Magnetic ligand fishing using immobilized DPP-IV for identification of antidiabetic ligands in lingonberry extract

Abstract

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 (IC50: 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.

Composition of Sugars, Organic Acids, Phenolic Compounds, and Volatile Organic Compounds in Lingonberries (Vaccinium vitis-idaea L.) at Five Ripening Stages

“…Flavour is also affected by volatile organic compounds (VOCs), but little is known about the aroma profile of lingonberries [9]. Lingonberries have a super-food potential, as several studies have found health beneficial effects of including them in the diet [10][11][12][13][14].…”

Efficient screening of pancreatic lipase inhibitors from cod meat hydrolysate through ligand fishing strategy

“…The traditional activity-guided separation procedures involve repeated fractionation steps and bioactivity tests, which are time-consuming, labor-consuming, and inefficient ( 18 – 20 ). Ligand fishing (LF) is an efficient screening technology developed in recent years, which has been successfully applied to rapidly discover active compounds from complex mixtures ( 21 – 23 ). Affinity ultrafiltration is a typical representative of LF, which has been successfully applied to the screening of XODI and ACEI peptides from protein hydrolysates ( 23 – 25 ).…”