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BMC Complementary Medicine and Therapies
Published in: BMC Complementary Medicine and Therapies 1/2017

Open Access 01-12-2017 | Research article

Flavonolignans inhibit the arachidonic acid pathway in blood platelets

Authors: Michal Bijak, Joanna Saluk-Bijak

Published in: BMC Complementary Medicine and Therapies | Issue 1/2017

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Abstract

Background

Arachidonic acid metabolism by cyclooxygenase (COX) is a major pathway for blood platelets’ activation, which is associated with pro-thrombotic platelet activity and the production of pro-inflammatory mediators. Inhibition of COX activity is one of the major means of anti-platelet pharmacotherapy preventing arterial thrombosis and reducing the incidence of cardiovascular events. Recent studies have presented that a silymarin (standardized extract of Milk thistle (Silybum marianum)) can inhibit the COX pathway. Accordingly, the aim of our study was to determine the effects of three major flavonolignans (silybin, silychristin and silydianin) on COX pathway activity in blood platelets.

Methods

We determined the effect of flavonolignans on arachidonic acid induced blood platelet aggregation, COX pathway metabolites formation, as well as COX activity in platelets. Additionally, we analysed the potential mechanism of this interaction using the bioinformatic ligand docking method.

Results

We observed that tested compounds decrease the platelet aggregation level, both thromboxane A2 and malondialdehyde formation, as well as inhibit the COX activity. The strongest effect was observed for silychristin and silybin. In our in silico study we showed that silychristin and silybin have conformations which interact with the active COX site as competitive inhibitors, blocking the possibility of substrate binding.

Conclusions

The results obtained from this study clearly present the potential of flavonolignans as novel antiplatelet and anti-inflammatory agents.
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Metadata
Title
Flavonolignans inhibit the arachidonic acid pathway in blood platelets
Authors
Michal Bijak
Joanna Saluk-Bijak
Publication date
01-12-2017
Publisher
BioMed Central
Published in
BMC Complementary Medicine and Therapies / Issue 1/2017
Electronic ISSN: 2662-7671
DOI
https://doi.org/10.1186/s12906-017-1897-7

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