Ectodomain shedding of glycoprotein Ibα(GPIbα), the von Willebrand Factor (vWF) - binding site of the platelet adhesion receptor GPIb-IX-V complex, in a disintegrin and metalloproteinase 17 (ADAM17)/Tumor necrosis factor- converting enzyme (TACE) - dependent mechanism is of great importance in the regulation of platelet function. Our previous study revealed that paeoniflorin (PF), hydroxyl-safflower yellow A (HSYA) and some of astragalasides (AS-III), major active ingredients contained in traditional Chinese medicines (TCM) Chi shao, Honghua and Huangqi, respectively, were capable of activating ADAM17 in vascular endothelial cells and thus by inducing the shedding of some cell surface proteins (such as TNFR1 and EGFR ligand) involved in the regulation of inflammation, immunity and cell survival. Through reviewing the function of platelet membrane receptor GPIbα, the shedding effect of ADAM17 on GPIbα and the mechanisms of ADAM17 activation by various endogenous substances and exogenous drugs, we presume that platelet ADAM17 could be an important player in the blood circulation-promoting and blood stasis-removing effect of TCM, thus by shedding a new light on the anti-platelet and anti-thrombosis activities of TCM.