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KMID : 1161420120150121073
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Journal of Medicinal Food
2012 Volume.15 No. 12 p.1073 ~ p.1080
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Antithrombotic Effect of Chikusetsusaponin IVa Isolated from Ilex paraguariensis (Mate)
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Dahmer Tabitha
Berger Markus
Barlette Adriana Gregory
Reck Jose Jr.
Segalin Jeferson
Verza Simone
Ortega George Gonzalez
Gnoatto Simone Cristina Baggio
Guimaraes Jorge Almeida
Verli Hugo
Gosmann Grace
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Abstract
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The triterpene chikusetsusaponin IVa was isolated from the fruit of Ilex paraguariensis. Using biochemical and pharmacological methods, we demonstrated that chikusetsusaponin IVa (1) prolongs the recalcification time, prothrombin time, activated partial thromboplastin time, and thrombin time of normal human plasma in a dose-dependent manner, (2) inhibits the amidolytic activity of thrombin and factor Xa upon synthetic substrates S2238 and S2222, (3) inhibits thrombin-induced fibrinogen clotting (50% inhibition concentration, 199.4±9.1?μM), and (4) inhibits thrombin- and collagen-induced platelet aggregation. The results also indicate that chikusetsusaponin IVa preferentially inhibits thrombin in a competitive manner (Ki=219.6?μM). Furthermore, when administered intravenously to rats, chikusetsusaponin IVa inhibited thrombus formation in a stasis model of venous thrombosis, although it did not induce a significant bleeding effect. Chikusetsusaponin IVa also prolonged the ex vivo activated partial thromboplastin time. Altogether, these data suggest that chikusetsusaponin IVa exerts antithrombotic effects, including minor hemorrhagic events. This appears to be important for the development of new therapeutic agents.
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KEYWORD
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chikusetsusaponin, hemostasis, Ilex paraguariensis, platelet aggregation, thrombosis, thrombin
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