A highly sensitive detection system for α-amylase was developed via host–guest complexation between γ-cyclodextrin and dansyl-modified diphenylalanine (FF-Dns). The host–guest inclusion of FF-Dns into the cavity of γ-CD in a HEPES buffer solution (10 mM, pH 7.4) significantly enhanced the fluorescence intensity, and the emission wavelength gradually shifted from 558 to 535 nm. The hydrolysis of γ-CD by the addition of α-amylase released FF-Dns, leading to the recovery of the fluorescence emission characteristics. Therefore, the FF-Dns/γ-CD host–guest complexation system can serve as a platform for the sensitive detection of α-amylase with good selectivity against potential interference. The limit of detection (LOD) of the system was 0.004 U/mL, with a linear working range of 0–6 U/mL. The detection assay was successfully applied in 0.1 % serum, achieving an LOD of 0.017 U/mL and a linear working range of 0–10 U/mL.
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