The isoflavonoid tectorigenin has better antiplatelet potential than acetylsalicylic acid

Applová, Lenka; Karlíčková, Jana; Říha, Michal; Filipský, Tomáš; Macáková, Kateřina; Spilková, Jiřina; Mladěnka, Přemysl

doi:10.1016/j.phymed.2017.08.023

Cited by 19 publications

(13 citation statements)

References 29 publications

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“…Furthermore, apigenin, genistein, quercetin, and catechin have been suggested to reversibly inhibit COX-1; however, the precise mechanism of action was not determined in this study [22]. In contrast to these results, Karlíčková et al [49] used isolated ovine COX-1 to measure flavonoid-induced inhibition of prostaglandin H 2 production and determined that 26 out of 28 flavonoids tested did not have a significant effect [49]. However, 100 μM genistein and 100 μM daidzein were significantly better than 100 μM acetylsalicylic acid (ASA) at inhibiting COX-1 activity in this assay, although in human PRP, they both were less potent and less efficacious than ASA.…”

Section: Naturally Occurring Flavonoidsmentioning

confidence: 60%

Synthetic Flavonoids as Novel Modulators of Platelet Function and Thrombosis

Vallance

Ravishankar

Albadawi

et al. 2019

IJMS

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Cardiovascular diseases represent a major cause of mortality and morbidity in the world, and specifically, thrombotic conditions such as heart attacks and strokes are caused by unwarranted activation of platelets and subsequent formation of blood clots (thrombi) within the blood vessels during pathological circumstances. Therefore, platelets act as a primary therapeutic target to treat and prevent thrombotic conditions. Current treatments are limited due to intolerance, and they are associated with severe side effects such as bleeding complications. Hence, the development of novel therapeutic strategies for thrombotic diseases is an urgent priority. Flavonoids are naturally occurring plant-derived molecules that exert numerous beneficial effects in humans through modulating the functions of distinct cell types. However, naturally occurring flavonoids suffer from several issues such as poor solubility, lipophilicity, and bioavailability, which hinder their efficacy and potency. Despite these, flavonoids act as versatile templates for the design and synthesis of novel molecules for various therapeutic targets. Indeed, several synthetic flavonoids have recently been developed to improve their stability, bioavailability, and efficacy, including for the modulation of platelet function. Here, we provide insight into the actions of certain natural flavonoids along with the advantages of synthetic flavonoids in the modulation of platelet function, haemostasis, and thrombosis.

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Section: Naturally Occurring Flavonoidsmentioning

confidence: 60%

Synthetic Flavonoids as Novel Modulators of Platelet Function and Thrombosis

Vallance

Ravishankar

Albadawi

et al. 2019

IJMS

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“…Mentioned positive effects include antioxidant, anticancer, anti‐diabetic, as well as other protective effects on the cardiovascular system . Formerly, the cardioprotective effect was considered to be based on the antioxidant properties, but currently it seems that there are other mechanisms including vasorelaxant properties and antiplatelet potential which are probably more relevant for the cardioprotective effect . However, studies analyzing flavonoid metabolism suggested that parent flavonoids cannot be the major players in their positive effects observed in humans since they reach virtually unmeasurable concentrations in blood .…”

Section: Discussionmentioning

confidence: 99%

“…[35,36] Formerly, the cardioprotective effect was considered to be based on the antioxidant properties, but currently it seems that there are other mechanisms including vasorelaxant properties and antiplatelet potential which are probably more relevant for the cardioprotective effect. [6,7,12,26,34,37] However, studies analyzing flavonoid metabolism suggested that parent flavonoids cannot be the major players in their positive effects observed in humans since they reach virtually unmeasurable concentrations in blood. [8] Metabolism in the human body also produces small phenolic compounds, which are absorbed into the systemic circulation at higher concentrations than the parent flavonoids.…”

Section: Discussionmentioning

confidence: 99%

“…Concerning cardiovascular diseases and higher flavonoid intake, there are reports of lower risk of coronary artery disease and also ischemic stroke. [3,4] Since approved antiplatelet drugs are used for the prevention of both coronary artery disease and ischemic stroke, [5] it is tempting to associate this finding, at least partially, with the antiplatelet effects of flavonoids and/or their metabolites, [6,7] but clear proof is missing. The bioavailability of parent flavonoids is considered to be very low.…”

Section: Introductionmentioning

confidence: 99%

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4‐Methylcatechol, a Flavonoid Metabolite with Potent Antiplatelet Effects

Applová

Karlíčková

Warncke

et al. 2019

Molecular Nutrition Food Res

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Scope Intake of flavonoids from the diet can be substantial, and epidemiological studies suggest that these compounds can decrease the incidence of cardiovascular diseases by involvement with increased platelet aggregation. Although parent flavonoids possess antiplatelet effects, the clinical importance is disputable due to their very low bioavailability. Most of them are metabolized by human colon bacteria to smaller phenolic compounds, which reach higher plasma concentrations than the parent flavonoids. In this study, a series of 29 known flavonoid metabolites is tested for antiplatelet potential. Methods and results Four compounds appear to have a biologically relevant antiplatelet effect using whole human blood. 4‐Methylcatechol (4‐MC) is clearly the most efficient being about 10× times more active than clinically used acetylsalicylic acid. This ex vivo effect is also confirmed using a potentially novel in‐vivo‐like ex ovo hen's egg model of thrombosis, where 4‐MC significantly increases the survival of the eggs. The mechanism of action is studied and it seems that it is mainly based on the influence on intracellular calcium signaling. Conclusion This study shows that some flavonoid metabolites formed by human microflora have a strong antiplatelet effect. This information can help to explain the antiplatelet potential of orally given flavonoids.

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“…Phloroglucinol (naturally present in brown seaweed, however it is used mainly as a pure synthetic chemical) has shown antiplatelet effect by inhibiting COX-1 and COX-2 by 45–74% and 49–72%, respectively, at concentrations of 10–50 μM. Some findings have been observed in animal models, for instance the intravenous administration of phloroglucinol in mice (2.5 and 5 μmol) suppressed the ex vivo ARA-induced platelet aggregation by 57–71% [78].…”

Section: Anti-inflammatory and Anti-platelet Aggregation Effects Omentioning

confidence: 99%

Roles of Phenolic Compounds in the Reduction of Risk Factors of Cardiovascular Diseases

et al. 2019

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The population is now living longer during the period classified as “elderly” (60 years and older), exhibiting multimorbidity associated to the lengthening of the average life span. The dietary intake of phenolic compounds (PC) may affect the physiology, disease development and progression during the aging process, reducing risk factors of age related diseases. The aim of this review is to briefly describe some of the possible effects of a series of PC on the reduction of risk factors of the onset of cardiovascular diseases, considering their potential mechanisms of action. The main actions described for PC are associated with reduced platelet activity, anti-inflammatory effects, and the protection from oxidation to reduce LDL and the generation of advanced glycation end products. Preclinical and clinical evidence of the physiological effects of various PC is presented, as well as the health claims approved by regulatory agencies.

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The isoflavonoid tectorigenin has better antiplatelet potential than acetylsalicylic acid

Cited by 19 publications

References 29 publications

Synthetic Flavonoids as Novel Modulators of Platelet Function and Thrombosis

Synthetic Flavonoids as Novel Modulators of Platelet Function and Thrombosis

4‐Methylcatechol, a Flavonoid Metabolite with Potent Antiplatelet Effects

Roles of Phenolic Compounds in the Reduction of Risk Factors of Cardiovascular Diseases

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