Selection of goat β-casein derived ACE-inhibitory peptide SQPK and insights into its effect and regulatory mechanism on the function of endothelial cells

Int J Biol Macromol. 2023 Dec 31;253(Pt 6):127312. doi: 10.1016/j.ijbiomac.2023.127312. Epub 2023 Oct 10.

Abstract

The angiotensin I-converting enzyme (ACE)-inhibitory peptide SQPK was selected by in silico digestion and virtual screening from goat β-casein, and its effect and regulatory mechanism on function of endothelial cells was further evaluated. The results showed that SQPK exhibited relatively good ACE inhibition capacity (IC50 = 452.7 μg/mL). Treatment with 25 μg/mL SQPK for 12 h significantly elevated nitric oxide (NO) production, stimulated eNOS expression (p < 0.05) and affected the transcriptomic profiling of EA. Hy926 cells. In particular, SQPK stimulated the expression of genes encoding inflammatory cytokines (CXCL1/2 and IL6) but depressed encoding mesenchymal markers (FN1 and CNN3). Furthermore, SQPK modified the expression of genes involved in endothelial-to-mesenchymal transition (EndMT). Therefore, the selected peptide SQPK may exert potential protective effects on the function of endothelial cells by inhibiting the EndMT.

Keywords: ACE inhibitory peptide; Endothelial cells; Goat β-casein; SQPK; Transcriptomic profiling.

MeSH terms

  • Angiotensin-Converting Enzyme Inhibitors* / pharmacology
  • Animals
  • Caseins* / metabolism
  • Endothelial Cells / metabolism
  • Goats / metabolism
  • Peptides / metabolism
  • Peptides / pharmacology
  • Peptidyl-Dipeptidase A / genetics
  • Peptidyl-Dipeptidase A / metabolism

Substances

  • Caseins
  • Angiotensin-Converting Enzyme Inhibitors
  • Peptidyl-Dipeptidase A
  • Peptides