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肝素(Heparin,Hep)可以看作是一类特殊的硫酸乙酰肝素(Heparan Sulfate,HS),不同于广泛存在于细胞膜表面和细胞外基质的HS,Hep主要发现于肥大细胞的包内蓄积颗粒中,其具体的生物学功能还不甚清楚。与HS相比,Hep具有更高的硫酸化度,硫酸羧基比达到2.7,且糖醛酸主要为艾杜糖醛酸(IdoUA),占比达90%,仅含有少量的葡萄糖醛酸(GlcUA),这些结构特征使Hep具有远高于HS的抗凝活性。一方面,Hep可以与抗凝血酶 III结合抑制凝血酶的活性,另一方面,可以抑制凝血活性因子FXa活性,从而有效预防术后血栓形成。自1935年被发现以来,Hep作为最主要的抗凝剂,被广泛的应用于临床治疗至今。
Heparin (Hep) can be regarded as a special type of heparan sulfate (HS). Unlike HS, which is widely present on the surface of cell membranes and extracellular matrix, Hep is mainly found in the accumulated granules inside mast cells, and its specific biological function is not yet clear. Compared with HS, Hep has a higher degree of sulfation, a carboxyl to sulfate ratio of 2.7, and the main glucuronic acid is iduronic acid (IdoUA), accounting for 90%, with only a small amount of glucuronic acid (GlcUA). These structural features make Hep have much higher anticoagulant activity than HS. On the one hand, Hep can bind with antithrombin III to inhibit the activity of thrombin, and on the other hand, it can inhibit the activity of coagulation factor FXa, effectively preventing postoperative thrombosis. Since its discovery in 1935, Hep has been widely used in clinical treatment as the primary anticoagulant.