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Among the commercially available 10 components presented in Rhei Radix et Rhizoma, gallic acid, (+)-catechin and epicatechin exhibited the strongest inhibitory effect on α-glucosidase. Their binding sites and modes with α-glucosidase were simulated via molecular docking to further verify the inhibition screening assay results. The positive results indicated that the Fe3O4@CS@ZIF-8-based screening strategy may provide a new avenue for discovering enzyme inhibitors from TCMs.Ferulic acid (FA) is a ubiquitous natural plant bioactive with di