Characterization of DPP-IV Inhibitory Peptides Using an In Vitro Cell Culture Model of the Intestine

• DOI: 10.1021/acs.jafc.0c05880
• Publication Date: 2021-02-25T15:59:49Z
• Authors: Ritian Jin; Jiaqi Shang; Xiangyu Teng; Ligang Zhang; Minhe Liao; Jiaxin Kang; Ran Meng; Dangfeng Wang; Haowei Ren; Ning Liu
• Keywords: Occludin; IC50

Here, we characterize the activities of two depeptidyl peptidase-IV (DPP-IV) inhibitory peptides, VLATSGPG and LDKVFER, using Caco-2 monolayer model for intestine. LDKVFR inhibited DPP-IV in cells via a mixed-type inhibition mode, with situ IC50 values 207.3 148.5 μM, respectively. Furthermore, were transported intact across cells, Papp 2.41 ± 0.16 4.23 0.29 × 10–7 cm/s, Fragmented peptides identified basolateral side membrane. Two these, GPG VLA, exhibited high 83.6 3.3 58.5 2.5%, respectively, at 100 μM concentration. Although 3 mM epithelium concentration-dependent manner, their transport did not damage tight junction proteins, ZO-1 occludin. This study demonstrates that potentially regulate activity