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Novel synthetic antithrombotic polypeptide, and preparation method and application thereof

An antithrombotic activity and antithrombotic drug technology, applied in the field of biomedicine, can solve problems such as small side effects, and achieve the effect of strong antithrombotic activity

Inactive Publication Date: 2011-05-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] With the aging of the population and the increase in the incidence of cardiovascular diseases, the current standard antithrombotic drugs can no longer adapt to and meet the existing needs, and the market capacity of such drugs is still increasing
The current antithrombotic drugs fail to meet the requirements of good activity, predictable drug effect, oral administration, fast onset of action, and few side effects

Method used

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  • Novel synthetic antithrombotic polypeptide, and preparation method and application thereof
  • Novel synthetic antithrombotic polypeptide, and preparation method and application thereof
  • Novel synthetic antithrombotic polypeptide, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1 Preparation and separation and purification of novel antithrombotic polypeptide BNC

[0026] BNCs were prepared according to the following sequence.

[0027] The amino acid sequence of BNC is: pyroglutamic acid-asparagine-cysteine.

[0028] In this example, the solid-phase peptide synthesis technique was used for manual synthesis, and the synthesized peptide was cleaved with high-concentration TFA to obtain a crude product. After purification by HPLC reverse phase column, it was confirmed by mass spectrometry analysis. The specific experimental steps are as follows:

[0029] 1) Preparation of BNC (taking the preparation of 1.323 mmol of BNC as an example to illustrate the method of solid-phase synthesis of polypeptides)

[0030] The following resins, Fmoc-protected amino acids, condensation reagents, and cleavage reagents for preparing antithrombotic polypeptide BNC were all purchased from Shanghai Gil Biochemical Co., Ltd.

[0031] The preparation is c...

Embodiment 2B

[0035] Example 2 Effect of BNC on Thrombosis after Electric Stimulation of Rat Common Carotid Artery Intima

[0036] 1) Preparation of sample solution

[0037] Before the positive control group was used, clopidogrel was diluted with normal saline to the required concentration of the drug solution (2mg / ml); the BNC group was dissolved with 0.2% L-arginine before use, and diluted with normal saline to the required concentration. Concentration of liquid medicine (2mg / ml). All groups were given tail vein administration with a volume of 10ml / kg.

[0038] 2) Preparation of animal models

[0039]Rats were intraperitoneally injected with 10 mg / L pentobarbital sodium solution (30 mg / kg), and fixed in a supine position after anesthesia. A midline incision was made in the neck, and the right common carotid artery was freed. The stimulating electrode of the BT87-3 experimental in vivo thrombosis measuring instrument was placed at the proximal end, and the temperature probe was placed a...

Embodiment 3B

[0048] The effect of embodiment 3BNC on the mouse acute pulmonary thrombosis induced by ADP

[0049] 1) Preparation of sample solution

[0050] Before use, the positive control group diluted clopidogrel with normal saline into a drug solution of the required concentration (the dose was 4 mg / kg); before use, the BNC group was diluted with normal saline into the drug solution of the required concentration (the dose was 4 mg / kg). kg); the inducer ADP solution was diluted with pure water to the required concentration (200mg / kg) before use. All groups were given tail vein administration with a volume of 10ml / kg.

[0051] 2) Experimental steps

[0052] Take 24 healthy ICR mice, weighing 20-25g, half male and half male, and randomly divide them into 3 groups according to body weight, 8 mice in each group, that is, model control group, positive control group and BNC group. Each group was given tail vein administration with a volume of 10ml / kg, the model control group was given equa...

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Abstract

The invention relates to the field of biomedicine, and discloses a synthetic polypeptide BNC (basal nucleus complex) with antithrombotic activity, a preparation method thereof and an application of the synthetic polypeptide BNC as an antithrombotic agent. The BNC is synthesized by using a Fomc solid-phase chemical process, and contains 3 amino acid residues; the sequence of the BNC is Pyr-Asn-Cys; the molecular weight of the BNC is 346; and the structural formula is shown in the specification. The animal experiment indicates that the polypeptide has inhibiting effects on the formation of thrombus after electrically stimulating the common carotid artery intima of a rat and the formation of ADP-induced (adenosine diphosphate-induced) acute lung thrombus of a mouse, and can prolong the coagulation time of the mouse. The structure formula of the BNC is shown in the specification.

Description

technical field [0001] The present invention relates to polypeptides, especially artificially modified and synthesized polypeptides with antithrombotic activity. The invention also relates to the preparation method of the polypeptide and its application as an antithrombotic agent, belonging to the field of biomedicine. Background technique [0002] With the aging of the population and the increase in the incidence of cardiovascular diseases, the current standard antithrombotic drugs can no longer adapt to and meet the existing needs, and the market capacity of such drugs is still increasing. The current antithrombotic drugs fail to meet the requirements of good activity, predictable efficacy, oral administration, rapid onset of action, and few side effects. [0003] Therefore, in view of the large market opportunities and the defects of existing drugs, finding safe and convenient new antithrombotic drugs has become a research hotspot in the medical field at home and abroad....

Claims

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Application Information

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IPC IPC(8): C07K5/097C07K1/20C07K1/06C07K1/04A61K38/06A61P7/02
Inventor 孔毅杨天雨邵妤赖伊丽
Owner CHINA PHARM UNIV
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