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The pharmacokinetics of anthocyanins and their metabolites in humans.
MedLine Citation:
PMID:  24602005     Owner:  NLM     Status:  Publisher    
BACKGROUND AND PURPOSE: Anthocyanins are phytochemicals with reported vasoactive bioactivity. However, given their instability at neutral pH, they are presumed to undergo significant degradation and subsequent biotransformation. The aim of the present study was to establish the pharmacokinetics of the metabolites of cyanidin-3-glucoside (C3G), a widely consumed dietary phytochemical with potential cardio-protective properties.
EXPERIMENTAL APPROACH: A 500 mg oral bolus dose of 6,8,10,3',5'-(13) C5 -C3G was fed to eight healthy male participants, followed by a 48 h collection (0, 0.5, 1, 2, 4, 6, 24, 48 h) of blood, urine, and faecal samples. Samples were analysed by HPLC-ESI-MS/MS with elimination kinetics established using non-compartmental pharmacokinetic modelling.
KEY RESULTS: 17 (13) C-labelled compounds were identified in serum, including (13) C5 -C3G, its degradation products, protocatechuic acid and phloroglucinaldehyde, 13 metabolites of protocatechuic acid and one metabolite derived from phloroglucinaldehyde. The maximal concentrations of the phenolic metabolites (Cmax ) ranged from 11 ± 3 nM to 1,962 ± 1,389 nM, between 1.8 ± 0.2 h and 30.1 ± 11.4 h (tmax ) post consumption, with half-lives of elimination observed between 0.4 h and 95.6 ± 77.8 h. The major phenolic metabolites identified were hippuric acid (Cmax, 1,962 ± 1,389 nM) and ferulic acid (Cmax, 827 ± 371 nM), which peaked in serum at 15.7 ± 4.1 h and 8.2 ± 4.1 h respectively.
CONCLUSIONS AND IMPLICATIONS: Anthocyanins are metabolised to a structurally diverse range of metabolites that exhibit dynamic kinetic profiles. Understanding the elimination kinetics of these metabolites is key to the design of future studies examining their utility in dietary interventions or as therapeutics for disease risk reduction.
R M de Ferrars; C Czank; Q Zhang; N P Botting; P A Kroon; A Cassidy; C D Kay
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2014-3-7
Journal Detail:
Title:  British journal of pharmacology     Volume:  -     ISSN:  1476-5381     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  2014 Mar 
Date Detail:
Created Date:  2014-3-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
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This article is protected by copyright. All rights reserved.
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