Comparative Effect of Quercetin and Quercetin-3-O-β-d-Glucoside on Fibrin Polymers, Blood Clots, and in Rodent Models

• Published in: Journal of biochemical and molecular toxicology 2016-11, Vol.30 (11), p.548-558
• Main Authors: Choi, Jun-Hui, Kim, Kyung-Je, Kim, Seung
• Format: Article
• Language: English
• Subjects: Acute Disease; Animals; Anticoagulation; Antithrombotic; Blood Coagulation - drug effects; Blood Platelets - drug effects; Blood Platelets - metabolism; Blood Platelets - pathology; Collagen - antagonists & inhibitors; Collagen - pharmacology; Disease Models, Animal; Epinephrine - antagonists & inhibitors; Epinephrine - pharmacology; Factor Xa - metabolism; Fibrin - antagonists & inhibitors; Fibrin - metabolism; Fibrinolytic Agents - pharmacology; Flavonoids - pharmacology; Male; Mice; Mice, Inbred ICR; Platelet Activation; Platelet Activation - drug effects; Primary Cell Culture; Quercetin; Quercetin - pharmacology; Quercetin-3-O-β-d-Glucoside; Rats, Sprague-Dawley; Signal Transduction; Thrombin - administration & dosage; Thrombin - antagonists & inhibitors; Thromboembolism - chemically induced; Thromboembolism - drug therapy; Thromboembolism - metabolism; Thromboembolism - pathology
• ISSN: 1095-6670; 1099-0461
• DOI: 10.1002/jbt.21822

ABSTRACT The present study evaluates the in vitro, in vivo, and ex vivo antithrombotic and anticoagulant effect of two flavonoids: quercetin and quercetin‐3‐O‐β‐d‐glucoside (isoquercetin). The present results have shown that quercetin and isoquercetin inhibit the enzymatic activity of thrombin and FXa and suppress fibrin clot formation and blood clotting. The prolongation effect of quercetin and isoquercetin against epinephrine and collagen‐induced platelet activation may have been caused by intervention in intracellular signaling pathways including coagulation cascade and aggregation response on platelets and blood. The in vivo and ex vivo anticoagulant efficacy of quercetin and isoquercetin was evaluated in thrombin‐induced acute thromboembolism model and in ICR mice. Our findings showed that in vitro and in vivo inhibitory effects of quercetin were slightly higher than that of quercetin glucoside, whereas in vitro and ex vivo anticoagulant effects of quercetin were weaker than that of quercetin glucoside because of their structural characteristics.