AUTHOR=Shi Rujie , Zhou Nong , Zhang Han , Gong Min , Han Lin 

TITLE=Bioaffinity ultrafiltration coupled with HPLC-ESI-MS/MS for screening potential α-glucosidase inhibitors from pomegranate peel

JOURNAL=Frontiers in Nutrition

VOLUME=Volume 9 - 2022

YEAR=2022

URL=https://www.frontiersin.org/journals/nutrition/articles/10.3389/fnut.2022.1014862

DOI=10.3389/fnut.2022.1014862

ISSN=2296-861X

ABSTRACT=Pomegranate peel (PoP) contains plenty of bioactive compounds and exhibits strong activity to prevent postprandial hyperglycaemia and improve diabetes mellitus. Presently, bioaffinity ultrafiltration coupled with HPLC-ESI-MS/MS is employed to screen and identify the efficient α-glucosidase inhibitors in PoP and the detailed inhibitory mechanisms are further investigated. The results show that many substances in PoP reveal strong activity to inhibit α-glucosidase and ellagic acid (EA) is screened as the most effective compound. Further research indicates that EA plays a competitive and reversible inhibition role against α-glucosidase with the value of Ki was 6.24×105 mol/L. EA also directly interacts with the amino acids of α-glucosidase mainly via van der Waals forces and hydrogen bonds, thereby, influencing the secondary structure and stability of α-glucosidase. Finally, the α-glucosidase inhibitory activity of EA is further confirmed to significantly reduce postprandial blood glucose in vivo.