Table 6. Inhibition of platelet activation in human whole blood.
TRAP-6 induced platelet activation was determined as fibrinogen binding to platelets and PE-selectin expression on platelets. PLP, EGCG, BBCl and Cur inhibited fibrinogen binding with IC50s of respectively 22.1, 65.9, 7.7 and 4.6 μM. PLP, BBCl and Cur inhibited PE-selectin expression with IC50s of respectively 83.2, 16.5 and 37.2 μM. The other compounds all had an Emax of < 30% and were considered to be unable to prevent platelet activation.
Fibrinogen binding | PE-selecting expression | |||||
---|---|---|---|---|---|---|
Compound | IC50 (μM) | Emax (%) | Fit (R2) | IC50 (μM) | Emax (%) | Fit (R2) |
PLP | 22.1 | 35 | 0.90 | 83.2 | 40 | 0.87 |
EGCG | 65.9 | 52 | 0.84 | - | < 30 | - |
BBCl | 7.7 | 64 | 0.89 | 16.5 | 38 | 0.91 |
Cur | 4.6 | 60 | 0.87 | 37.2 | 33 | 0.79 |
Apo | - | < 30 | - | - | < 30 | - |
Apo-e | - | < 30 | - | - | < 30 | - |
PN | - | < 30 | - | - | < 30 | - |
PTS | - | < 30 | - | - | < 30 | - |
PSS | - | < 30 | - | - | < 30 | - |