Dual Anticoagulant/Antiplatelet Activity of Polyphenolic Grape Seeds Extract

Abstract

Because of the side-effects of commonly used anti-platelet and anticoagulant drugs, investigations into plant substances with similar activities are very common. Based on our own studies in recent years, we estimate that it is possible to use natural compounds to both inhibit coagulation pathway enzymes and to reduce blood platelets’ activation. As such, in our current study we wanted to verify the anti-platelet and anticoagulant properties of grape seed extract (GSE) using in vitro models. During our analysis, the following parameters were analyzed: Coagulation times, thromboelastometry assays (coagulation time, clot formation time and maximum clot firmness), aggregation of platelets and phosphorylation of vasodilator-stimulated phosphoprotein (VASP). Adenosine diphosphate (ADP)-induced aggregation was lower in GSE 7.5 µg/mL as well as in GSE 15.0 µg/mL. A similar dependence was observed in VASP assays for GSE 7.5 µg/mL and GSE 15 µg/mL. The effect on plasma coagulation tests was distinct only with GSE 15 µg/mL. All of the thromboelastometry variables were statistically significant with 15.0 µg/mL GSE concentration. Our results show, for the first time, the multi-potential effect of grape seed extract on coagulation systems, and clearly suggest that grape seed extract could be considered a promising nutraceutical in the prevention of cardiovascular thrombotic events caused by different mechanisms.

Grape Seeds: Chromatographic Profile of Fatty Acids and Phenolic Compounds and Qualitative Analysis by FTIR-ATR Spectroscopy

“…For this reason, in the last decade an ever-increasing interest in the seeds appeared, since they contain bioactive compounds such as fatty acids and polyphenols [5,[10][11][12][13][14], which are attractive from a nutraceutical perspective [15][16][17][18][19][20][21][22]. Their potential benefits ranges from anti-platelet and anticoagulant activity, to antioxidant, hypoglycemic, and even activity against cancer [23][24][25][26][27].…”

Polyphenols: Modulators of Platelet Function and Platelet Microparticle Generation?

“…On the contrary, some studies have demonstrated no significant antiplatelet effect in hypertensive populations [93,94,96] (Table 1). Chokeberries and grapes used in these intervention studies are food sources that have previously shown antiplatelet effects in vitro [43,113]. This may highlight that biological variables and different baseline platelet functions of study populations may lead to differences in the antiplatelet effect of polyphenols.…”

“…The enzyme-linked immunoassay (ELISA) method can also be used to count and perform functional analysis on PMPs but without size information [39]. In addition, the vasodilator-stimulated phosphoprotein (VASP) phosphorylation assay is a special flow cytometry method that has been used in research studies to evaluate platelet function [42][43][44]. It works on the principle that activation of the P2Y 12 receptor by ADP reduces VASP phosphorylation and thus inhibition of receptor activation increases VASP phosphorylation.…”

“…Reduced ADP-induced platelet aggregation and platelet reactivity index (by increasing VASP phosphorylation) [43] In vitro Olive leaves 11 healthy male subjects…”

Antithrombotic activity of flavonoids and polyphenols rich plant species

“…The advantage of using different agonists of aggregation is assessment of different signaling pathways that are inhibited. Quite often concentrations of extract are arbitrarily used in the studies, e.g., grape (Vitis vinifera L.) seed extracts reduced platelet aggregation in the test induced by ADP in relatively high concentrations of 7.5 and 15 g L -1 , equivalent of 25 and 50 mmol L -1 if recalculated to molarity based on quercetin molar mass (302.24 g mol -1 ) (14).…”