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Use of protegrin-1 antimicrobial peptide derivatives in the preparation of anti-oral pathogenic bacteria drugs

A technology for pathogenic bacteria and uses, applied in antibacterial drugs, drug combinations, topical antibacterial agents, etc., can solve the problems of oral mucosa irritation, heavy bitterness, taste changes, etc., achieving better therapeutic effect, good application prospects, clear effect

Active Publication Date: 2022-03-08
成都山信药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The most commonly used non-antibiotic chemicals in the oral cavity, such as chlorhexidine, have a very heavy bitter taste. At therapeutic concentrations, patients are basically unwilling to use it if the taste is not modified. Therefore, the chlorhexidine products on the market now require Add a lot of flavors and other flavoring agents
The second disadvantage is that long-term use will stain the surface of the oral mucosa and teeth, yellow the tongue coating, and change the sense of taste.
The third disadvantage is that chlorhexidine is easy to cause irritation to the oral mucosa, and long-term use is not conducive to the protection of oral health
Antimicrobial peptide Protegrin-1 (PG-1) is a porcine antimicrobial peptide composed of 18 amino acid residues isolated from porcine neutrophils. Currently, a series of derivatives are developed based on Protegrin-1. Staphylococcus aureus, Escherichia coli and Candida albicans all have good bactericidal activity, but there is no literature report on the use of specific Protegrin-1 derivatives to kill oral pathogens, let alone specific Protegrin-1 derivatives Bibliographical reports on the preparation of stable formulations for the treatment of various oral diseases

Method used

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  • Use of protegrin-1 antimicrobial peptide derivatives in the preparation of anti-oral pathogenic bacteria drugs
  • Use of protegrin-1 antimicrobial peptide derivatives in the preparation of anti-oral pathogenic bacteria drugs
  • Use of protegrin-1 antimicrobial peptide derivatives in the preparation of anti-oral pathogenic bacteria drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] The preparation of embodiment 1 anti-oral oral pathogenic bacteria medicine of the present invention

[0067] Weigh 60-500mg of the Protegrin-1 antimicrobial peptide derivative shown in any one of SEQ ID NO.1~SEQ ID NO.8, 600-5000mg of polylysine, and then weigh one or more stabilizers (according to the types and proportions in Table 4), the components are dissolved in distilled water, pre-frozen at -20°C, frozen at -80°C, and freeze-dried to obtain a condensed mixture of functional ingredients and stabilizers. Then this mixture is dissolved with distilled water, and the volume is adjusted to 1 L, and the spray for treating oral diseases is obtained.

Embodiment 2

[0068] Embodiment 2 Preparation of anti-oral pathogenic bacteria medicine of the present invention

[0069] Weigh 40 mg of the Protegrin-1 antimicrobial peptide derivative shown in SEQ ID NO.1 to SEQ ID NO.8, 440 mg of polylysine, then weigh 10 mg of cysteine ​​and 80 mg of valine, and mix the components After dissolving in distilled water, it was pre-frozen at -20°C, frozen at -80°C, and freeze-dried to obtain a mixture. Then this mixture is dissolved with distilled water, and the volume is adjusted to 1 L, and the spray for treating oral diseases is obtained.

Embodiment 3

[0070] Example 3 Investigation of the killing effect of the polypeptide of the present invention on oral pathogenic bacteria

[0071] 1. Preparation of different peptide samples

[0072] Polylysine, Protegrin-1, polypeptides shown in SEQ ID NO.1-SEQ ID NO.10 and their complexes were used as samples respectively to study the effect of different polypeptides on oral pathogenic bacteria.

[0073] The drug formulation is shown in Table 1.

[0074] Table 1 Recipe of different polypeptide samples

[0075]

[0076]

[0077] Table 1 (continued) Recipe of different polypeptide samples

[0078]

[0079] Remark:

[0080] The sequence of Protegrin-1 is: ArgGlyGlyArgLeuCys Tyr CysArgArgArgPheCys Val CysVal GlyArg;

[0081] h 2 N-RGGRLCYCRRRFCVCVGR-CONH 2

[0082] The sequence of SEQ No.9 is:

[0083] h 2 N-Arg-Gly-Gly-Leu-{D-Cys}-Tyr-Cys-Arg-Gly-Arg-Phe-Cys-Val-Cys-Val-Gly-Arg-CONH 2 ;

[0084] h 2 N-RGGLCYCRGRFCVCVGR-CONH 2

[0085] The sequence of SEQ No.10 is:

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Abstract

The present invention provides the use of a polypeptide with an amino acid sequence as shown in any one of SEQ ID NO.1 to SEQ ID NO.8 in the preparation of drugs against oral pathogenic bacteria. The invention also provides a medicine against oral pathogenic bacteria and its application. The Protegrin-1 antimicrobial peptide derivatives of the specific sequence of the present invention can specifically kill various oral pathogenic bacteria, and can be used for the treatment and prevention of oral diseases, and the prepared specific preparation has strong stability and has a therapeutic effect on oral diseases. Better, good application prospects.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to the use of Protegrin-1 antibacterial peptide derivatives in the preparation of drugs against oral pathogenic bacteria. Background technique [0002] There are a large number of various types of bacteria in the human oral cavity, including various normal flora or pathogenic bacteria. Among them, the normal flora of the oral cavity are represented by Streptococcus sanguis and Streptococcus salivarius, which play a role in maintaining the normal health and normal function of the host. Oral pathogens are closely related to oral diseases. Common oral pathogens include Porphyromonas gingivalis, Prevotella intermedia, Fusobacterium nucleatum, Streptococcus mutans, and Actinobacillus concomitante. Among them, Porphyromonas gingivalis belongs to Gram-negative anaerobic bacteria and is the main pathogenic bacteria causing chronic periodontitis, mainly colonizing in gingival sulcus a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/10A61P31/02A61P31/04A61P1/02C07K7/08
CPCA61K38/10A61P1/02A61P31/02A61P31/04C07K7/08
Inventor 林山伍明斯蒂文·林
Owner 成都山信药业有限公司
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