Evangelista V, Piccardoni P, de Gaetano G, Cerletti C
Giulio Bizzozero Laboratory of Platelet and Leukocyte Pharmacology, Istituto di Ricerche Farmacologiche Mario Negri, Santa Maria Imbaro, Italy.
Thromb Haemost. 1992 Jun 1;67(6):660-4.
Defibrotide is a polydeoxyribonucleotide with antithrombotic effects in experimental animal models. Most of the actions of this drug have been observed in in vivo test models but no effects have been reported in in vitro systems. In this paper we demonstrate that defibrotide interferes with polymorphonuclear leukocyte-induced human platelet activation in vitro. This effect was not related to any direct interaction with polymorphonuclear leukocytes or platelets, but was due to the inhibition of cathepsin G, the main biochemical mediator of this cell-cell cooperation. Since cathepsin G not only induces platelet activation but also affects some endothelial cell functions, the anticathepsin G activity of defibrotide could help to explain the antithrombotic effect of this drug.
去纤苷是一种在实验动物模型中具有抗血栓形成作用的多脱氧核糖核苷酸。该药物的大多数作用已在体内试验模型中观察到，但在体外系统中未报告有任何作用。在本文中，我们证明去纤苷在体外可干扰多形核白细胞诱导的人血小板活化。这种作用与去纤苷与多形核白细胞或血小板的任何直接相互作用无关，而是由于组织蛋白酶G受到抑制，组织蛋白酶G是这种细胞间相互作用的主要生化介质。由于组织蛋白酶G不仅诱导血小板活化，还影响一些内皮细胞功能，去纤苷的抗组织蛋白酶G活性可能有助于解释该药物的抗血栓形成作用。
