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Application of indole-2-ketone compound in preparation of product for preventing and treating oral bacteria

A technology of ketone compounds and compounds, which is applied in the field of biomedicine, can solve the problems of high toxicity and difficult removal of deep biofilms in dentinal tubules, and achieve good selective effects

Inactive Publication Date: 2021-01-05
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sodium hypochlorite solution with a concentration of 0.5% to 5.25% is the most commonly used root canal disinfection and irrigation solution in clinical root canal therapy at present. It has good antibacterial effect and tissue dissolution effect, but it is highly toxic, and it is still harmful to the biofilm in the deep layer of dentinal tubules. Difficult to remove

Method used

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  • Application of indole-2-ketone compound in preparation of product for preventing and treating oral bacteria
  • Application of indole-2-ketone compound in preparation of product for preventing and treating oral bacteria
  • Application of indole-2-ketone compound in preparation of product for preventing and treating oral bacteria

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Embodiment 1. The in vitro antibacterial activity experiment of formula (I) compound

[0025] The preparation of Streptococcus mutans UA159, Streptococcus sanguis ATCC10556, Streptococcus villatum DL1 and Enterococcus faecalis bacterial strain ATCC29212 and formula (I) compound is as follows:

[0026]Streptococcus mutans UA159, Streptococcus sanguis ATCC10556, Streptococcus mutans DL1 and Enterococcus faecalis ATCC29212 strains used in the present invention are all model strains. The reference genome numbers in the NCBI database (www.ncbi.nlm.nih.gov / ) correspond to NC_004350, NC_009009, NC_009785 and NC_004668. Its optimum culture medium is preferably brain heart infusion (BrainHeartInfusion) medium (Braininfusionsolids12.5g / L, Beefheartinfusionsolids5.0g / L, Proteose peptone10.0g / L, Glucose2.0g / L, Sodiumchloride5.0g / L, Di- Sodium phosphate2.5g / L, pH7.4±0.2), static culture at 37°C, the most suitable condition for anaerobic culture.

[0027] The medium for cultivating...

Embodiment 2

[0046] Embodiment 2. The toxicity test of formula (I) compound to human oral cavity cell

[0047] The preparation of human oral keratinocyte HOK, human gingival epithelial cell HGE, human macrophage RAW, human periodontal ligament fibroblast PDLC, human osteosarcoma cell MG63 and formula (I) compound is as follows:

[0048] Human oral epithelial keratinocyte HOK, human gingival epithelial cell HGE, human macrophage RAW, human periodontal ligament fibroblast PDLC, and human osteosarcoma cell MG63 used in the present invention are all cell lines. The culture medium used is DMEM high-glucose medium (containing L-glutamine, 110mg / L sodium pyruvate)+10% fetal bovine serum+1% penicillin and streptomycin mixed solution

[0049] The compound of formula (I) was prepared according to the method described in Example 1.

[0050] The medium for culturing human oral keratinocytes HOK, human gingival epithelial cells HGE, human macrophages RAW, human periodontal ligament fibroblasts PDLC, a...

Embodiment 3

[0058] Embodiment 3. formula (I) compound is to oral cavity bacteria multi-species biofilm removal experiment

[0059] According to the method described in Example 1, Streptococcus mutans, Streptococcus sanguis, Streptococcus sanguinis bacterium liquid and formula (I) compound are prepared, will be in logarithmic phase Streptococcus mutans, Streptococcus sanguis with brain heart infusion-sucrose culture medium , Dilute Streptococcus streptococci to a final concentration of 1×10 5 CFU / mL, mix the three bacterial solutions 1:1:1 for use.

[0060] Add 300 μL of the mixed bacterial solution in (1) to a sterile U-Slide well plate (brand Ibidi, product number 80826), and culture in an anaerobic incubator at 37°C for 24 hours.

[0061] Add brain heart infusion-sucrose medium to prepare the concentration of the formula (I) compound that is 62.5 μ g / mL in each hole, control group adds the chlorhexidine of equal concentration, handles 3 times every day, each processing time is 5 Minut...

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Abstract

The invention discloses application of an indole-2-ketone compound with structural characteristics of a formula (I) in preparation of a product for preventing and treating oral bacteria, and belongs to the technical field of biological medicines. The compound has an excellent inhibiting or killing effect on planktonic bacteria of common pathogenic bacteria streptococcus mutans and Enterococcus faecalis and biological membranes thereof in an oral cavity in vitro; the compound has relatively low cytotoxicity to cells which can be contacted with an oral cavity under short-time exposure; and meanwhile, the compound has certain selectivity for killing biological membranes of oral pathogenic bacteria (S.mutans) and symbiotic bacteria (S.sanguinis and S.glodonii). Therefore, the compound shown inthe formula (I) can be used for preparing products for preventing and treating oral bacteria.

Description

Technical field: [0001] The invention relates to the use of indol-2-one compounds in the preparation of products for preventing and treating oral bacteria, and belongs to the technical field of biomedicine. Background technique: [0002] Caries is a chronic progressive disease that occurs in dental hard tissues, and its occurrence and development may be closely related to the ecological imbalance of dental plaque biofilm. Salivary proteins or glycoproteins form an acquired film on the tooth surface, and planktonic bacteria colonize and multiply rapidly to form a plaque biofilm. The microbial metabolism in the biofilm produces acid, local demineralization of the tooth tissue, and eventually tooth tissue defect. Streptococcus mutans (S.m) is currently recognized as one of the most important cariogenic bacteria in the formation of dental plaque biofilm and cariogenic process. Streptococcus mutans is a Gram-positive facultative anaerobic bacterium. On the basis of physical adso...

Claims

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Application Information

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IPC IPC(8): C07D405/06A61K31/454A61P1/02A61P31/02A61P31/04A61K8/49A61Q11/00
CPCA61K8/4973A61K31/454A61Q11/00A61P1/02A61P31/02A61P31/04C07D405/06
Inventor 杨涛徐欣罗有福彭显
Owner SICHUAN UNIV
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