The pharmacokinetics of anthocyanins and their metabolites in humans.
The pharmacokinetics of anthocyanins and their metabolites in humans.
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DOI：
10.1111/bph.12676
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发表时间：
2014-07
影响因子：
7.3
通讯作者：
Kay CD
中科院分区：
文献类型：
--
作者：
de Ferrars RM;Czank C;Zhang Q;Botting NP;Kroon PA;Cassidy A;Kay CD
花青素是一种具有血管活性的植物化学物质。然而，鉴于它们在中性pH值下的不稳定性，推测它们会发生显著的降解和随后的生物转化。本研究的目的是建立矢车菊素-3-葡萄糖苷（C3 G）的代谢产物的药代动力学，C3 G是一种广泛食用的具有潜在心脏保护特性的膳食植物化学物质。向8名健康男性参与者喂食500 mg口服推注剂量的6，8，10，3 ′，5 ′-13 C5-C3 G，随后收集48 h（0、0.5、1、2、4、6、24、48 h）的血液、尿液和粪便样品。通过HPLC-ESI-MS/MS分析样品，使用非房室药代动力学模型建立消除动力学。在血清中鉴定出17种~（13）C标记化合物，包括~（13）C5-C3 G及其降解产物、原儿茶酸（PCA）和间苯三甲醛（PGA）、13种PCA代谢产物和1种PGA代谢产物。酚类代谢物的最大浓度（Cmax）范围为10至2000 nM，在食用后2至30 h（tmax）之间，观察到的消除半衰期为0.5至96 h。确定的主要酚类代谢产物是马尿酸和阿魏酸，分别在血清中约16和8 h达到峰值。花色苷被代谢为具有结构多样性的代谢产物，其表现出动态动力学特征。了解这些代谢物的消除动力学是设计未来研究的关键，研究它们在饮食干预或降低疾病风险的治疗中的效用。
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 cardioprotective properties. A 500 mg oral bolus dose of 6,8,10,3′,5′-13C5-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. Seventeen 13C-labelled compounds were identified in the serum, including 13C5-C3G, its degradation products, protocatechuic acid (PCA) and phloroglucinaldehyde (PGA), 13 metabolites of PCA and 1 metabolite derived from PGA. The maximal concentrations of the phenolic metabolites (Cmax) ranged from 10 to 2000 nM, between 2 and 30 h (tmax) post-consumption, with half-lives of elimination observed between 0.5 and 96 h. The major phenolic metabolites identified were hippuric acid and ferulic acid, which peaked in the serum at approximately 16 and 8 h respectively. Anthocyanins are metabolized 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.
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影响因子：
6.1
作者：
Nizamutdinova, Irina Tsoy;Kim, Young Min;Kim, Hye Jung
通讯作者：
Kim, Hye Jung
影响因子：
5.2
作者：
de Ferrars, Rachel M.;Cassidy, Aedin;Kay, Colin D.
通讯作者：
Kay, Colin D.
影响因子：
5.2
作者：
Kay, Colin D.;Kroon, Paul A.;Cassidy, Aedin
通讯作者：
Cassidy, Aedin
影响因子：
37.8
作者：
Cassidy A;Mukamal KJ;Liu L;Franz M;Eliassen AH;Rimm EB
通讯作者：
Rimm EB
DOI：
10.1186/1472-6904-5-2
发表时间：
2005-03-03
期刊：
BMC clinical pharmacology
影响因子：
--
作者：
Anupongsanugool E;Teekachunhatean S;Rojanasthien N;Pongsatha S;Sangdee C
通讯作者：
Sangdee C