Protamine active peptide analogs, and preparation method and application thereof

A protamine and active peptide technology, applied in the field of biomedicine, can solve the problems of drug safety, drug uncontrollability, and difficulty in maintaining the quality of preparation batches.

Inactive Publication Date: 2017-09-29
山东卓莱生物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because protamine has the following defects, its antibacterial properties are limited to in vitro applications:
[0005] 1. Since protamine is derived from fish testis extracts of different species, its molecular weight is non-uniform and dispersed, and various protamines are mixed, so the quality between preparation batches is difficult to be constant, and there is uncontrollability as a drug;
[0006] 2. Such mixed natural protamine macromolecules are prone to allergic reactions, and there are drug safety issues
[0007] When protamine is us

Method used

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  • Protamine active peptide analogs, and preparation method and application thereof
  • Protamine active peptide analogs, and preparation method and application thereof
  • Protamine active peptide analogs, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0046] Experimental example 1. The inhibitory effect of protamine-like active peptides on Staphylococcus aureus

[0047] Staphylococcus aureus is a gram-positive bacterium (G + ), is the most common pathogenic bacteria that causes suppurative infection of human wounds, and is also the culprit that causes enteritis, pneumonia, sepsis, and sepsis. This experiment reflects the antibacterial effect of protamine-like active peptides by detecting the inhibitory rate of protamine-like active peptides on Staphylococcus aureus.

[0048] Preparation of LB culture medium:

[0049] Tryptone (Tryptone) 10g / L, yeast extract (Yeast extract) 5g / L, sodium chloride (NaCl) 10g / L, add distilled water to 1000ml, shake gently until the content dissolves, wrap the mouth of the bottle with tinfoil, and It can be used after high temperature and high pressure sterilization.

[0050] 1. Weigh the following 2mg samples of protamine-like active peptide freeze-dried powder:

[0051] (R 9 ) 2 KG, mole...

experiment example 2

[0065] Experimental example 2. The inhibitory effect of protamine-like active peptides on Pseudomonas aeruginosa

[0066] Pseudomonas aeruginosa is a Gram-negative bacteria (G - ), is the main pathogenic bacteria that commonly causes burn wounds and wound infection and suppuration in clinical practice, and is the main pathogenic bacteria that causes diseases such as otitis media, keratitis, urethritis, gastroenteritis, and pneumonia. This experiment reflects the antibacterial effect of protamine-like active peptides by detecting the inhibitory rate of protamine-like active peptides on Pseudomonas aeruginosa.

[0067] Steps 1-3 are the same as Experimental Example 1;

[0068] 4. After burning the inoculation loop on the flame of the alcohol lamp, pick a little Pseudomonas aeruginosa and mix it in 1ml of normal saline to get the bacteria solution. Take 100μl of the bacteria solution and add it to the #0-#5 culture tube of Group A-E get culture fluid;

[0069] 5. Cultivate in ...

experiment example 3

[0074] Experimental Example 3: Allergenicity Detection of Protamine-like Active Peptides

[0075] 1. Take 4 healthy New Zealand white rabbits for 8 weeks and divide them into 2 groups (2 rabbits / group): protamine-like peptide group and natural protamine group (protamine sulfate injection, 50mg / 5ml, purchased from Beijing Yue Kangkaiyue Pharmaceutical Co., Ltd.), the immune antigens in the two groups were protamine-like peptide and natural protamine;

[0076] 2. Initial immunization: subcutaneously inject Freund's complete adjuvant emulsion containing 1 mg / 1 ml immune antigen at 3 points on the back of each group of white rabbits;

[0077] The first booster immunization: 4 weeks after the initial immunization, the white rabbits in each group were subcutaneously injected with Freund's incomplete adjuvant emulsion containing 1mg / 1ml immune antigen again at 3 points;

[0078] The second booster immunization: 2 weeks after the first booster immunization, the white rabbits in each ...

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Abstract

The invention discloses a protamine-like active peptide and its preparation method and application. Its structural formula is: (Rn)2-KX, n is a natural number; wherein, R represents arginine; K represents lysine, and n is R X is empty or any one or more amino acids or chemical groups capable of forming peptide bonds with lysine. The protamine-like active peptide is an artificially synthesized polypeptide molecule with a definite molecular structure, molecular mass and consistency of the finished product. It is used to prepare mucous membrane cleaning and disinfectant, and acts on humans or animals to prevent and alleviate exogenous pathogenic microorganisms, The damage and stimulation of the mucous membrane by dust and soot particles can achieve the purpose of preventing and alleviating diseases.

Description

technical field [0001] The invention relates to the field of biomedicine, focuses on polypeptide compound molecules, and specifically relates to a protamine-like active peptide and its preparation method and application. Background technique [0002] Protamine is a kind of polycationic basic protein extracted from the testis of deep-sea fish, and its molecular weight is mainly distributed between 4000 and 10000 Daltons. About two-thirds of the amino acid composition of protamine is basic amino acid, and its isoelectric point pI is between 10 and 12. Since 1937, it has been found that protamine has antibacterial effect, and continuous research has extended the application of protamine to food preservation and clinical antagonism against heparin. [0003] As a polycationic protein, the antibacterial mechanism of protamine mainly involves: protamine reacts with peptidoglycan on the outer wall of bacteria and the cell membrane, causing the properties of the bacterial wall and c...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K1/06C07K1/04A61K38/10A61P31/04A61P31/10
CPCC07K7/08A61K38/00
Inventor 韩震王健
Owner 山东卓莱生物科技有限公司
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