Anti-microbial lipopenic compound with target function and preparation method thereof

An antibacterial lipopeptide and complex technology, applied in the direction of antibacterial drugs, liposome delivery, etc., can solve the problem of little research on targeting, and achieve the effects of avoiding drug resistance, high antibacterial activity, and long duration of action

Inactive Publication Date: 2017-03-22
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, there are few studies on the targeting of bacterial cell membranes based on carriers. Studies by Neoh et al. have shown that using glucose and mannose units as chemotactic agents can effectively target bacteria in the process of sugar transport in bacterial cell membranes.

Method used

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  • Anti-microbial lipopenic compound with target function and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0029] The active peptide (RLARIVVIRVAR) was synthesized by Fmoc (9-fluorenylmethoxycarbonyl) solid-phase synthesis using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and N-hydroxy The active peptide-palmitic acid (Palm) was coupled with succinimide (NHS) to obtain the lipopeptide product RLARIVVIRVAR-Palm. Glycolipids were prepared by coupling oligosaccharides with dipalmitate phosphatidylethanolamine (DHPE purchased from sigma) by reductive amination. Add the tetrasaccharide solution to a polytetrafluoroethylene bottle, add DHPE, and the molar ratio of the two is 32:1. Add chloroform / methanol / water mixed solution, add freshly prepared NaCNBH after ultrasonic bath 3 , continue to react for 72 hours. Take an appropriate amount of lipopeptide and pseudoglycolipid, add chloroform / methanol mixed solvent, and ultrasonically treat the probe intermittently for 30 minutes to prepare the antibacterial lipopeptide complex.

Embodiment 2

[0031] Active peptide (RIWVIWRR) was synthesized by solid-phase synthesis using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and N-hydroxysuccinimide (NHS) coupling Active peptide-stearic acid (Stearic), to obtain the lipopeptide product RIWVIWRR-Stearic. Take the hexasaccharide solution and add it to a polytetrafluoroethylene bottle, add DHPE, and the molar ratio of the two is 32:1. Add chloroform / methanol / water mixed solution, add freshly prepared NaCNBH after ultrasonic bath 3 , continue to react for 48 hours. Take an appropriate amount of lipopeptide and pseudoglycolipid, add chloroform / methanol mixed solvent, and ultrasonically treat the probe intermittently for 15 minutes to prepare the antibacterial lipopeptide complex.

[0032] The minimum inhibitory concentration and minimum bactericidal concentration of lipopeptide-mimicking glycolipid complex liposomes to different bacterial species were evaluated by turbidity method and plate coating method. The results ar...

Embodiment 3

[0036] Active peptide (KRWWKWWRR) was synthesized by solid-phase synthesis, coupled with 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) and N-hydroxysuccinimide (NHS) Active peptide-lauric acid (Lauric), to obtain the lipopeptide product KRWWKWWRR-Lauric. Add the tetrasaccharide solution to a polytetrafluoroethylene bottle, add DHPE, and the molar ratio of the two is 32:1. Add chloroform / methanol / water mixed solution, add freshly prepared NaCNBH after ultrasonic bath 3 , continue to react for 72 hours. Take an appropriate amount of lipopeptide and pseudoglycolipid, add chloroform / methanol mixed solvent, and ultrasonically treat the probe intermittently for 30 minutes to prepare the antibacterial lipopeptide complex.

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Abstract

The invention discloses an anti-microbial lipopenic compound with a target function and a preparation method thereof. The anti-microbial lipopenic compound is prepared from lipopeptid and neoglycolipid which are self assembled in solution, wherein the lipopeptid and the neoglycolipid are similar in structure, the lipopeptid is prepared from bioactive peptide and a hydrophobic chain section, and the neoglycolipid is prepared from oligosaccharide and a similar hydrophobic chain section. According to the anti-microbial lipopenic compound with the target function, a glycosyl unit in the neoglycolipid is utilized as a chemotactic agent to target bacterial membranes, and the anti-microbial lipopeptid plays an anti-microbial role; thus, the anti-microbial lipopenic compound has the characteristics of being high in anti-microbial activity, long in action time, low in dosage and not prone to generating drug resistance.

Description

technical field [0001] The invention is an antibacterial lipopeptide complex with targeting function, relates to a material that can be used in biomedicine and other aspects, and belongs to the field of biomedical materials. Background technique [0002] In recent years, with the widespread use and abuse of antibiotics, multi-drug-resistant bacteria have emerged, and infections caused by multi-drug-resistant bacteria have posed a serious threat to human health. More importantly, the development of antibiotics is far behind the speed of bacterial resistance. In order to solve this problem, the main measures taken by researchers include research and development of new antibiotics, search for new drug targets, and use of drug carrier systems. [0003] Antimicrobial peptides are short peptides produced by the natural immune system in the host defense system and have a certain bactericidal effect, and have broad-spectrum antibacterial properties. Many antimicrobial peptides not...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/08A61K38/10A61K9/127A61K47/26A61K47/36A61P31/04
CPCA61K38/08A61K9/1272A61K38/10A61K47/26A61K47/36
Inventor 姚琛周宾
Owner SOUTHEAST UNIV
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