Heparin sodium is a sodium salt of amino glucan sulfate extracted from the intestinal mucosa of pigs or cattle. Due to the physical and chemical properties of strong negative charge, heparin sodium can interfere with many links in the process of blood coagulation, and has anticoagulant effects in vivo and in vitro. The specific anticoagulant principles are described as follows:
1. Inhibiting the formation of prothrombin kinase :(enhancing the activity of antithrombin ⅲ by hundreds of times) heparin binds with antithrombin ⅲ (at-i) to form heparin at-i complex. AT- ⅲ is a serine protease inhibitor that inactivates clotting factors such as factors Xla, Xla and XA that have the activity of serine protease.
2. Interference of thrombin: after low-dose heparin is combined with AT- ⅲ, even the reaction site of AT- ⅲ (arginine residue) is more likely to combine with the active center of thrombin (serine residue) to form a stable thrombin - antithrombin complex, thus inactivating thrombin and inhibiting the conversion of fibrinogen to fibrin.
3. It interferes with the activation of factor ⅲ by thrombin and affects the formation of insoluble fibrin. Prevent thrombin from activating factor ⅷ and V normally.
4, prevent platelet aggregation and destruction: heparin can prevent platelet adhesion and aggregation, so as to prevent platelet prelysis and release of platelet factor 3 and 5-hydroxytryptamine. The anticoagulant effect of heparin is related to the strong negative charge sulfate in the molecule. When the sulfate group is hydrolyzed or neutralized by protamine with strong positive charge, the anticoagulant activity is quickly lost.
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