Table 2.
IC50, safety indices, platelet hemostatic functions, and tail-bleeding time of TFV-1, TFV-3, and clinical anti-thrombotic agents.
Antithrombotic Agents | TFV-1 | TFV-3 | Abciximab | Eptifibatide | Control | ||||
---|---|---|---|---|---|---|---|---|---|
The Dose of Agents (Fold of IC50) | 2× | 6× | 2× | 6× | 2× | 6× | 2× | 6× | - |
IC50 (μg/mL) | 0.74 | 0.45 | 5 | 0.52 | - | ||||
Safety index | 20.27 | 2.22 | 2.00 | 1.92 | - | ||||
Clot formation time (s) | 135 (NS) | 172 (NS) | 540 (*) | 967 (**) | 569 (***) | 1355 (***) | 518 (**) | 622 (**) | 105 |
Inhibition of Clot retraction (%) | 0 | 0 | 77.3 | 86.1 | 54.7 | 92.5 | 63.2 | 89.4 | - |
Tail-bleeding time (s) | 66.8 (NS) | 102.5 (NS) | 233.3 (**) | 574.0 (***) | 373.4 (***) | 580.8 (***) | 538.6 (***) | 1341.2 (***) | 68.7 |
IC50 of collagen (10 μg/mL)-induced platelet aggregation in washed platelet suspension. Safety index is estimated as the lowest concentration of disintegrin to activate platelet (combining with 4 μg/mL AP2)/IC50 of disintegrin on collagen-induced platelet aggregation. Inhibition of thrombin-induced clot retraction of human PRP (%) was measured by the volume of serum (agent−control)/volume of serum (control). Tail bleeding times of mice were measured at increasing antithrombotic dosages as compared with the control group (68.7 s, n = 28). (These experiments were repeated at least three times and values were presented as means. * p < 0.05, ** p < 0.01, *** p < 0.001 compared with control group by Dunnett’s test; NS, non-significance).