LTFPGSAED (P7) is a multifunctional hypocholesterolemic and hypoglycemic lupin peptide. While assessing its angiotensin-converting enzyme (ACE) inhibitory activity, it was more effective in intestinal Caco-2 cells (IC50 of 13.7 μM) than in renal HK-2 cells (IC50 of 79.6 μM). This discrepancy was explained by the metabolic transformation mediated by intestinal peptidases, which produced two main detected peptides, TFPGSAED and LTFPG. Indeed LTFPG, dynamically generated by intestinal dipeptidyl peptidase IV as well as its parent peptide P7 were linearly absorbed by mature Caco-2 cells. An in silico study demonstrated that the metabolite was a better ligand of the ACE enzyme than P7. These results are in agreement with an in vivo study, previously performed by Aluko et al., which has shown that LTFPG is an effective hypotensive peptide. Our work highlights the dynamic nature of bioactive food peptides that may be modulated by the metabolic activity of intestinal cells.

Assessment of multifunctional behavior of lupin P7 and its metabolite using an integrate strategy / C. Lammi, G. Aiello, L. Dellafiora, C. Bollati, G. Boschin, G. Ranaldi, S. Ferruzza, Y. Sambuy, G. Galaverna, A. Arnoldi. - In: JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY. - ISSN 0021-8561. - 68:46(2020), pp. 13179-13188. [10.1021/acs.jafc.0c00130]

Assessment of multifunctional behavior of lupin P7 and its metabolite using an integrate strategy

C. Lammi
Primo
;
G. Aiello
Secondo
;
C. Bollati;G. Boschin;A. Arnoldi
Ultimo
2020

Abstract

LTFPGSAED (P7) is a multifunctional hypocholesterolemic and hypoglycemic lupin peptide. While assessing its angiotensin-converting enzyme (ACE) inhibitory activity, it was more effective in intestinal Caco-2 cells (IC50 of 13.7 μM) than in renal HK-2 cells (IC50 of 79.6 μM). This discrepancy was explained by the metabolic transformation mediated by intestinal peptidases, which produced two main detected peptides, TFPGSAED and LTFPG. Indeed LTFPG, dynamically generated by intestinal dipeptidyl peptidase IV as well as its parent peptide P7 were linearly absorbed by mature Caco-2 cells. An in silico study demonstrated that the metabolite was a better ligand of the ACE enzyme than P7. These results are in agreement with an in vivo study, previously performed by Aluko et al., which has shown that LTFPG is an effective hypotensive peptide. Our work highlights the dynamic nature of bioactive food peptides that may be modulated by the metabolic activity of intestinal cells.
ACE; DPP-IV; bioactive peptides; hypotensive; intestinal transport; peptide
Settore CHIM/10 - Chimica degli Alimenti
2020
30-mar-2020
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/796922
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