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Application of oxazolone compound as streptococcus mutans biofilm inhibitor

A streptococcus mutans and inhibitor technology, which is applied in the application field of oxazolone compounds as streptococcus mutans biofilm inhibitors, can solve the problems of weak effect, fluorosis, and poor effect, and achieve strong pertinence and solute molecular weight Small, inhibitory effects on formation and maturation

Active Publication Date: 2015-05-20
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the anti-caries effect of fluoride is controversial: firstly, excessive intake of fluoride may cause fluorosis; secondly, fluoride has a selective effect on the site of action of teeth, and has a poor effect on caries of pits and fissures on the occlusal surface; at the same time , fluoride has little effect on dental plaque, and cannot completely control caries from the perspective of etiology (Cheng et al., 2007)

Method used

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  • Application of oxazolone compound as streptococcus mutans biofilm inhibitor
  • Application of oxazolone compound as streptococcus mutans biofilm inhibitor
  • Application of oxazolone compound as streptococcus mutans biofilm inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: the preparation of the culture of bacterial strain and liquid inhibitor

[0031] Preparation of test strains:

[0032] The test strain in this example involves Streptococcus mutans (strain number: 32401; obtained from China Medical Bacteria Collection and Management Center, website: http: / / www.cmccb.org.cn / ).

[0033] Components and preparation of medium:

[0034] Components of bovine heart and brain infusion (for convenience of description, hereinafter referred to as BHI) liquid medium and its preparation method: 37g of commercially available BHI powder (the BHI powder was purchased from Sigma, USA, item number: 53286) was added to 1000mL of distilled water Medium, high temperature and high pressure (121.3°C, 103.4kPa) sterilization for 15 minutes, cooled for later use. This liquid medium is a typical liquid medium for planktonic culture of Streptococcus mutans.

[0035]Components of BHI sucrose liquid medium and its preparation method: 37 g of commerc...

Embodiment 2

[0041] Embodiment 2: Inhibitor experiment on the formation of Streptococcus mutans biofilm

[0042] According to the aseptic procedure of Example 1, the Streptococcus mutans suspension (bacteria number: 32401) of Example 1 was inoculated respectively in BHI sucrose liquid medium containing different concentrations of inhibitors, to determine the inhibitory effect on Inhibitory activity of Streptococcus mutans biofilm formation. The specific method is: according to the ratio of 1:100, inoculate the Streptococcus mutans suspension in Example 1 into BHI sucrose containing inhibitors at a final concentration of 0.05 μg / mL, 0.5 μg / mL, 5 μg / mL and 50 μg / mL respectively. In liquid medium, at 37 °C, facultative anaerobic (5% CO 2 ) for 16 hours. Then, carefully suck out the planktonic bacteria and supernatant in the 48-well plate, and use pH = 7.4, 0.01M phosphate buffer solution (the buffer solution is purchased from Thermo Company, USA, product number: P5368. The content of one ba...

Embodiment 3

[0043] Embodiment 3: Inhibitor experiments on the inhibition of Streptococcus mutans biofilm maturation

[0044] According to the aseptic operation procedure of Example 1, first inoculate the Streptococcus mutans suspension (bacteria number: 32401) of Example 1 in BHI sucrose liquid medium to form a biofilm, and then add inhibitors of different concentrations respectively To determine the inhibitory activity of inhibitors on Streptococcus mutans biofilm maturation. The specific method is: inoculate the Streptococcus mutans suspension in Example 1 into a 48-well plate containing BHI sucrose liquid medium according to a dilution ratio of 1:100, and inoculate it at 37° C. under facultative anaerobic (5% CO 2 ) for 24 hours to form a biofilm. At this point, add inhibitors at final concentrations of 5 μg / mL and 50 μg / mL to the biofilm cultures of Streptococcus mutans, respectively, and incubate at 37°C in facultative anaerobic (5% CO 2 ) to continue culturing for 48 hours. Then,...

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Abstract

The invention discloses an application of an oxazolone compound as a streptococcus mutans biofilm inhibitor, which belongs to the field of screening technologies of antibacterial drugs. The chemical name of the compound is 2-(4-chlorphenyl)-4-{[(6-methyl-2-pyridyl) amino] methylene}-1,3-oxazole-5((tetrahydro)-ketone, and an inhibitor formed by dissolving the oxazolone compound in DMSO can inhibit the formation and maturation of streptococcus mutans biofilms. The inhibitor has the advantages of small molecular weight, simple structure, good specificity and the like, can significantly inhibit the formation and maturation of biofilms of streptococcus mutans-a main pathogenic bacterium of caries, but has an unobvious influence on streptococcus mutans in a floating state. The inhibitor has an anti-caries potential and can be used as a candidate targeted drug of novel anti-caries strategies.

Description

technical field [0001] The invention belongs to the technical field of screening antibacterial drugs, and in particular relates to the application of a small molecular compound capable of inhibiting the formation and maturation of Streptococcus mutans biofilm, that is, an oxazolone compound as an inhibitor of Streptococcus mutans biofilm. Background technique [0002] Caries is the most common dental disease in humans, which causes progressive destruction of tooth color, shape, and texture, and seriously affects the pronunciation, chewing, and language functions of the oral cavity. Everyone is at risk of caries, whether they are infants, adolescents or adults. Dental caries has become a common oral health and public health problem worldwide (Jeon et al., 2011). The World Health Organization has listed it together with tumors and cardiovascular diseases as the three major diseases of human beings. [0003] Oral Streptococci, especially Streptococcus mutans, are the main car...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61P31/04A61P1/02
Inventor 李雨庆陈卢璐任智李明云李继遥邹静
Owner SICHUAN UNIV
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