| Pharmacokinetics of proline-rich tripeptides in the pig. | |
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MedLine Citation:
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PMID: 18789987 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Tripeptides may possess bioactive properties. For instance, blood pressure lowering is attributed to the proline-rich tripeptides Ile-Pro-Pro (IPP), Leu-Pro-Pro (LPP), and Val-Pro-Pro (VPP). However, little is known about their absorption, distribution, and elimination characteristics. The aim of this study was to characterize the pharmacokinetic behavior of IPP, LPP, and VPP in a conscious pig model. Synthetic IPP, LPP, and VPP were administered intravenously or intragastrically (4.0 mg kg(-1) BW in saline) to 10 piglets (approximately 25 kg body weight) in the postabsorptive state. After intravenous dosing, the elimination half-life for IPP was significantly higher (P<0.001) than for LPP and VPP (2.5+/-0.1, 1.9+/-0.1, and 2.0+/-0.1 min, respectively). After intragastric dosing, however, the elimination half-lives were not significantly different between the peptides (9+/-1, 15+/-4, and 12+/-6 min, respectively). Maximum plasma concentrations were about 10 nmol l(-1) for the three tripeptides. The fraction dose absorbed was 0.077+/-0.010, 0.059+/-0.009, and 0.073+/-0.015%, for IPP, LPP, and VPP, respectively. Proline-rich tripeptides reach the blood circulation intact, with an absolute bioavailability of about 0.1% when administered via a saline solution. Because half-lives of absorption and elimination were maximally about 5 and 15 min, respectively, this suggests that under these conditions a bioactive effect of these tripeptides would be rather acute. |
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Authors:
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Pieter C van der Pijl; Arie K Kies; Gabriella A M Ten Have; Guus S M J E Duchateau; Nicolaas E P Deutz |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2008-08-23 |
Journal Detail:
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Title: Peptides Volume: 29 ISSN: 0196-9781 ISO Abbreviation: Peptides Publication Date: 2008 Dec |
Date Detail:
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Created Date: 2008-11-21 Completed Date: 2009-02-19 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8008690 Medline TA: Peptides Country: United States |
Other Details:
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Languages: eng Pagination: 2196-202 Citation Subset: IM |
Affiliation:
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Unilever Food & Health Research Institute, Olivier van Noortlaan 120, 3133 AT Vlaardingen, The Netherlands. pieter-van-der.pijl@unilever.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Antihypertensive Agents / pharmacokinetics* Female Oligopeptides / pharmacokinetics* Swine |
| Chemical | |
Reg. No./Substance:
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0/Antihypertensive Agents; 0/Oligopeptides; 0/isoleucyl-prolyl-proline; 0/leucyl-prolyl-proline; 0/valyl-prolyl-proline |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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