Extracts from Uncaria tomentosa as antiplatelet agents and thrombin inhibitors – The in vitro and in silico study. (1st March 2021)

• Record Type: Journal Article
• Authors: Kolodziejczyk-Czepas, Joanna; Ponczek, Michał; Sady-Janczak, Magdalena; Pilarski, Radosław; Bukowska, Bożena
• Is Part Of: Journal of ethnopharmacology. Volume 267(2021)
• Publication Date: 2021-03-01
• Subjects: Anticoagulant -- Blood platelets -- Thrombin -- Uncaria tomentosa; Ethnopharmacology -- Periodicals; Pharmacognosy -- Periodicals; Herbs -- Periodicals; Herbs -- Periodicals; Pharmacognosy -- Periodicals; Pharmacognosie -- Périodiques; Herbes -- Périodiques; 615.1
• DOI: 10.1016/j.jep.2020.113494
• Languages: English
• ISSNs: 0378-8741

Abstract

Abstract: Ethnopharmacological relevance: A wide range of traditional medicine applications of Uncaria tomentosa (Willd. ex Schult.) DC., commonly known as 'vilcacora' or 'cat's claw', includes blood purification, its anticoagulant properties and its use in haemorrhage therapy. Aim of the study: Our work is devoted to the effects of ethanol and aqueous extracts (1–50 μg/ml) from U. tomentosa leaves and bark on the haemostatic system. The study is based on two main questions: Can these extracts influence the coagulation cascade of blood plasma or the activation of blood platelets? Do they feature any anticoagulant properties? Materials and methods: Blood platelet aggregation was measured in human platelet-rich plasma; the anticoagulant tests were based on the thrombin, prothrombin and the activated partial thromboplastin time. For the thrombin (TH)-inhibitory activity evaluation, the chromogenic substrate S-2238 and fibrinogen, i.e. physiological substrate for this enzyme, were used. In silico studies included the interactions of TH and the main components of the extracts. Results: The examined extracts demonstrated slight antiplatelet activity. The thrombin time was slightly prolonged. The most efficient TH inhibitor was the ethanolic fraction from leaves (IC50 = 5.86 and 12.48 μg/ml, for the amidolytic and proteolytic assay, respectively). The plant ingredients interacted with TH within and outside the active site, dependently on the compound. The higher binding affinity was found for procyanidins B2 and C1. Conclusions: The examined extracts demonstrated slight antiplatelet effects; however, they may be promising candidates for the natural inhibitors of TH, which is critical for the formation of fibrin clot. Graphical abstract: Image 1