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Antibacterial peptide derivate and application thereof

A technology of antibacterial peptides and antibacterial drugs, which is applied in the field of hydrophobically modified antibacterial peptide DP7 derivatives, which can solve the problems of red blood cell toxicity, red blood cell destruction, red blood cell hemolysis, etc., and achieve good antibacterial activity, small molecular weight, freeze-dried and redissolved stability Effect

Active Publication Date: 2017-12-08
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, high-concentration DP7 will lead to hemolysis of red blood cells and death of mice after intravenous injection, indicating that high-concentration DP7 is toxic to red blood cells and will destroy red blood cells.

Method used

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  • Antibacterial peptide derivate and application thereof
  • Antibacterial peptide derivate and application thereof
  • Antibacterial peptide derivate and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1 Synthesis of Antimicrobial Peptide DP7 and Cholesterol Conjugate (DP7-C)

[0083] Antimicrobial peptide DP7 and hydrophobic segment conjugates are made of figure 1 Synthesized by the synthetic route shown. Wherein, the hydrophobic segment includes: cholesterol, cholic acid, palmitic acid, stearic acid, lauric acid and the like.

[0084] 2-chlorotrityl chloride Resin, whose name is 2-chlorotrityl chloride resin; Fmoc-RinkAmide MBHA Resin, whose name is 4-(2',4'-dimethoxyphenyl-fluorenylmethoxycarbonyl-ammonia Methyl)-phenoxyacetamido-methyl benzhydrylamine resin; Fmoc: fluorenylmethoxycarbonyl; pbf, tbu, Otbu, Trt, Boc are all protecting groups, the names are 2, 2, 4, 6, 7-pentamethyldihydrobenzofuran-5-sulfonyl, tert-butyl, tert-butoxy, trityl, tert-butoxycarbonyl.

[0085] Concrete synthesis method is as follows:

[0086] 1. Resin swelling activation and deprotection:

[0087] Swelling: Weigh 1.0g Rink MBHA (4-(2′,4′-dimethoxyphenyl-fluorenylmethoxycarbo...

Embodiment 2

[0109] The critical micelle concentration of embodiment 2 DP7-C

[0110] DP7-C can assemble into micelles in aqueous solution, we use pyrene fluorescence probe spectroscopy to detect the critical micelle concentration (CMC) of DP7-C.

[0111] Pyrene is insoluble in water, and the solubility of pyrene in water is about 6×10 -7 mol / L, but easily soluble in ethanol and ether. The aqueous fluorescence emission spectrum of pyrene has 5 fluorescence peaks, and the ratio of the light intensity I1 of the first emission spectrum of pyrene to the light intensity I3 of the third emission spectrum in aqueous solution (the ratio of the fluorescence intensity at 373nm to that at 384nm) is about 1.8. According to literature reports, since surfactants have a solubilizing effect on non-polar organic compounds, different concentrations of surfactants have different solubilizing abilities for pyrene. After exceeding the critical micelle concentration (CMC), the solubilization of the solution ...

Embodiment 3

[0113] Physical characteristics of embodiment 3 DP7-C micelles

[0114] We used atomic force microscopy and Malvern particle sizer to detect some physical characteristics of DP7-C micelles, such as particle size and Zeta potential.

[0115] 1. Atomic force microscope photography: Prepare different concentrations of DP7-C solutions, drop them on the mica sheet, let it dry naturally, and place the mica sheet coated with DP7-C on the atomic force microscope to take pictures.

[0116] 2. Detection of particle size and Zeta potential: Dissolve DP7-C in MilliQ water, measure the particle size and Zeta potential with a Malvern particle size analyzer, measure each sample 4 times, and take the average value.

[0117] 3. DP7-C appearance and solution state: Observe the appearance of MilliQ water, DP7-C aqueous solution and freeze-dried powder, and take pictures with a camera. a is MilliQ water, b is DP7-C dissolved in aqueous solution, c is the state of DP7-C freeze-dried powder after ...

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Abstract

The invention belongs to the field of biological medicines, mainly relates to an antibacterial peptide derivate and the application thereof, in particular to a hydrophobic modified antibacterial peptide DP7 derivate and the application thereof. The hydrophobic modified antibacterial peptide is characterized in that a hydrophobic fragment is coupled to nitrogen terminal of the antibacterial peptide to realize the hydrophobic modification. The invention also provides a micelle which is prepared through the hydrophobic modified antibacterial peptide, and the application of the hydrophobic modified antibacterial peptide and the micelle in preparation of antibacterial medicines, preparation of a nucleic acid transporter and the preparation of an immunologic adjuvant. The antibacterial peptide is small in molecular weight and can be conveniently synthesized through an Fmoc solid-phase multi-peptide synthesis method; the hydrophobic fragment based chemical synthesizing coupling method is simple and easy to carry out.

Description

technical field [0001] The invention belongs to the field of biomedicine, and mainly relates to antimicrobial peptide derivatives and applications thereof, especially hydrophobically modified antimicrobial peptide DP7 derivatives and applications thereof. Background technique [0002] Antimicrobial peptides, also known as host defense peptides (HDPs), generally consist of 12 to 100 amino acid residues, are a type of basic polypeptide, and most antimicrobial peptides are positively charged. Antimicrobial peptides have a broad-spectrum antibacterial effect, can effectively inhibit and kill fungi, viruses, parasites and other pathogens, and can selectively kill tumor cells, and are not easy to produce drug resistance. They constitute the first barrier for the host to defend against the invasion of pathogenic microorganisms. As an important component of the body's immune system, antimicrobial peptides have become potential drugs to replace antibiotics to prevent and control dise...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/08A61K38/10A61K9/107A61K39/39A61K48/00A61K47/54A61P35/00A61P31/04A61P31/10
CPCA61K45/00A61K9/127A61K31/7052A61K38/10A61K2300/00A61K39/39A61K9/107C07K7/08A61P31/04A61P31/10A01K2227/105A01K2267/0337A61K39/001135A61K39/001188A61K2039/53A61K2039/55561A61K38/00Y02P20/55A61K48/00Y02A50/30A61K47/6907A61K47/543A61K47/62A61K47/542A61K45/06C12N15/113C12N2310/14C12N2310/17
Inventor 杨莉门可何谷魏于全
Owner SICHUAN UNIV
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