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Polypeptide antibiotic and preparation method and application thereof

A technology of polypeptide antibiotics and antimicrobial peptides, applied in the field of antibiotics, can solve the problems of increasing morbidity and mortality, and achieve the effects of improving bactericidal effect, significant antibacterial effect, and efficient synthesis process

Active Publication Date: 2020-07-31
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, infection of implantable medical devices in the body often allows bacteria to form biofilms, which can protect bacterial cells from antimicrobial agents and immune defenses, leading to persistent infection and increased morbidity and mortality

Method used

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  • Polypeptide antibiotic and preparation method and application thereof
  • Polypeptide antibiotic and preparation method and application thereof
  • Polypeptide antibiotic and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0048] The preparation of embodiment 1 antimicrobial peptide

[0049] (1) Adopt the Fmoc solid-phase synthesis method, select the modified density of Wang resin to be 0.35, synthesize the polypeptide on the resin, remove the Fmoc protection of the amino terminal with the DMF solution of hexahydropyridine, and use the carboxyl group of the next amino acid with 4- The DMF solution of methylmorpholine and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate is activated, and then the condensation reaction with the first deprotected amino acid is carried out, and the above steps until the condensation of all amino acids is completed;

[0050] (2) The synthesized polypeptide is removed from the resin with a trifluoroacetic acid solution containing 2.5% water and 2.5% triisopropylsilane, and the side chain protection of the amino acid is removed simultaneously; The acetic acid was removed by rotary evaporation, and then the crude peptide was precipitated with anhydrous et...

Embodiment 2

[0056] The preparation of embodiment 2 polypeptide antibiotics

[0057] (1) Adopt Fmoc solid-phase synthesis method, select Wang resin with a modification density of 0.35, synthesize the SEQ ID NO.61 polypeptide on the resin, remove the Fmoc protection of the amino terminal with a DMF solution of hexahydropyridine, and convert the next amino acid The carboxyl group was activated with 4-methylmorpholine and benzotriazole-N,N,N',N'-tetramethyluronium hexafluorophosphate in DMF, and then reacted with the deprotected first amino acid Condensation reaction, repeat the above steps until the condensation of all amino acids is completed;

[0058] (2) wherein the synthesis step of connecting azidoacetic acid is consistent with the amino acid linking method in step (1);

[0059] (3) The synthesized polypeptide is removed from the resin with a trifluoroacetic acid solution containing 2.5% water and 2.5% triisopropylsilane, and the side chain protection of the amino acid is removed simul...

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Abstract

The invention provides a polypeptide antibiotic as well as a preparation method and application thereof. The polypeptide antibiotic comprises an antibacterial peptide and a nitric oxide donor, and theantibacterial peptide is connected to the nitric oxide donor. According to the polypeptide antibiotic, the antibacterial peptide is connected to the nitric oxide donor, the antibacterial peptide cooperates with nitric oxide, a biological membrane is dispelled, the sterilization effect is enhanced, bacteria forming the biological membrane are effectively killed, and the polypeptide antibiotic is wide in application range.

Description

technical field [0001] The invention belongs to the field of antibiotics and relates to a polypeptide antibiotic and its preparation method and application. Background technique [0002] Implantable medical devices such as intravascular catheters, heart valves, pacemakers, prosthetic joints, dialysis catheters, dental implants, orthopedic and trauma devices provide beneficial healthcare, treatment and rehabilitation to patients. However, medical device-associated infections have become increasingly important, causing undue patient suffering. [0003] Antimicrobial peptides (AMPs), also known as antimicrobial peptides or peptide antibiotics, are a class of small molecule polypeptides produced by specific bacterial genes and have broad-spectrum antibacterial properties. Antimicrobial peptides usually consist of 12-50 amino acid residues, have a molecular weight of less than 10kDa, and are amphipathic and cationic. The main biological function of antimicrobial peptides is tha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/46A61K38/17A61P31/04
CPCC07K14/46C07K19/00A61P31/04A61K38/00Y02A50/30
Inventor 王浩李莉莉黄张建费越
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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