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Cation antibacterial peptides, their preparation method and application

An ion exchange chromatography, cyclic peptide technology, applied in the preparation method of peptides, antibacterial drugs, antifungal agents, etc., can solve the problems of high antibacterial activity and low hemolytic activity, and achieve the effect of significant bactericidal effect

Active Publication Date: 2012-11-07
SHANGHAI INST OF PHARMA IND +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Subbalakshmi and others artificially synthesized the C-terminal 15 amino acid residues (MCF) of Melittin. MCF contains most of the amphipathic fragments of Melittin, and its antibacterial activity is 5-7 times higher than that of Melittin, while its hemolytic activity is 300 times lower.

Method used

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  • Cation antibacterial peptides, their preparation method and application
  • Cation antibacterial peptides, their preparation method and application
  • Cation antibacterial peptides, their preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: Preparation and purification of AMP-1

[0046] Sequence: Phe-Leu-Phe-Leu-Phe-Leu-Lys-Lys-Arg-Lys-Lys-Arg-Lys-His-NH 2 (SEQ ID NO: 1)

[0047] (1) Materials and reagents

[0048] Rink Amide MBHA resin, substitution value 0.41mmol / g.

[0049] The amino acids to be protected are Fmoc-L-Arg(Pbf)-OH, Fmoc-L-Leu-OH, Fmoc-L-Lys(Boc)-OH, Fmoc-L-Phe-OH and Fmoc-L-His (Trt)-OH.

[0050] Reagents: HOBt, DIC, DMF, piperidine.

[0051] (2) Instrument

[0052] PSI300 peptide synthesizer, Waters600 semi-preparative high performance liquid chromatography, magnetic stirrer.

[0053] (3) Operation steps (take 0.25mmol as an example)

[0054] a. Solid-phase chemical synthesis of peptides

[0055] Weigh 0.61g of Rink Amide MBHA resin, put it in the reactor of the peptide synthesizer, add 10mL of DMF, soak for 2h, then add 15mL of 20% PIP / DMF solution, mix for 30min to remove the amino protecting agent, and wash the resin 7 times with DMF , then add 619.8mg Fmoc-L-His...

Embodiment 2

[0070] Embodiment 2: Preparation and purification of AMP-2 and AMP-3

[0071] Sequence: Phe-Leu-Leu-Phe-Leu-Leu-Lys-Lys-Arg-Lys-Lys-Arg-Lys-His-NH 2 (SEQ ID NO: 2)

[0072] Trp-Trp-Trp-Phe-Trp-Trp-Lys-Lys-Arg-Lys-Lys-Arg-Lys-His-NH 2 (SEQ ID NO: 3)

[0073] (1) Materials and reagents

[0074] Rink Amide MBHA resin, substitution value 0.41mmol / g.

[0075] Required protected amino acids Fmoc-L-Arg(Pbf)-OH, Fmoc-L-Leu-OH, Fmoc-L-Lys(Boc)-OH, Fmoc-L-Phe-OH, Fmoc-L-Trp( Boc)-OH and Fmoc-L-His(Trt)-OH.

[0076] Reagents: HOBt, DIC, DMF, piperidine.

[0077] (2) Instrument

[0078] PSI300 peptide synthesizer, Waters600 semi-preparative high performance liquid chromatography, magnetic stirrer.

[0079] (3) Operation steps (take 0.25mmol as an example)

[0080] AMP-2 and AMP-3 were prepared and purified in a manner similar to the steps a-c in Example 1, and the fractions with a purity greater than 99% were collected and then concentrated to dryness at 50°C under reduced pressu...

Embodiment 3

[0082] Embodiment 3: Preparation and purification of cationic antimicrobial peptides in table 2

[0083] The cationic antimicrobial peptides in Table 4 were prepared and purified in a similar manner to Example 1, but the cationic antimicrobial peptides involved in the present invention are not limited thereto.

[0084] Table 4 Cationic Antimicrobial Peptides

[0085]

[0086]

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PUM

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Abstract

The invention belongs to the field of medicines and specifically relates to a set of cation antibacterial peptides with broad-spectrum antibacterial activity, their preparation method and an application thereof. The general formula of an amino acid sequence of the cation antibacterial peptides provided by the invention is X-(C)m-(B)n-His-X.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a group of cationic antibacterial peptides with broad-spectrum antibacterial activity, their preparation method and application. Background technique [0002] Since the discovery of penicillin, antibiotics have been a powerful weapon for humans to treat pathogenic microbial infections. However, with the abuse of traditional antibiotics, more and more pathogenic bacteria have begun to develop resistance to traditional antibiotics. Therefore, it is urgent to find a new class of antibacterial drugs. Use instead of antibiotics. [0003] Cationic antimicrobial peptides are cationic (rich in arginine and lysine) polypeptides produced by plants and animals, generally composed of 12-50 amino acid residues, which can protect the host from external pathogenic microorganisms. The antibacterial spectrum of cationic antimicrobial peptides is wider than that of traditional antibiotics. Cat...

Claims

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Application Information

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IPC IPC(8): C07K7/08C07K7/64C07K1/06C07K1/04C07K1/107A61K38/10A61K38/12A61P31/04A61P31/10
CPCY02P20/55
Inventor 冯军路建光张喜全徐宏江吴勇朱裕辉杨洁
Owner SHANGHAI INST OF PHARMA IND
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