A Bi-Functional Anti-Thrombosis Protein Containing Both Direct-Acting Fibrinogenolytic and Plasminogen-Activating ActivitiesReportar como inadecuado




A Bi-Functional Anti-Thrombosis Protein Containing Both Direct-Acting Fibrinogenolytic and Plasminogen-Activating Activities - Descarga este documento en PDF. Documentación en PDF para descargar gratis. Disponible también para leer online.

Direct-acting fibrinogenolytic agents such as plasmin have been proved to contain effective and safety thrombolytic potential. Unfortunately, plasmin is ineffective when administered by the intravenous route because it was neutralized by plasma antiplasmin. Direct-acting fibrinogenolytic agents with resistance against antiplasmin will brighten the prospect of anti-thrombosis. As reported in ‘Compendium of Materia Medica’, the insect of Eupolyphaga sinensis Walker has been used as traditional anti-thrombosis medicine without bleeding risk for several hundreds years. Currently, we have identified a fibrinogenolytic protein Eupolytin1 containing both fibrinogenolytic and plasminogen-activating PA activities from the beetle, E. sinensis. Objectives: To investigate the role of native and recombinant eupolytin1 in fibrinogenolytic and plasminogen-activating processes. Methods and Results: Using thrombus animal model, eupolytin1 was proved to contain strong and rapid thrombolytic ability and safety in vivo, which are better than that of urokinase. Most importantly, no bleeding complications were appeared even the intravenous dose up to 0.12 µmol-kg body weight 3 times of tested dose which could completely lyse experimental thrombi in rabbits. It is the first report of thrombolytic agents containing both direct-acting fibrinogenolytic and plasminogen-activating activities. Conclusions: The study identified novel thrombolytic agent with prospecting clinical potential because of its bi-functional merits containing both plasmin- and PA-like activities and unique pharmacological kinetics in vivo.



Autor: Hailong Yang , Yipeng Wang , Yao Xiao , Ying Wang, Jing Wu, Cunbao Liu, Huahu Ye, Fengliang Li, Haining Yu , Ren Lai

Fuente: http://plos.srce.hr/



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