Chemical and biological characterization of the DPP-IV inhibitory activity exerted by lupin (Lupinus angustifolius) peptides: From the bench to the bedside investigation

• Published in: Food chemistry 2023-11, Vol.426, p.136458-136458, Article 136458
• Main Authors: Cruz-Chamorro, Ivan, Santos-Sánchez, Guillermo, Bollati, Carlotta, Bartolomei, Martina, Capriotti, Anna Laura, Cerrato, Andrea, Laganà, Aldo, Pedroche, Justo, Millán, Francisco, del Carmen Millán-Linares, María, Arnoldi, Anna, Carrillo-Vico, Antonio, Lammi, Carmen
• Format: Article
• Language: English
• Subjects: Animals; Bioactive peptides; Caco-2 Cells; Diabetes; Diabetes Mellitus; Dipeptidyl Peptidase 4 - metabolism; Dipeptidyl-Peptidase IV Inhibitors - chemistry; Dipeptidyl-Peptidase IV Inhibitors - pharmacology; DPP-IV; Food clinical trial; Glucose; Glycemia; Humans; Lupin peptides; Lupinus - chemistry; Mice; Peptides - chemistry
• ISSN: 0308-8146; 1873-7072
• DOI: 10.1016/j.foodchem.2023.136458

•Lupinus angustifolius hydrolysate (LPH) contains 141 bioavailable peptides with DPP-IV inhibitor motifs.•LPH reduces in vitro and cellular DPP-IV activity.•LPH peptides are capable to cross the monolayer of intestinal barrier cells.•LPH modulates the glycemia by the direct DPP-IV activity inhibition in mice.•LPH consumption decreases the DPP-IV activity and glucose concentration in humans. Dipeptidyl peptidase IV (DPP-IV) is considered a key target for the diabetes treatment, since it is involved in glucose metabolism. Although lupin protein consumption shown hypoglycemic activity, there is no evidence of its effect on DPP-IV activity. This study demonstrates that a lupin protein hydrolysate (LPH), obtained by hydrolysis with Alcalase, exerts anti-diabetic activity by modulating DPP-IV activity. In fact, LPH decreased DPP-IV activity in a cell-free and cell-based system. Contextually, Caco-2 cells were employed to identify LPH peptides that can be intestinally trans-epithelial transported. Notably, 141 different intestinally transported LPH sequences were identified using nano- and ultra-chromatography coupled to mass spectrometry. Hence, it was demonstrated that LPH modulated the glycemic response and the glucose concentration in mice, by inhibiting the DPP-IV. Finally, a beverage containing 1 g of LPH decreased DPP-IV activity and glucose levels in humans.