Plant extracts inhibit ADP-induced platelet activation in humans: their potential therapeutic role as ADP antagonists

Abstract

Adenosine diphosphate (ADP) plays a pivotal role in platelet activation. Platelet hyperactivity is associated with vascular disease and also has a key role in haemostasis and thrombosis. ADP activates platelets through three purinoceptor subtypes, the G q -coupled P2Y 1 receptor, G icoupled P2Y 12 receptor and P2X 1 ligand-gated cation channel. Platelet ADP purinergic receptors are therefore suitable targets for antiplatelet drugs. Thienopyridines such as clopidogrel and ticlopidine, as well as other ADP receptor antagonists like prasugrel, ticagrelor, cangrelor and elinogrel have demonstrated clinical benefits via the inhibition of the selective purinergic ADP receptor, P2Y 12 . However, they still have limitations in their mode of action and efficacy, like increased risk of bleeding. Thus, the ongoing pursuit to develop newer and more effective antiplatelet agents continues. There is a growing interest in the purinergic antiplatelet properties exhibited by plant extracts. This article considers the following: pomolic acid isolated from Licania pittieri, brazilin isolated from the heartwood of Caesalpinia sappan L, phylligenin isolated from the twigs of Muraltia vulpina , bark oil of Gonystylus velutinus , seed and bark extracts from Aesculus hippocastanum L . and red wine phenolics and catechins isolated from green tea. Moreover, the method used to investigate platelet purinergic receptors should be considered, since using a more sensitive, highresolution platelet sizer can sometimes detect platelet variations when the light transmission method was not able to do so. The exact mechanisms by which these plant extracts work need further investigation. They all however inhibit ADP-induced activation in human platelets. This could explain, at least in part, the protective effect of plant extracts as antiplatelet agents.

Acute Effusive Pericarditis due to Horse Chestnut Consumption

“…Some researchers suggest that horse chestnut is a strong inhibitor of adenosine diphosphate – induced thrombocyte aggregation [ 13 , 14 ]. The development of pericardial effusion after consumption of horse chestnut could be due to this strong antiaggregant feature.…”

Bioactive Natural Compounds with Antiplatelet and Anticoagulant Activity and Their Potential Role in the Treatment of Thrombotic Disorders

“…It is a popular spice that has been used for both culinary and medicinal purposes for thousands of years [ 134 ]. Plants belonging to the Allium genus, such as garlic ( Allium sativum ), have been shown to exert multiple effects, including lowering blood pressure, reducing cholesterol and triglyceride levels, and promoting fibrinolysis and platelet aggregation inhibition [ 135 , 136 , 137 , 138 ]. Bioactive chemical constituents of garlic include sulfur compounds such as alliin, allicin, ajoene, allyl propyl disulfide, diallyl trisulfide (DATS), S-allylcysteine (SAC), vinyldithiins, S-allylmercaptocysteine; enzymes such as alliinase, peroxidases, tyrosinase; amino acids (arginine and others) and their glycosides; and some minerals.…”

Inhibidores del receptor plaquetario P2Y12. Parte 2 de 2: etiología, diagnóstico y manejo de la resistencia

“…Ante el auge del consumo de productos «naturales» es importante referenciar la interferencia que se ha informado en la literatura médica universal con los inhibidores del receptor plaquetario P2Y 12 , en particular en relación con el consumo concomitante del Ginkgo biloba [229,230], el tanaceto (Tanacetum parthenium) [231][232][233][234], el castaño de las Indias (Aesculus hippocastanum) [235] y el té verde (Camellia sinensis) [236,237], entre otros de estos productos de venta libre. Se ha demostrado con estos compuestos naturistas algún grado de efecto antiagregante que puede, por tanto, aumentar el riesgo hemorrágico en los pacientes que toman antiagregantes plaquetarios como la aspirina y los inhibidores del receptor plaquetario P2Y 12 .…”

“…z z El uso cada vez más frecuente de medicinas «naturales» con efecto antiagregante como el Ginkgo biloba [229,230], el tanaceto (Tanacetum parthenium) [231][232][233][234], el castaño de las Indias (Aesculus hippocastanum) [235] y el té verde (Camellia sinensis) [236,237].…”