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Application of fluorine-containing catechol structure compound serving as mycobacterium tuberculosis inhibitor

A technology of mycobacterium tuberculosis and catechol, which is applied in the fields of biomedicine and chemistry, can solve the problems of long treatment cycle and achieve the effect of inhibiting proliferation and increasing expression level

Active Publication Date: 2017-02-22
INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The treatment cycle of drug-resistant tuberculosis is longer than that of ordinary patients, and the cost of treatment is 100 times that of ordinary patients

Method used

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  • Application of fluorine-containing catechol structure compound serving as mycobacterium tuberculosis inhibitor
  • Application of fluorine-containing catechol structure compound serving as mycobacterium tuberculosis inhibitor
  • Application of fluorine-containing catechol structure compound serving as mycobacterium tuberculosis inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1, the direct inhibitory action of test drug to Mycobacterium tuberculosis

[0036] Test drug: 3-fluorocatechol, product of Sigma-Aldrich, product number 344656.

[0037] Adjust the concentration of Mycobacterium bovis BCG 1173P2 to OD 600 The reading value is 0.05 (corresponding to 1.5×10 7 CFU / mL), seeded in 96-well plate, 99 μL per well. Add 1.0 μL of the 2-fold concentration gradient dilution solution of the test drug to each well, and incubate at 37°C for 72 hours. 4.879 μM, 9.758 μM, 19.516 μM, 39.032 μM, 78.064 μM, 156.128 μM, 312.256 μM, 624.512 μM; at the same time set positive control rifampicin group (that is, there is BCG 1173P2 strain in the incubation system, but no test drug is added, and was added rifampicin), negative control dimethyl sulfoxide group (DMSO group, only 1 μL of DMSO was added). put each group in The fluorescence value of GFP was detected under the Multilabel Reader fluorescence microplate reader, the excitation wavelength...

Embodiment 2

[0039] Example 2, the inhibitory effect of the test drug on Mycobacterium tuberculosis in macrophages

[0040] Test drug: 3-fluorocatechol, product of Sigma-Aldrich, product number 344656.

[0041] THP-1 cells were divided into 5×10 5Cells / mL were inoculated in 96-well plates, 100 μL per well, differentiated with phorbol ester (PMA) at a final concentration of 100 ng / mL for 24 hours, and then the cells adhered to the wall to obtain macrophages derived from THP-1 cells. Macrophages derived from THP-1 cells were infected with Mycobacterium bovis BCG 1173P2 at an infectivity of MOI=10 for 4 hours. Wash away extracellular BCG 1173P2 with PBS, add 199 μL of 1640 medium containing 10% (volume fraction) fetal bovine serum, and then add 1 μL of each test drug at different concentrations, so that the final concentrations in the system are 2.440 μM and 4.879 μM respectively , 9.758 μM, 19.516 μM, 39.032 μM, 78.064 μM, 156.128 μM, 312.256 μM, 624.512 μM, continue to incubate for 48 hou...

Embodiment 3

[0046] Example 3, Test of Induced Effect of Test Drugs on Intracellular Nitric Oxide in Macrophages Infected by Mycobacterium tuberculosis

[0047] Test drug: 3-fluorocatechol, product of Sigma-Aldrich, product number 344656.

[0048] THP-1 cells were divided into 5×10 5 Cells / mL were inoculated in 96-well plates, 100 μL per well, and differentiated with 100 ng / mL phorbol ester (PMA) for 24 hours to adhere to the wall to obtain macrophages derived from THP-1 cells. Macrophages derived from THP-1 cells were infected with Mycobacterium bovis BCG 1173P2 at an infectivity of MOI=10 for 4 hours. Wash away extracellular BCG 1173P2 with PBS, add 199 μL of 1640 medium containing 10% (volume fraction) fetal bovine serum, and then add 1 μL of each test drug at different concentrations, so that the final concentrations in the system are 5 μM, 20 μM, and 78 μM respectively , 312μM, and continue to incubate for 3h, 6h, 12h and 24h, respectively. After drug action at different times, dis...

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Abstract

The invention discloses an application of a fluorine-containing catechol structure compound serving as a mycobacterium tuberculosis inhibitor. The application is the specific application of the fluorine-containing catechol structure compound in preparing medicine for treating and / or preventing disease caused by mycobacterium tuberculosis inflection. Experiments show that the fluorine-containing catechol structure compound (such as 3-fluorocatechol) has the direct inhibiting effect on growth of mycobacterium tuberculosis, proliferation of the mycobacterium tuberculosis in macrophage can be inhibited, and the expression level of nitric oxide in the macrophage inflected by the mycobacterium tuberculosis can be improved. In addition, cytotoxicity tests also show that the fluorine-containing catechol structure compound (such as the 3-fluorocatechol) is free of obvious toxic and side effects, and in cell pharmacodynamics tests, in the effective dose range, obvious toxicity change of cells does not appear. Therefore, the fluorine-containing catechol structure compound is of great significance in researching and developing novel antituberculosis medicine.

Description

technical field [0001] The invention belongs to the fields of biomedicine and chemistry, and relates to the application of a fluorine-containing catechol structure compound as an inhibitor of mycobacterium tuberculosis. Background technique [0002] Tuberculosis (TB) is a respiratory infectious disease caused by Mycobacterium tuberculosis (MTB). my country is now one of the 22 countries with a high burden of tuberculosis in the world, and the number of tuberculosis patients ranks second in the world. [0003] Multidrug resistance and extensive drug resistance are the key factors restricting the clinical use of antimicrobials. These phenomena also exist in anti-tuberculosis drugs. The latest epidemiological survey shows that more than 40% of tuberculosis infection cases are resistant to at least one second-line drug. The treatment cycle of drug-resistant tuberculosis is longer than that of ordinary patients, and the cost of treatment is 100 times that of ordinary patients....

Claims

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Application Information

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IPC IPC(8): A61K31/055A61P31/04
Inventor 张立新马荣代焕琴纪增春崔金辉王钦钦宋福行
Owner INST OF MICROBIOLOGY - CHINESE ACAD OF SCI
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