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EXTRACT EXHIBITING INHIBITION ACTIVITY ON THROMBIN, PROCESS OF ITS PREPARATION, POLYPEPTIDE PREPARED FROM THIS EXTRACT, PROCESS OF ITS PREPARATION, A PHARMACEUTICAL PREPARATION BASED ON SAID POLYPEPTIDE, THE USE OF THE POLYPEPTIDE FOR THE PREPARATION OF THE PHARMACEUTICAL PREPARATION AND USE OF RHYNCHOBDELLIDA STRAIN LEECHES
EXTRACT EXHIBITING INHIBITION ACTIVITY ON THROMBIN, PROCESS OF ITS PREPARATION, POLYPEPTIDE PREPARED FROM THIS EXTRACT, PROCESS OF ITS PREPARATION, A PHARMACEUTICAL PREPARATION BASED ON SAID POLYPEPTIDE, THE USE OF THE POLYPEPTIDE FOR THE PREPARATION OF THE PHARMACEUTICAL PREPARATION AND USE OF RHYNCHOBDELLIDA STRAIN LEECHES
In the present invention there is disclosed a purified polypeptide exhibiting inhibiting activity to thrombin, isolated from a tissue or a secret of leeches of the Rhynchobdellida strain and being selected from a polypeptide of relative molecular weight of 9000 +/- 1000, having the following N-terminal sequence of amino acids Glu Asp Asp Asn Pro Gly Pro Pro Arg Ala Cys Pro Gly Glu or a polypeptide of relative molecular weight of 14 000 +/- 1000, having the following N-terminal sequence of amino acids Ser Glu Leu Gly Gln Ser Cys Ser Lys Glu Asn Pro Cys Pro Ser Asn Met Lys Cys Asn Arg Glu Thr Phe Lys. In the present invention there is also claimed a process for preparing such polypeptide, which preparation process is characterized by homogenizing a tissue or secrets of the leeches of the Rhynchobdellida strain, producing from the obtained homogenate a fraction containing water-soluble components thereof and purifying this fraction by employing thrombin-specific affinity chromatography being followed up with at least one another stage of a gel filtration and at least one another stage HPLC with reverse phases. In the present invention there is further claimed an extract, containing water-soluble components of homogenized tissue or secrets of the leeches of the Rhynchobdellida strain as an intermediate for preparing this polypeptide. In the present invention there is also claimed a pharmaceutical preparation containing this polypeptide and a pharmaceutically acceptable carrier. In the present invention there is further claimed the use of this polypeptide for preparing a medicament intended for treating diseases connected with thrombosis or for inhibition of blood platelet aggregation in extracorporeal blood.
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机译：在本发明中，公开了一种纯化的多肽，该多肽显示出对凝血酶的抑制活性，该多肽分离自Rhynchobdellida菌株的组织或水分泌物，并且选自相对分子量为9000 +/- 1000的多肽，具有以下N氨基酸Glu Asp Asp Asn Pro Gly Pro Pro Arg Ala Cys Pro Gly Glu的末端序列或相对分子量为14 000 +/- 1000的多肽，其N末端序列具有以下氨基酸Ser Glu Leu Gly Gln Cy Cys Ser Lys Glu Asn Pro Cys Pro Ser Asn Met Lys Cys Asn Arg Glu Thr Phe Lys。在本发明中，还要求保护该多肽的制备方法，该制备方法的特征在于使Rhynchobdellida菌株的组织或水lee分泌物均质化，从所得的均质物中产生包含其水溶性成分的级分并纯化。通过使用凝血酶特异性亲和色谱分离级分，随后进行至少另一阶段的凝胶过滤和至少另一阶段的反相HPLC。在本发明中，进一步要求保护一种提取物，其包含匀浆组织的水溶成分或Rhynchobdellida菌株的水lee分泌物的水溶性作为制备该多肽的中间体。在本发明中，还要求保护含有该多肽和药学上可接受的载体的药物制剂。在本发明中，进一步要求保护该多肽在制备用于治疗与血栓形成有关的疾病或抑制体外血液中血小板凝集的药物中的用途。
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