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Application of compound FDEFA1 in preparation of gram-positive coccus inhibitor

A gram-positive, gram-positive technology is applied in the field of compound FDEFA1 in the preparation of gram-positive coccus inhibitors

Pending Publication Date: 2022-01-21
FUDAN UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

According to reports, in recent years, due to the non-standard use of antibacterial drugs and the horizontal transmission of drug-resistant genes, the above-mentioned multi-drug-resistant strains of Gram-positive cocci continue to appear clinically, especially the vancomycin and linezolid-resistant strains. appear and become a difficult problem in clinical and therapeutic practice
In addition, because this type of bacteria is easy to form biofilm and has strong resistance to antibiotics, there is currently no effective drug for removing bacterial biofilm. Therefore, new antibiotics that specifically destroy biofilm and kill bacteria have more bactericidal effects. broad prospects

Method used

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  • Application of compound FDEFA1 in preparation of gram-positive coccus inhibitor
  • Application of compound FDEFA1 in preparation of gram-positive coccus inhibitor
  • Application of compound FDEFA1 in preparation of gram-positive coccus inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Compound FDEFA1 inhibits the activity of Enterococcus faecalis histidine kinase YycG

[0024] Obtain the Enterococcus faecalis histidine kinase YycG gene sequence (NC_017316) through the Pubmed database: design an NcoI restriction site at the 5' end of the sense strand primer, and design an XhoI restriction site at the 5' end of the antisense strand primer: sense: 5' -CATG CCATG G TCGAAAGACGGGAATTTGTTTCCAAT-3', the underlined part is NcoⅠ restriction site; antisense: 5'-CCG CTCG AG AGGTTCATATGGTAGTGAAATATAG-3', the underlined part is the XhoI restriction site; the target fragment of Enterococcus faecalis histidine kinase YycG was amplified by PCR with the above primers, and the restriction endonuclease (NcoI and XhoI) digestion reaction and T 4 DNA ligase ligation reaction, the above target fragments were connected with the pET28(a) vector, transformed into DH5α bacteria, positive colonies were selected, and sequencing confirmed the successful construct...

Embodiment 2

[0029] Embodiment 2 Compound FDEFA1 inhibits the growth of Gram-positive planktonic bacteria

[0030] Bacterial strains used in the antibacterial test: Enterococcus faecalis FB-1, Enterococcus faecium EF16M64, Staphylococcus aureus SA113, Staphylococcus epidermidis RP62A and Streptococcus agalactiae NSGC64.

[0031]The strain was cultured overnight, inoculated into 4 mL of fresh TSB medium at 1:200, and compound FDEFA1 was serially diluted with TSB medium (from 200 μM to 3.13 μM), and after dilution, 150 μL was added to the matching detection orifice plate of the Bioscreen instrument; Then add 150 μL of the above-mentioned bacterial solution to three replicate wells, and use the bacterial solution without compound as the positive control; set the parameters and read the OD every half an hour 600 Value, continuous monitoring for 24h, the obtained value draws the growth curve, and the experiment is repeated three times;

[0032] The results showed that the compound FDEFA1 could...

Embodiment 3

[0033] Antibacterial activity test of embodiment 3 compound FDEFA1 to 477 enterococci and streptococcus agalactiae clinical strains

[0034] This embodiment uses the micro broth dilution method recommended by the U.S. Clinical and Laboratory Standards Institute (CLSI) to detect the effect of compound FDEFA1 on 477 clinical strains (including 257 strains of Enterococcus faecalis; 102 strains of Enterococcus faecium; 118 strains of Streptococcus agalactiae). MIC value.

[0035] Resuscitate the bacteria, inoculate them in 5 mL of fresh TSB liquid medium, and cultivate overnight at 37°C with shaking at 220rpm; dilute the above-mentioned bacterial liquid with TSB medium to OD=0.1, place on a shaker at 37°C and shake and culture until logarithmic growth phase, Take 1 mL of the bacterial solution in the growth period and centrifuge it in a 1.5 mL EP tube, and dilute the bacterial cells with sterile saline to adjust the turbidity to 0.5 McFarland turbidity (that is, equivalent to 1.0×...

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Abstract

The invention belongs to the field of biotechnology, and relates to a novel application of a compound FDEFA1 in pharmacy, in particular to an application of a compound FDEFA1 in a formula (1) in preparation of a gram-positive coccus inhibitor. The compound FDEFA is used as an inhibitor for inhibiting gram-positive coccus YycG histidine kinase, and can inhibit growth of Gram-positive bacteria and formation of biological membranes; particularly, the compound has an inhibition effect on YycG kinase in an enterococcus faecalis two-component signal transduction system, and is used for inhibiting the formation of floating bacteria and biological membranes of enterococcus faecalis, enterococcus faecium, staphylococcus aureus, streptococcus agalactiae and staphylococcus epidermidis; the compound can be used for preparing a gram-positive coccus inhibitor and a medicine for resisting enterococcus faecalis infection or treating diseases caused by gram-positive bacterium infection.

Description

technical field [0001] The invention belongs to the field of biological technology, and relates to a new application of compound FDEFA1 in pharmacy, in particular to an application of compound FDEFA1 in the preparation of Gram-positive cocci inhibitors. As a small molecule inhibitor, the compound FDEFA can inhibit the growth of Gram-positive bacteria and inhibit the formation of biofilm. Background technique [0002] Enterococcus faecalis, Enterococcus faecium, Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus agalactiae are Gram-positive cocci, opportunistic pathogens, and one of the main pathogens of hospital infection. The prior art discloses that under normal conditions, the above-mentioned Gram-positive cocci colonize the human intestinal tract, skin, oral cavity, and urinary tract, which can cause skin and soft tissue infections, urinary tract infections, infective endocarditis, and abdominal infections. curative infection. According to reports, in ...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61P31/04
CPCA61K31/496A61P31/04
Inventor 瞿涤陈重郑金鑫余治健邓启文
Owner FUDAN UNIV
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