An activity-integrated strategy involving ultra-high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry and fraction collector for rapid screening and characterization of the α-glucosidase inhibitors in Coptis chinensis Franch. (Huanglian)

Abstract

An activity integrated strategy was established and validated to screen α-glucosidase inhibitors by ultra-high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry and fraction collector (UHPLC/Q-TOF-MS-FC). UHPLC was used to separate the components in Coptis chinensis Franch. (Huanglian in Chinese) extract, which was identified by UHPLC-Q-TOF-MS to acquire structural information and collected by the fraction collector. Finally, the collected fractions were tested for inhibitory activity of α-glucosidase. The results showed that Huanglian extract had the α-glucosidase inhibitory activity with the IC50 value at 3.528mg mL(-1), which could be used for the treatment of diabetes. Alkaloids were the main components that had inhibitory activity of α-glucosidase in Huanglian extract, while the inhibitory activity of phenolic acids against α-glucosidase was relatively weaker. Coptisine, epiberberine, jatrorrhizin and berberine were screened and identified as α-glucosidase inhibitors from Huanglian extract in vitro. Compared with conventional methods, the integrated UHPLC/Q-TOF-MS-FC method could quantitatively analyze α-glucosidase inhibitory activity of individual constituent and provide the total α-glucosidase inhibitory activity of the samples. The results demonstrated that the activity integrated UHPLC/Q-TOF-MS-FC method was an effective and powerful tool for screening and identifying active ingredients from Traditional Chinese medicines.

Keywords: Alkaloids; Coptis chinensis Franch. (Huanglian); Diabetes; Phenolic acids; UHPLC/Q-TOF-MS-FC; α-Glucosidase inhibitors.