Evaluation of antiaggregatory activity of flavonoid aglycone series

Mirza Bojić,Željko Debeljak,Marica Medić-Šarić,Siniša Tomić,Maja Tomičić

doi:10.1186/1475-2891-10-73

Abstract

BackgroundAmong natural compounds, present in every day diet, flavonoids have shown beneficial effect in prevention of cardiovascular diseases that can be attributed, at least partially to the described antiaggregatory activity i.e. antiplatelet effects of flavonoids. Due to the ever increasing pharmacological interest in antiplatelet agents a systematic experimental evaluation of large flavonoid series is needed.MethodsA set of thirty flavonoid aglycones has been selected for the evaluation. All measurements of aggregation were done under standardized and firmly controlled in vitro conditions. The whole blood samples, multiple platelet functional analyzer and adenosine diphosphate (ADP) as a weak agonist of aggregation were selected for this purpose.ResultsThe results were expressed as minimal concentration of flavonoid that can significantly lower the platelet aggregation compared to the corresponding untreated sample (minimal antiaggregatory concentration - MINaAC). All analyzed flavonoids exhibited antiaggregatory activity MINaAC ranging from 0.119 μM to 122 μM, while the most potent representatives were 3,6-dihydroxyflavone (0.119 μM) and syringetin (0.119 μM).ConclusionsMeasurable antiplatelet activity established at submicromolar flavonoid concentrations suggests that even a dietary consumption of some flavonoids can make an impact on in vivo aggregation of platelets. These findings also point out a therapeutical potential of some flavonoids.

Highlights

Among natural compounds, present in every day diet, flavonoids have shown beneficial effect in prevention of cardiovascular diseases that can be attributed, at least partially to the described antiaggregatory activity i.e. antiplatelet effects of flavonoids
In the developed countries most of the older population is affected by cardiovascular diseases
Flavonoids naturally occur in a free form or bound to a sugar moiety via hydroxyl groups

Summary

Introduction

Present in every day diet, flavonoids have shown beneficial effect in prevention of cardiovascular diseases that can be attributed, at least partially to the described antiaggregatory activity i.e. antiplatelet effects of flavonoids. Most commonly used drug in prevention of mentioned diseases is acetylsalicylic acid while clopidogrel represents another therapeutic option. Neither of these drugs is free of side effects, the search for new and safer drug from this group continues [1]. Present in every day diet, polyphenols, mainly flavonoids (Figure 1), have shown beneficial effect in prevention of cardiovascular diseases [2,3,4,5,6,7]. Flavonoids naturally occur in a free form (aglycones) or bound to a sugar moiety via hydroxyl groups (glycosides)

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