The pharmacokinetics of anthocyanins and their metabolites in humans

摘要: Background and Purpose Anthocyanins are phytochemicals with reported vasoactive bioactivity. However, given their instability at neutral pH, they presumed to undergo significant degradation subsequent biotransformation. The aim of the present study was establish pharmacokinetics metabolites cyanidin-3-glucoside (C3G), a widely consumed dietary phytochemical potential cardioprotective properties. Experimental Approach A 500 mg oral bolus dose 6,8,10,3′,5′-13C5-C3G fed eight healthy male participants, followed by 48 h collection (0, 0.5, 1, 2, 4, 6, 24, 48 h) blood, urine faecal samples. Samples were analysed HPLC-ESI-MS/MS elimination kinetics established using non-compartmental pharmacokinetic modelling. Key Results Seventeen 13C-labelled compounds identified in serum, including 13C5-C3G, its products, protocatechuic acid (PCA) phloroglucinaldehyde (PGA), 13 PCA 1 metabolite derived from PGA. maximal concentrations phenolic (Cmax) ranged 10 2000 nM, between 2 30 h (tmax) post-consumption, half-lives observed 0.5 96 h. major hippuric ferulic acid, which peaked serum approximately 16 8 h respectively. Conclusions Implications Anthocyanins metabolized structurally diverse range that exhibit dynamic kinetic profiles. Understanding these is key design future studies examining utility interventions or as therapeutics for disease risk reduction.