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Protegrin-1 antimicrobial peptide derivative and preparation method and application thereof

A technology of antimicrobial peptides and derivatives, applied in the field of medicine, can solve the problems of limited resources of natural antimicrobial peptides, loss of activity of natural antimicrobial peptides, difficulty in realizing industrial application, etc., achieves strong antibacterial activity, low hemolytic activity, and is conducive to industrial production Effect

Inactive Publication Date: 2017-03-22
成都山信药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, natural antimicrobial peptides are easily degraded and inactivated by proteases in the body, making it difficult to exert their antibacterial activity
At the same time, natural antimicrobial peptide resources are limited, and it is difficult to realize industrial application

Method used

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  • Protegrin-1 antimicrobial peptide derivative and preparation method and application thereof
  • Protegrin-1 antimicrobial peptide derivative and preparation method and application thereof
  • Protegrin-1 antimicrobial peptide derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: Synthesis of Protegrin-1 antimicrobial peptide derivative SEQ No.5

[0065] (1) Synthesize the linear polypeptide of SEQ No.5

[0066] Take 2g of Rink Amide resin with a degree of substitution of 0.76mmol / g in a solid-phase reactor, add DCM to swell for 20min, then add 20%PIP / DMF solution to react for 20min to remove the Fmoc protecting group (that is, use the Rink Amide resin as a carrier , Fmoc protected L-amino acids, Fmoc protected D-amino acids as raw materials), washed with DCM, MeOH and DMF for several times, and drained. Add Fmoc-Arg(pbf)-OH (1.53mmol), HOBt (0.25g, 1.83mmol), DIC (0.28mL, 1.83mmol), DMF (10mL) into the solid phase reactor, and react at 20°C for 40min. The resin was washed and dried to obtain Fmoc-Arg(pbf)-Rink Amide resin, and the measured resin substitution degree was 0.35 mmol / g. Add 8 mL of blocking reagent (acetic anhydride (mmol): DIPEA (mmol) = 1:1) to the resin, react for 2 h, block the remaining amino groups, and use DCM...

Embodiment 2

[0095] Embodiment 2: Bactericidal experiment of SEQ No.1~10 and its compound preparation

[0096] 1. Main experimental materials

[0097] BaCl 2 (AR), H 2 SO 4 (AR), KH 2 PO 4 , Na 2 HPO 4 , SEQ No.1-8 (the test concentration is 40 μg / ml, 50 μg / ml, 60 μg / ml), nutrient agar medium, Sabouraud agar medium, etc.

[0098] Experimental strains: Staphylococcus aureus (ATCC 6538), Escherichia coli (CMCC 8099), Candida albicans (ATCC10231)

[0099] 2. Main experimental instruments

[0100] BT125D balance, BSA224s balance, DT-1001A balance, JC101 electric drum drying oven, UPT-1-10T Youpu purification machine, LD2M-40KCS vertical pressure steam sterilizer, YSEI immortal mold incubator, Sujing Antai clean work Taiwan SW-CJ-1FD, centrifuge, pipette gun, microporous filter head, etc.

[0101] 3. Experimental steps

[0102] (1) Preparation of bacteria-stained samples: Take the nutrient agar medium slant of the 3rd-14th generation of the strain and culture it freshly (18-24h), was...

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PUM

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Abstract

The invention provides a Protegrin-1 antimicrobial peptide derivative and a preparation method and application thereof. The preparation method of the Protegrin-1 antimicrobial peptide derivative comprises the steps that linear polypeptide is synthesized; the linear polypeptide is synthesized into cyclase polypeptide, the Cys in the fifth position and the fourth position and the Cys in the seventh position and the twelfth position of the amino acid sequence in the cyclase polypeptide form two pairs of disulfide bonds. According to the Protegrin-1 antimicrobial peptide derivative and the preparation method and the application thereof, molecule improvement is performed on the Protegrin-1 antimicrobial peptide by replacing amino acid in corresponding positions, the antibacterial peptide derivative which is high in antibacterial activity, low in hemolytic activity and more stable in protease is screened by a lot of activity experiments, the artificial synthesis of the group of antibacterial peptides is simple and the cost is lower, the derivative is beneficial for industrial production, and excellent candidate peptides are provided for the research and development of novel antibacterial agents.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a novel antimicrobial peptide derivative used in medicine and a preparation method thereof. Furthermore, the present invention also relates to preparations or combined preparations for killing microorganisms such as bacteria or fungi. Background technique [0002] With the large-scale and inappropriate use of traditional antibiotics, the problem of bacterial resistance has become increasingly serious. A large number of microorganisms and bacteria that can widely tolerate antibiotics have appeared clinically. The existing antibiotics are effective against these pathogenic microorganisms and pathogenic diseases. Bacteria are powerless. Antibacterial peptides, also known as antimicrobial peptides or host defense peptides, are an important component of the body's innate immunity and the first barrier for many organisms to resist the invasion of foreign pathogenic bacter...

Claims

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Application Information

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IPC IPC(8): C07K7/08A61K38/10A61P31/04A61P31/10A61K31/198A61K31/722
CPCC07K7/08A61K31/198A61K31/722A61K38/00A61K2300/00
Inventor 苏贤斌林山武明
Owner 成都山信药业有限公司
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