A New Potent Inhibitor of Thrombin from the Leech Haemendipsa Yanyuanensis

1　Ｉｎｔｒｏｄｕｃｔｉｏｎ　Ｔｈｒｏｍｂｕｓｄｉｓｅａｓｅｏｆｈｅａｒｔａｎｄｂｒａｉｎｂｌｏｏｄｖｅｓｓｅｌｈａｓｂｅｃｏｍｅａｋｉｌｌｅｒｏｆｍａｎ .Ｂｅｃａｕｓｅｏｆｔｈｅｓｉｄｅｅｆｆｅｃｔｓｏｆｈａｅｍｏｒｒｈａｇｅｏｒｔｈｅｓｈｏｒｔｈａｌｆ ｌｉｆｅｉｎｖｉｖｏ ,ｔｈｅｐｒｅ ｓｅｎｔａｎｔｉｃｏａｇｕｌａｎｔｄｒｕｇｓａｒｅｕｎｓａｔｉｓｆｉｅｄ ,ａｎｄｓｅａｒｃｈ ｉｎｇｆｏｒｎｅｗａｎｔｉｃｏａｇｕｌａｎｔｓｗｉｔｈｈｉｇｈｅｒｅｆｆｉｃｉｅｎｔａｎｄｍｏｒｅｓｔａｂｉｌｅｈａ…     

一种测定凝血酶抑制剂活性的新方法

报告了一种新的测定凝血酶抑制剂抑制活性的测定方法——发色底物吸光值变化率法；以发色底物S-2238与标准凝血酶反应测定未抑制吸光值变化率，同时以发色底物S-2238与凝血酶抑制剂和标准凝血酶反应测定抑制吸光值变化率，然后以抑制吸光值变化率与未抑制吸光值变化率的比值计算凝血酶抑制剂的抑制活性．实验证明，这种凝血酶抑制剂抑制活性测定方法简便易行，重复性高，偶然误差小，可信度大。     

四种蛭体内抗凝血活性物含量的比较研究初探

根据匈牙利BagdyD。利用水溶性介质从蛭体内提取水蛭素的方法,初步研究比较邓广泛分布于我省境内4种蛭体内搞凝血活性物含量的差异,确定了我省可用于抗凝血活性物提取的蛭类,为开发我省的蛭类动物提供了一定的依据。     

棒纹牛蛭体内抗凝血蛋白的提取

通过离子交换、凝胶过滤、亲和层析及反向高效液相色谱操作，分析鉴定了棒纹牛蛭体内主要抗凝血物质成分为凝血酶抑制蛋白，其组成是三个相对分子质量分别为。7528，7446和7016的小分子量蛋白质，综合分析后认为属水蛭素类物质．     

A New potent Inhibitor of Thrombin from the Leech Haemendipsa Yanyuznensis

Two components of anticoagulant protein were isolated from the leech Haemendipsa yanyuanensis by heparin agarose affinity chromatography and ultracentrifugation,The determination of anticoagulant activity and characterization analysis of the protein using the method of chromogenic substrate indicates that the anticoagulant protein is thrombin-specific but not factor Xa-specific.The resylts lay a foundation for the research of the anticoaguklant mechanism and application of anticoagulant protein from H.yanguanensis.     

Recent insights on biochemical and molecular basis for developing antihaemostatic agents: A review

The normal coagulation process is initiated by disruption and exposure of the subendothelial components of blood vessels. Platelets adhere to subendothelium-bound von Willebrand factor via glycoprotein (GP) Ib complex. This initial interaction per se and the release of platelet agonists transduce signals that leads to the rise in intracellular Ca2+ which induces shape change, prostaglandin synthesis, release of granular contents and conformational changes in platelet Gp IIb-IIIa. Gp IIb-IIIa in activated platelets binds fibrinogen and other adhesive proteins and mediates platelet cohesion the primary haemostatic plug. Furthermore, the activated platelets due to aggregation, result in the formation of fibrin (secondary hemostasis). Normally the haemostatic process plays a delicate balance between keeping the blood in the fluid state to maintain flow and rapidly forming an occluding plug following vessel injury. Thrombosis occurs because of alteration in this delicate balance. Arterial thrombosis occurs in the setting of previous vessel wall injury mostly because of atherosclerosis, while venous thrombosis occurs in areas of stasis. The recent advances in understanding of the haemostatic process have led to a better understanding of the mechanism of action of many antithrombotic drugs and identification of new targets for drug development. The molecular target of the ticlopidine has been identified. Large numbers of IIb-IIIa inhibitors have been developed. The mechanism of action of heparin has been defined at the molecular level. As a result, a synthetic pentasaccharide, based on antithrombin-binding domain of heparin, has been developed and tested successfully in clinical trials. New generation direct thrombin inhibitors are being developed. Factor Xa has a critical position at the convergence of intrinsic and extrinsic pathway. The clinical tolerability and the efficacy of low molecular weight heparins has established that inhibition of further thrombin generation, by blocking factor Xa alone can be an effective way of preventing thrombus growth without inactivating thrombin. A large number of specific factor Xa inhibitors are under development. Some of these are in preliminary clinical trials and appear to be promising. Future clinical trials will determine whether these new drugs will provide better risk-benefit ratio in treatment of thrombotic disorders. Similarly role of thrombolytics has been clearly established in many diseases including coronary artery disease.     

凝血酶治疗拔牙后出血的疗效观察

本文对４３例拔牙后出血局部应用凝血酶治疗，显效３２例（７４．４％），有效１１例（２５．６％），总有效率１００％，未见任何不良反应．凝血酶与一些传统的方法相比具有快速、高效等优点，因此是一种理想的预防和治疗拔牙后出血的局部止血药物．