Lima Rita de Cássia Lemos, Böcker Ulrike, McDougall Gordon J, Allwood J William, Afseth Nils Kristian, Wubshet Sileshi Gizachew
NOFIMA AS, Ås, Norway.
Plant Biochemistry and Food Quality Group, Environmental and Biochemical Sciences Department, The James Hutton Institute, Invergowrie, Dundee, Scotland, United Kingdom.
PLoS One. 2021 Feb 22;16(2):e0247329. doi: 10.1371/journal.pone.0247329. eCollection 2021.
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.
在本研究中，开发了一种用于发现二肽基肽酶IV（DPP-IV）抑制性配体的新型磁性配体垂钓探针，并以越橘（红豆越橘）果实提取物作为概念验证对其进行了测试。结果表明，这些配体具有显著的二肽基肽酶IV（DPP-IV）抑制活性（IC50：31.8 μg mL-1）。抑制DPP-IV是治疗2型糖尿病（T2D）的一种众所周知的治疗方法。DPP-IV成功固定在磁珠上，并在模型混合物中显示出保留其催化活性和选择性。使用HPLC/HRMS共成功钓出并鉴定出四种配体，分别为矢车菊素-3-半乳糖苷（2）、矢车菊素-3-阿拉伯糖苷（3）、原花青素A（4）和10-羧基-吡喃芍药素3-O-（6″-O-对香豆酰基）-葡萄糖苷（5）。
