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Physiologically relevant screening of polyphenol-rich commercial preparations for bioactivity in vascular endothelial cells and application to healthy volunteers: a viable workflow and a cautionary tale

Jones, Huw; Papageorgiou, M.; Gordon, A.; Ehtesham; Javed, Z.; Wells, L.K.; Greetham, S.; Doyle, B.; Hayes, N.; Rigby, A.; Atkin, S.L.; Courts, F.L.; Sathyapalan, T.

Authors

Huw Jones

M. Papageorgiou

A. Gordon

Ehtesham

Z. Javed

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Mrs Liz Wells Liz.Wells@hull.ac.uk
Lecturer in Nutrition and Dietetics

S. Greetham

B. Doyle

N. Hayes

A. Rigby

S.L. Atkin

F.L. Courts

T. Sathyapalan



Abstract

This study describes the screening of 13 commercially-available plant extracts for pharmacological activity modulating vascular function using an endothelial cell model. A French maritime pine bark extract (FMPBE) was found to have the greatest effect upon nitric oxide availability in control (181% ± 36% of untreated cells) and dysfunctional cells (132% ± 8% of untreated control cells). In healthy volunteers, the FMPBE increased plasma nitrite concentrations 8 h post-consumption compared to baseline (baseline corrected median 1.71 ± 0.38 (25% IQR) and 4.76 (75% IQR) µM, p0.05), however HPLC-UV fingerprinting showed that the new batch had a 5-15% in major constituents (including procyanidins A2, B1 and B2) compared to the original batch. This research describes a robust mechanism for screening bioactive extracts for vascular effects. It also highlights batch variability as a significant limitation when using complex extracts for pharmacological activity, and suggests the use of in vitro systems as a tool to identify this problem in future studies.

Journal Article Type Article
Publication Date 2020-03
Print ISSN 0006-2952
Electronic ISSN 0006-2952
Publisher Elsevier
Peer Reviewed Peer Reviewed
Volume 173
Article Number 113754
APA6 Citation Jones, H., Papageorgiou, M., Gordon, A., Ehtesham, , Javed, Z., Wells, L., …Sathyapalan, T. (2020). Physiologically relevant screening of polyphenol-rich commercial preparations for bioactivity in vascular endothelial cells and application to healthy volunteers: a viable workflow and a cautionary tale. Biochemical Pharmacology, 173, https://doi.org/10.1016/j.bcp.2019.113754
DOI https://doi.org/10.1016/j.bcp.2019.113754
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