Protamine mimetic peptide and pharmaceutical salt and application thereof

A protamine and peptide-mimicking technology, which is applied in the field of biomedicine, can solve problems such as difficulty in achieving uniformity and consistency in quality, lack of substitute drugs for protamine, and restrictions on the production of protamine, so as to facilitate artificial synthesis and eliminate bleeding Tendency, the effect of reducing the sensitization rate

Active Publication Date: 2014-10-01
FIELD OPERATION BLOOD TRANSFUSION INST OF PLA SCI ACAD OF MILITARY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 2. Since the finished product of protamine is a heterogeneous molecular group, its antagonizing effect on heparin varies with different batches of protamine preparation, and its quality is difficult to achieve uniformity and consistency;
[0005] 3. Protamine is extracted from the mature sperm of fish, which limits and restricts the production of protamine from the perspective of raw material resources
[0006] 4. Protamine is an exogenous macromolecular protein, and the human body will have an allergic reaction to it, especially for patients who use protamine again, it may cause major medical accidents, and there are hidden dangers and risks in clinical use
[0007] Although the use of protamine has disadvantages or disadvantages, so far no other protamine alternative drugs that can antagonize heparin have appeared

Method used

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  • Protamine mimetic peptide and pharmaceutical salt and application thereof
  • Protamine mimetic peptide and pharmaceutical salt and application thereof
  • Protamine mimetic peptide and pharmaceutical salt and application thereof

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Embodiment 1

[0036] Embodiment 1: the design of protamine mimetic peptide

[0037] Design ideas and methods: Heparin is a natural anticoagulant substance extracted from bovine lung or pig small intestinal mucosa. Its average molecular weight is 15KD mucopolysaccharide sulfate, which is strongly acidic and has a large amount of negative charge. According to the characteristics of the chemical properties of heparin, the present invention first uses a polypeptide composed of positively charged basic amino acids to neutralize or antagonize heparin with a large amount of negative charge.

[0038] Arranged according to the strength of basicity, the three basic amino acids are arginine (Arg, R) > lysine (Lys, K) > histidine (His, H). Through theoretical design and effective experimental verification, the present invention finally determines a series of artificially designed and artificially synthesized protamine mimetic peptides. They are linear polypeptides with 9 to 20 amino acids consisting o...

Embodiment 2

[0064] Embodiment 2: the synthesis of protamine mimetic peptide

[0065] In 1963, American scientist R.B. Merrifield invented the method of immobilizing the carboxyl terminal (C terminal) of the amino acid of the target peptide on an insoluble resin, and the amino terminal (N terminal) of the amino acid bound to the resin is condensed with the carboxyl terminal of the amino acid to be connected. Solid-phase synthesis to elongate peptide chains. The sequence of peptide synthesis starts from the carboxy-terminal (C-terminal) of the polypeptide and extends one by one in the direction of the amino-terminal (N-terminal) of the peptide. When carrying out the carboxyl conjugation reaction of amino acid, its amino group and side chain group should be protected to avoid the reaction. At present, tert-butoxycarbonyl (Boc) protection method and fluorenylmethyloxycarbonyl (Fmoc) protection method are commonly used. Therefore, every To connect an amino acid, it needs to undergo a condensa...

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Abstract

The invention discloses a protamine mimetic peptide and pharmaceutical salt and application thereof. The protamine mimetic peptide is a straight chain polypeptide composed of 9-20 alkaline amino acids, the alkaline amino acid is one or more of arginine (Arg, R), lysine (Lys, K) and histidine (His, H). According to verification, the serial protamine mimetic peptide and pharmaceutical salt thereof have the function of the protamine, have neutralization and antagonism effect on the heparin in the blood, and can be used for clinically neutralizing and antagonizing bleeding tendency caused by heparin in the blood by replacing protamine.

Description

technical field [0001] The present invention belongs to the field of biomedicine, and in particular relates to an artificially designed and artificially synthesized linear polypeptide molecule (protamine mimic peptide) composed of basic amino acids. Neutralization and antagonism, can replace protamine in clinical use to eliminate and neutralize the bleeding tendency caused by heparin in the blood. Background technique [0002] Patients with cardiovascular diseases need to inject anticoagulant heparin into the blood vessels before the operation of extracardiac circulation or stent intervention to avoid thrombus during the operation, but the heparin in the blood vessels needs to be eliminated in time after the operation is completed to avoid bleeding of vicious events. At present, the only drug clinically used to antagonize heparin is protamine, but the use of protamine has the following disadvantages or disadvantages: [0003] 1. Protamine is a protein extracted from the nu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08C07K7/06A61K38/10A61K38/08A61P7/04
CPCC07K7/06C07K7/08A61K38/08C07K7/04A61K38/10A61P7/02A61P7/04
Inventor 窦桂芳韩苏孟志云朱晓霞甘慧顾若兰吴卓娜刘桃云李俭郑颖李通
Owner FIELD OPERATION BLOOD TRANSFUSION INST OF PLA SCI ACAD OF MILITARY
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