits to "fish out" the ligands in TCM extracts, followed by identification of the ligands dissociated from the target-ligand complexes by liquid chromatography-mass spectrometry. Ganjiang Huangqin Huanglian Renshen Decoction (GHHRD), a classical TCM prescription for diabetes treatment, was chosen as a model sample to evaluate the feasibility of the proposed strategy. Three bioactive components were successfully screened out from GHHRD. Coptisine was identified as the ligand of a-glucosidase and baicalin as the ligand of angiotensin-converting enzyme (ACE). Berberine was found to be a dual inhibitor of alpha-glucosidase and ACE. The results were further verified by enzyme inhibitory assay and molecular docking simulation. The study suggested that our developed strategy would be a powerful tool for screening bioactive components from multi-component and multi-target TCMs.

• 出版日期2017-9-5
• 单位沈阳药科大学