Related Experiment Video
Updated: Jun 16, 2025

An In Ovo Model for Testing Insulin-mimetic Compounds
Published on: April 23, 2018
Potential antidiabetic activity and permeability assessment of the modified yeast-derived peptide, VLSTSFPPW (VW9)
Samira Alahyaribeik1, Saeed Mirdamadi2, Hyunjin Shim3
1Department of Environmental Technology, Food Technology, and Molecular Biotechnology, Ghent University Global Campus, 21985, Incheon, South Korea.
Abstract:
This study investigates the antidiabetic activity, gastrointestinal stability, and permeability of a modified yeast-derived peptide, VLSTSFPPW (VW9), using in vitro gastrointestinal digestion and Caco-2 cell models. LC-MS/MS analysis revealed that VW9 with DPP-IV inhibitory activity, was extensively cleaved during digestion into smaller fragments like PPW, FPPW, FPP, ST, and SFPP. Among these, PPW displayed the highest activity in vitro (IC50: 22.60 ± 0.18 μM) and in situ (IC50: 474 ± 10.2 μM). Kinetic and molecular docking studies indicated that PPW may inhibit the DPP-IV enzyme in a competitive way mainly due to hydrogen-bond interactions between Trp residue at C-terminus of PPW and the active site residues of DPP-IV. PPW could not penetrate epithelial cells, but a modified derivative was found on both apical and basolateral sides without DPP-IV inhibitory activity. These findings highlight the challenges of stability, activity, and permeability of VW9 and its derived peptides for potential therapeutic applications.
Related Concept Videos
Glucagon-like Receptor Agonists
GLP-1, when administered in high doses intravenously, triggers insulin secretion, inhibits glucagon release, slows gastric emptying, reduces food intake, and restores normal insulin secretion. However, its rapid inactivation by...
Dipeptidyl Peptidase 4 Inhibitors
Oral Hypoglycemic Agents: α-Glucosidase Inhibitors
Acarbose and miglitol are...
Oral Hypoglycemic Agents: Biguanides and Glitazones
Oral Hypoglycemic Agents: Glinides
Glucose Transporters
Facilitated diffusion-glucose transporters (GLUTs) are encoded by the solute-linked carrier (SLC) family 2, subfamily A gene family, or SLC2A. The 14 GLUT protein members are distributed into three classes:

