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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

L.K. Wells

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