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Article Abstract
Background: KALVAP is an angiotensin-converting enzyme inhibitor derived from Ziziphus jujuba, but shows poor dipeptidyl peptidase (DPP)-IV inhibitory activity. To remedy this shortcoming, KALVAP was modified according to the distinctive features of DPP-IV inhibitory peptides, yielding nine novel peptides. The DPP-IV inhibitory activity of the peptides was further verified in vitro and in vivo.
Results: The in vitro DPP-IV inhibitory activities of WALVAP and WPLVAP were respectively 6.25- and 3.52-fold higher than that of KALVAP (360.39 ± 14.39 μmol L) after screening through molecular docking. Moreover, WALVAP (201.88 ± 8.27 μmol L) and WPLVAP (450.61 ± 16.83 μmol L) displayed superior DPP-IV inhibitory activity to KALVAP (1372.57 ± 49.52 μmol L) in Caco-2 cells. On the basis of in vitro and cellular experiments, oral glucose tolerance tests indicated that WALVAP and WPLVAP significantly improved glucose metabolism in C57BL/6 mice by promoting the secretion of insulin (11.13 ± 0.89% and 11.61 ± 0.44%), GLP-1 (11.12 ± 0.89% and 11.61 ± 0.44%) and GIP (7.58 ± 0.78% and 7.66 ± 0.11%). Molecular dynamics simulations revealed that WALVAP and WPLVAP mainly inhibited DPP-IV through Glu205, Trp629, Glu206, Arg125 and Arg429.
Conclusion: In summary, two new peptides, WALVAP and WPLVAP, were screened and exhibited excellent DPP-IV inhibitory activity. The results implied that the optimization strategy is feasible and can provide a reference for drug design. Thus WALVAP and WPLVAP could serve as potential drug candidates for patients with hypertension and diabetes mellitus. © 2025 Society of Chemical Industry.
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