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Antibacterial auxiliary material having bacterial conditioning characteristic as well as preparation method and application of antibacterial auxiliary material

A technology of auxiliary materials and bacteria, applied in the field of pharmacy, to achieve the effect of protecting toxic and side effects, improving antibacterial efficacy, and promoting phagocytosis

Active Publication Date: 2020-11-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the toxic and side effects of antimicrobial peptides or nanosilver in these combined strategies are still worrying, and it will be of great significance to develop new non-antibiotic treatment strategies for combined treatment

Method used

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  • Antibacterial auxiliary material having bacterial conditioning characteristic as well as preparation method and application of antibacterial auxiliary material
  • Antibacterial auxiliary material having bacterial conditioning characteristic as well as preparation method and application of antibacterial auxiliary material
  • Antibacterial auxiliary material having bacterial conditioning characteristic as well as preparation method and application of antibacterial auxiliary material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 2-Chlorobenzotrichlorotoluene resin (0.4 mmol, 100-200 mesh, 1% DVB) was placed in a synthesis column and immersed in DCM until the resin was completely dissolved. Fmoc-L-lys-OH was introduced into the reactor, and 0.5 mL of HBTU was used as the condensation agent. After reacting for 2 h under nitrogen stirring, the resin was washed 3 times with DMF and DCM. Then, 15 ml of the deprotection solution was added to the obtained Fmoc-protected amino acid resin. Subsequently, the Fmoc-amino acid-OH was reacted with the resin by the condensing agent HBTU according to the amino acid sequence from the C-terminus to the N-terminus in the expected lipopolysaccharide-binding protein mimetic peptide WKVRKSFFKLQGK. After each condensation reaction, the resin was washed alternately with DMF and methanol. A portion of the resin was then removed and examined by the ninhydrin method. The condensation is complete when the resin develops a pale yellow color. The resulting polypeptide w...

Embodiment 2

[0035] 2-Chlorobenzotrichlorotoluene resin (0.4 mmol, 100-200 mesh, 1% DVB) was placed in a synthesis column and immersed in DCM until the resin was completely dissolved. Fmoc-amino acid(biotin)-OH was introduced into the reactor, and 0.5 mL of HBTU was used as a condensing agent. After reacting for 2 h under nitrogen stirring, the resin was washed 3 times with DMF and DCM. Then, 15 ml of the deprotection solution was added to the obtained Fmoc-protected amino acid resin. Subsequently, Fmoc-amino acid-OH was reacted with the resin by the condensing agent HBTU according to the amino acid sequence from the C-terminus to the N-terminus in the expected mimetic peptide FHRNHRSPVTLL. After each condensation reaction, the resin was washed alternately with DMF and methanol. A portion of the resin was then removed and examined by the ninhydrin method. The condensation is complete when the resin develops a pale yellow color. The resulting polypeptide was cleaved from the resin and p...

Embodiment 3

[0037] 2-Chlorobenzotrichlorotoluene resin (0.4 mmol, 100-200 mesh, 1% DVB) was placed in a synthesis column and immersed in DCM until the resin was completely dissolved. Fmoc-L-lys-OH was introduced into the reactor, and 0.5 mL of HBTU was used as the condensation agent. After reacting for 2 h under nitrogen stirring, the resin was washed 3 times with DMF and DCM. Then, 15 ml of the deprotection solution was added to the obtained Fmoc-protected amino acid resin. Subsequently, Fmoc-amino acid-OH was reacted with the resin by the condensing agent HBTU according to the amino acid sequence from the C-terminus to the N-terminus in the expected mimetic peptide FHRNHRSPVTLL. After each condensation reaction, the resin was washed alternately with DMF and methanol. A portion of the resin was then removed and examined by the ninhydrin method. The condensation is complete when the resin develops a pale yellow color. The resulting polypeptide was cleaved from the resin and purified b...

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Abstract

The invention discloses an antibacterial auxiliary material having a bacterial conditioning characteristic as well as a preparation method and application of the antibacterial auxiliary material. Theantibacterial auxiliary material is a natural opsonin protein or an opsonoid compound formed by a mimic peptide and a phagocytic effect promoting related material. The invention also discloses an antibiotic prodrug formed by chemically coupling the antibacterial auxiliary material with antibiotics, and preparation and application of an antibiotic-entrapped nano preparation taking the antibacterialauxiliary material as a prescription component. The antibiotic prodrug is prepared from the antibacterial auxiliary material and the antibiotics or derivatives thereof through a mixed anhydride method or a liquid phase synthesis method. According to the antibacterial auxiliary material, bacteria can be delivered to the surfaces of immune cells while the bacteria are adhered in a targeting manner,the ingestion of the immune cells is activated, the phagocytosis of macrophages to the bacteria is promoted, and the purpose of immune sterilization is achieved. The antibiotic prodrug and an antibiotic nano preparation are used to achieve combined treatment of antibiotic treatment and immune cell sterilization, so that the antibacterial drug effect is improved, and besides, the antibacterial spectrum is expanded.

Description

technical field [0001] The invention relates to an antibacterial auxiliary material with bacterial conditioning properties, a preparation method and application thereof, and belongs to the technical field of pharmacy. Background technique [0002] Antibiotics, as compounds that can kill or inhibit the growth of bacteria, have brought many infectious diseases that have seriously endangered human life and health under control. However, as the problem of bacterial drug resistance has become increasingly prominent, it is difficult to completely kill bacteria with a single antibiotic drug treatment, and the development speed of new antibiotic drugs is lower than the speed of bacterial drug resistance. Therefore, in recent years, researchers have gradually turned their attention to how to deliver antibiotics and other antibacterial drugs to the site of infection. This treatment method can selectively enrich a large number of drugs around pathogenic bacteria, effectively fight dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/395A61K38/17A61K38/10A61K38/16A61K47/54A61K47/55A61K47/34A61K9/107A61K9/127A61P31/04
CPCA61K39/39533A61K38/1732A61K38/10A61K38/16A61K47/549A61K47/557A61K47/545A61K47/55A61K47/34A61K9/1075A61K9/127A61P31/04Y02A50/30
Inventor 张文丽刘建平刘欣悦
Owner CHINA PHARM UNIV
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