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Signatures of anthocyanin metabolites identified in humans inhibit biomarkers of vascular inflammation in human endothelial cells
Author(s) -
Warner Emily F.,
Smith Michael J.,
Zhang Qingzhi,
Raheem K. Saki,
O'Hagan David,
O'Connell Maria A.,
Kay Colin D.
Publication year - 2017
Publication title -
molecular nutrition and food research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.495
H-Index - 131
eISSN - 1613-4133
pISSN - 1613-4125
DOI - 10.1002/mnfr.201700053
Subject(s) - anthocyanin , metabolite , tumor necrosis factor alpha , vcam 1 , chemistry , pharmacology , biological activity , biochemistry , endocrinology , medicine , biology , cell , cell adhesion , in vitro , food science
Scope The physiological relevance of contemporary cell culture studies is often perplexing, given the use of unmetabolized phytochemicals at supraphysiological concentrations. We investigated the activity of physiologically relevant anthocyanin metabolite signatures, derived from a previous pharmacokinetics study of 500 mg 13 C 5 ‐cyanidin‐3‐glucoside in eight healthy participants, on soluble vascular adhesion molecule‐1 (VCAM‐1) and interleukin‐6 (IL‐6) in human endothelial cells. Methods and results Signatures of peak metabolites (previously identified at 1, 6, and 24 h post‐bolus) were reproduced using pure standards and effects were investigated across concentrations ten‐fold lower and higher than observed mean (<5 μM) serum levels. Tumor necrosis factor‐α (TNF‐α)‐stimulated VCAM‐1 was reduced in response to all treatments, with maximal effects observed for the 6 and 24 h profiles. Profiles tested at ten‐fold below mean serum concentrations (0.19–0.44 μM) remained active. IL‐6 was reduced in response to 1, 6, and 24 h profiles, with maximal effects observed for 6 h and 24 h profiles at concentrations above 2 μM. Protein responses were reflected by reductions in VCAM‐1 and IL‐6 mRNA, however there was no effect on phosphorylated NFκB‐p65 expression. Conclusion Signatures of anthocyanin metabolites following dietary consumption reduce VCAM‐1 and IL‐6 production, providing evidence of physiologically relevant biological activity.