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Cyclopeptide capable of resisting multi-drug-resistant bacteria and application of cyclopeptide

A technology for multi-drug-resistant bacteria and multi-drug resistance, applied in the direction of antibacterial drugs, peptides, pharmaceutical formulations, etc., can solve the problems of identifying antibacterial peptides, such as difficulty, and achieve broad-spectrum killing activity, strong operability, and low cost low effect

Active Publication Date: 2021-08-13
CHONGQING UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is difficult to identify effective antimicrobial peptides from a large number of peptide samples and predict their antibacterial activity experimentally

Method used

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  • Cyclopeptide capable of resisting multi-drug-resistant bacteria and application of cyclopeptide
  • Cyclopeptide capable of resisting multi-drug-resistant bacteria and application of cyclopeptide
  • Cyclopeptide capable of resisting multi-drug-resistant bacteria and application of cyclopeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] 1. CPeptide-A: (Arg-Arg-Trp-Trp-Trp-Arg), cyclic peptide synthesis.

[0050] Using Fmoc solid-phase peptide synthesis, with 2-CTC resin as the carrier, the fully protected peptide line peptide is first synthesized, then cyclized in the liquid phase, and finally the crude peptide is obtained by ether precipitation after deprotection with TFA solution.

[0051] Swell 1g of initial resin with 10ml of DCM at room temperature for 30min;

[0052] The first amino acid coupling operation:

[0053] Weigh the protected amino acid Fmoc-Arg(Pbf)-OH with a total resin substitution value of 3eq and add it to the DCM solution, then add DIEA with a total resin substitution value of 9eq for dissolution, and add the dissolved clear solution to the resin for coupling After reacting for 3 hours, the waste liquid was discharged and washed 3 times with DMF.

[0054] The second amino acid coupling operation:

[0055] Remove the Fmoc protecting group: add 5ml 20% PPD / DMF reagent to the reac...

experiment example 1

[0081] Bactericidal activity detection of experimental example 1 cationic antimicrobial cyclic peptide

[0082] Various bacterial strains used in the following examples were purchased from China Institute for the Control of Biological Products.

[0083] Adopt agar punching method to detect the bactericidal activity of cationic antibacterial cyclic peptide, and use the cationic antibacterial peptide LfcinB64-9 RRWQWR synthesized by solid-phase chemical method as contrast, to evaluate CPeptide-A, CPeptide-B, CPeptide-C in the present invention , CPeptide-D, CPeptide-E, CPeptide-F bactericidal activity.

[0084] Measure the bactericidal activity of antimicrobial peptides according to the following steps:

[0085] Strain recovery: inoculate drug-resistant Acinetobacter baumannii, streak in NA nutrient agar medium, and place in a constant temperature incubator for cultivation at a temperature of 37°C for 16-20 hours.

[0086] Strain culture: Pick a single colony and place it in 1...

experiment example 2

[0093] Antibacterial Activity Detection of Experimental Example 2 Cationic Antibacterial Cyclic Peptide

[0094] Various bacterial strains used in the following examples were purchased from China Institute for the Control of Biological Products.

[0095] Determination of the minimum antibacterial ability of cationic antibacterial cyclic peptide, and the cationic antibacterial peptide LfcinB6 synthesized by solid-phase chemical method 4-9 RRWQWR is used as a control to evaluate the antibacterial ability of CPeptide-A, CPeptide-B, CPeptide-C, CPeptide-D, CPeptide-E and CPeptide-F of the present invention.

[0096] The antibacterial activity of the antimicrobial cyclic peptide was determined according to the following steps:

[0097] Collect the bacteria growing in the logarithmic phase, centrifuge at 4°C and 8000 rpm for 2 min, wash with normal saline three times, add fresh broth medium, and make the concentration of the bacterial suspension 2.0×105cfu / mL. Add 50uL of bacterial...

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PUM

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Abstract

The invention discloses a cyclopeptide capable of resisting multiple drug resistance bacteria and application of the cyclopeptide. The cyclopeptide is characterized in that the amino acid sequence of the cyclopeptide is any one of the following six types: R-R-W-W-W-R, R-W-R-W-R-W, R-R-W-W-W-R-R, R-R-W-W-R-R-W, R-R-W-W-W-W-R-R, and R-R-W-W-R-R-R-W. The antibacterial cyclopeptide is obtained by cyclizing any one of the above amino acid sequences. The invention provides six novel antibacterial peptides with artificially designed cations. The antibacterial peptides can be synthesized by adopting an Fmoc solid-phase chemical method. The cationic antibacterial peptide has broad-spectrum killing activity on multi-drug-resistant acinetobacter baumannii, staphylococcus aureus and escherichia coli, has no toxic effect on animal and plant cells, and is high in operability and low in cost.

Description

technical field [0001] The invention relates to a cyclic peptide against multidrug-resistant bacteria and its application, and relates to the field of cyclic peptides. Background technique [0002] With the widespread use of antibiotics in clinical practice, multidrug-resistant bacteria have also emerged and increased. In recent years, the emergence of the most common multidrug-resistant Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii) and Gram-positive bacteria (Staphylococcus aureus) causing nosocomial infections It is a growing problem and challenge worldwide. Facing the increasingly serious problem of drug resistance, however, enough drugs have not yet been developed to solve this problem. Polymyxins (such as colistin) have become the last effective means of treatment of drug-resistant bacterial infections again, so it is urgent to develop new drugs. Antimicrobials. [0003] Antimicrobial peptides (AMPs) are a class of short p...

Claims

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Application Information

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IPC IPC(8): C07K7/64A61K38/08A61P31/04
CPCC07K7/64A61P31/04A61K38/00Y02A50/30
Inventor 王远强何清秀李广平赵丽楠庹燕刘周李跃鹏
Owner CHONGQING UNIV OF TECH
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