The antihypertensive effect of the bovine casein-derived peptide Met-Lys-Pro (MKP) was examined in vitro and in vivo. MKP showed angiotensin I-converting enzyme (ACE)-inhibitory activity in vitro (IC50 = 0.43 μM). An in vivo kinetics study using radiolabeled Met-[1-(14)C]Lys-Pro ((14)C-MKP) showed that orally administered (14)C-MKP to spontaneously hypertensive rats (SHRs) was absorbed and moved into the plasma. In vitro vasoconstriction of thoracic aorta preparations, which was induced by adding angiotensin I, was reduced by prior exposure of MKP. A single oral dose of MKP lowered systolic blood pressure (SBP) of SHRs, and repeated oral administration of MKP for 28 days significantly lowered SBP of SHRs. The results obtained in the present study suggest that orally administrated MKP can be absorbed into the plasma and its ACE-inhibitory activity may contribute to induce the antihypertensive effect in vivo.
Keywords: (14)C-labeled peptide; ACE-inhibitory peptide; Angiotensin I-converting enzyme; Bioavailability; Casein; Hypertension; Ile-Pro-Pro (CID 24978506); Val-Pro-Pro (CID 9818200); Val-Tyr (CID 4065033).
Copyright © 2014 Elsevier Ltd. All rights reserved.