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New antibacterial application of cyanine dye ir780

A technology of dyes and cyanines, which can be used in antibacterial drugs, medical preparations containing active ingredients, and resistance to media-borne diseases. It can solve the problems of direct antibacterial effects that have not been reported, and achieve the effect of alleviating bacterial infections.

Active Publication Date: 2022-05-10
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, IR780 is mainly used as a fluorescent probe for in vivo and in vitro imaging, as well as laser-assisted phototherapy, but its direct antibacterial effect has not been reported at home and abroad.

Method used

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  • New antibacterial application of cyanine dye ir780
  • New antibacterial application of cyanine dye ir780
  • New antibacterial application of cyanine dye ir780

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Embodiment 1: IR780 is measured to the MIC value of bacteria

[0079] According to the microbroth dilution method recommended by the American Clinical Laboratory Standards Institute (CLSI), the MIC of standard strains and clinical isolates of IR780 was determined, and the MIC results were judged mainly according to the CLSI M100-S25 (2015) standard. Use MH medium to dilute the drug to 512, 256, 128, 64, 32, 16, 8, 4, 2, 1 μg / mL, respectively add to the first 10 wells of a 96-well U-shaped plate, and use MH medium to detect strains diluted to 10 5 -10 6 CFU / mL, add 100 μL per well into the drug-containing wells, add 100 μL medium in the 11th hole as a negative control, and add 100 μL bacterial solution in the 12th well as a positive control. Place in a 37°C incubator for 12-16 hours, read the results, and the minimum concentration that inhibits bacterial growth is the MIC value. In order to ensure the accuracy of the experimental results, the experiment was repeated ...

Embodiment 2

[0083] Embodiment 2: IR780 is measured to the time sterilization curve of bacteria

[0084] The strains in Table 1 were grown to the logarithmic phase of the bacteria solution (OD 600 =0.8~1) Dilute 1:1000 times, take 1mL of the diluted bacterial solution and add it to the shaker tube. According to the experimental results of MIC, different concentrations of IR780 (0-32 μg / mL) were incubated with the bacterial liquid at 37°C and 250 rpm, and the control group did not add the liquid. 30 μL was taken at 0, 3, 6, 9, 12, and 24 h to coat the plate. After the plate was placed at 37°C for 12-16 hours, count single colonies and draw a growth curve to observe the growth trend of bacteria.

[0085] The result is as Figure 1-11 As shown in Figure A, the bacteria in each control group grew and multiplied rapidly within 0-12 hours, and the bacteria grew in a stable period within 12-24 hours. After adding different concentrations of IR780, the growth of each bacterium was significantl...

Embodiment 3

[0086] Example 3: Effect of IR780 on Bacterial DNA Extravasation

[0087] The strains in Table 1 were grown to the logarithmic phase of the bacteria solution (OD 600 =0.8~1) Dilute 1:1000 times with MH broth, take 1mL of the diluted bacterial solution and add it to the shaker tube. According to the experimental results of MIC, drug concentrations of 1 / 4MIC, 1 / 2MIC and MIC were selected to incubate with bacterial solution at 37°C and 250rpm, and the control group did not add drug solution. After incubation for 12 hours, centrifuge at 12000 rpm for 2 minutes, collect the supernatant, and measure the DNA content in the supernatant with a micro-spectrophotometer.

[0088] The result is as Figure 1-11 As shown in Figure B, in order to detect the effect of IR780 on the permeability of the bacterial cell membrane, the extravasation of intracellular macromolecular substances (DNA) was further measured after adding the drug. After incubation for 12 hours, 1 / 4MIC, 1 / 2MIC and MIC of ...

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Abstract

The invention belongs to the field of biomedicine, and specifically relates to the new application of cyanine dye IR780 or an acceptable salt thereof as an antibacterial drug. The specific performance is that IR780 has obvious inhibitory effect on Gram-positive bacteria Staphylococcus aureus and Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii. Destroying the cell membrane of the bacteria, increasing its permeability, leading to DNA extravasation, and degrading the DNA and soluble proteins of the bacteria. The invention provides a new choice for the current application of the cyanine dye IR780, and has new clinical application prospects.

Description

technical field [0001] The invention belongs to the technical field of biomedicine and relates to the new application of cyanine dye IR780, in particular to the application of IR780 or an acceptable salt thereof in inhibiting bacterial infection. Background technique [0002] The current abuse of antibiotics leading to bacterial resistance has become a worldwide problem, therefore, it is imperative to find new and highly effective antibacterial drugs. [0003] IR780 is a lipophilic cationic small molecule cyanine dye, which belongs to the indole tricarbocyanine dye, and has a maximum absorption peak at the absorption wavelength of 780nm. The molecular formula of IR780 is C 36 h 44 ClIN 2 , the molecular weight is 667Da, and its structural formula is as follows: [0004] [0005] At present, IR780 has gained widespread attention due to its excellent characteristics. First, it can accumulate in tumor sites without coupling with tumor-targeting ligands; Imaging fluoresc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/404A61P31/04
CPCA61K31/404A61P31/04Y02A50/30
Inventor 陈刚范雪莲宗荣玲
Owner YANGZHOU UNIV
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