Open AccessMagnetic ligand fishing using immobilized DPP-IV for identification of antidiabetic ligands in lingonberry extract
Author(s) -
Rita de Cássia Lemos Lima,
Ulrike Böcker,
Gordon J. McDougall,
J. William Allwood,
Nils Kristian Afseth,
Sileshi Gizachew Wubshet
Publication year - 2021
Publication title -
plos one
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.99
H-Index - 332
ISSN - 1932-6203
DOI - 10.1371/journal.pone.0247329
Subject(s) - chemistry , ligand (biochemistry) , glucoside , biochemistry , combinatorial chemistry , chromatography , receptor , medicine , alternative medicine , pathology
In this work, a new magnetic ligand fishing probe for discovery of DPP-IV inhibitory ligands was developed and it was tested as a proof of concept on the fruit extract of Vaccinium vitis-idaea (lingonberry). The ligands were shown to have appreciable dipeptidyl peptidase IV (DPP-IV) inhibitory activity (IC 50 : 31.8 μg mL-1).) Inhibition of DPP-IV is a well-known therapeutic approach for management of type 2 diabetes (T2D). DPP-IV was successfully immobilized onto magnetic beads and was shown to retain its catalytic activity and selectivity over a model mixture. A total of four ligands were successfully fished out and identified as cyanidin-3-galactoside ( 2 ), cyanidin-3-arabinoside ( 3 ), proanthocynidin A ( 4 ), and 10-carboxyl-pyranopeonidin 3- O -(6″- O -p-coumaroyl)-glucoside ( 5 ) using HPLC/HRMS.