In vitro intestinal transport and antihypertensive activity of ACE inhibitory pea and whey digests.
Angiotensin I converting enzyme (ACE) inhibitory peptides cause an antihypertensive effect if they reach the systemic circulation. This was investigated for the high ACE inhibitory activity present in peas and whey in vitro gastrointestinal digests. The samples retained high ACE inhibitory activity when incubated in Caco-2 homogenates or rat intestinal acetone powder, both sources of small intestine peptidases. Only little ACE inhibitory activity was transported through Caco-2 cell monolayers in 1 h. As the Caco-2 model is tighter than intestinal mammalian tissue, sufficient absorption of these peptides might occur in vivo. After intravenous administration of 50 mg protein kg(-1) BW in spontaneously hypertensive rats (SHR), pea digest exerted a transient, but strong antihypertensive effect of 44.4 mmHg. Whey digest exerted no effect at this dose. These results suggest that pea digest could be a promising source of ACE inhibitory peptides for use in the prevention and treatment of hypertension.
Vermeirssen
Vanessa
V
Laboratory for Pharmacotechnology and Biopharmacy, Catholic University of Leuven, Faculty of Pharmaceutical Sciences, Leuven, Belgium.
Augustijns
Patrick
P
Morel
Nicole
N
Van Camp
John
J
Opsomer
Anne
A
Verstraete
Willy
W
D000096:Acetone; D000806:Angiotensin-Converting Enzyme Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000818:Animals; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001692:Biological Transport / Q000502:physiology; D001794:Blood Pressure / Q000187:drug effects / Q000502:physiology; D018938:Caco-2 Cells / Q000378:metabolism; D004063:Digestion / Q000502:physiology; D017097:Electric Impedance; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007275:Injections, Intravenous; D008894:Milk Proteins / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics*; D009994:Osmolar Concentration; D018532:Pisum sativum / Q000737:chemistry*; D051381:Rats; D011918:Rats, Inbred SHR; D000067816:Whey Proteins
D000806:Angiotensin-Converting Enzyme Inhibitors; D000959:Antihypertensive Agents; D008894:Milk Proteins; D000067816:Whey Proteins; D000096:Acetone