Journal
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
Volume 143, Issue -, Pages 269-276Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jpba.2017.06.001
Keywords
Hollow fiber; Ligand fishing; Liquid chromatography-mass spectrometry; alpha-Glucosidase inhibitors; Angiotensin-converting enzyme inhibitors; Traditional Chinese medicines
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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. (C) 2017 Elsevier B.V. All rights reserved.
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