Deconvoluting the Dual Antiplatelet Activity of a Plant Extract

• Published in: Journal of agricultural and food chemistry Vol. 64; no. 22; pp. 4511 - 4521
• Main Authors: Kontogianni, Vassiliki G, Tsoumani, Maria E, Kellici, Tahsin F, Mavromoustakos, Thomas, Gerothanassis, Ioannis P, Tselepis, Alexandros D, Tzakos, Andreas G
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 08-06-2016
• Subjects: Blood Platelets - cytology; Blood Platelets - drug effects; Blood Platelets - metabolism; Dual Specificity Phosphatase 2 - metabolism; Humans; Olea - chemistry; P-Selectin - metabolism; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plant Leaves - chemistry; Platelet Aggregation - drug effects; Platelet Aggregation Inhibitors - chemistry; Platelet Aggregation Inhibitors - pharmacology; cardiovascular disease; olive leaf extract; antiplatelet activity; human platelets; triterpenes
• ISSN: 0021-8561; 1520-5118
• DOI: 10.1021/acs.jafc.6b00544

A thorough evaluation of the antiplatelet activity profile of hexane olive leaf extract in human platelets indicated a potent activity accomplished through a two axis inhibition of platelet activation triggered both by ADP and thrombin. To delineate the extract components responsible for this dual activity, an NMR based method was established to determine and quantify the triterpenoid content leading to the characterization of uvaol, erythrodiol, and oleanolic acid. The antiplatelet profile of the total extract and of the 3 determined triterpenoids was evaluated against in vitro platelet aggregation induced by several platelet agonists as also on PAC-1 binding and P-selectin membrane expression both in healthy volunteers and in platelets from patients with an acute coronary syndrome receiving dual antiplatelet therapy with aspirin and ticagrelor. The extract was identified to inhibit ADP-induced platelet activation due to its erythrodiol content and TRAP-induced platelet activation due to the activity of uvaol and oleanolic acid.