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Application of celecoxib derivative OSU-03012 in preparation of anti-tubercle bacillus drugs

A technology for celecoxib and anti-tuberculosis bacteria, applied in antibacterial drugs, drug combinations, respiratory diseases, etc., can solve the unreported OSU-03012 and other problems, and achieve good clinical application prospects

Inactive Publication Date: 2018-10-23
SHANGHAI PULMONARY HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that there is no report in the prior art that OSU-03012 can be used as an anti-tuberculosis drug

Method used

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  • Application of celecoxib derivative OSU-03012 in preparation of anti-tubercle bacillus drugs
  • Application of celecoxib derivative OSU-03012 in preparation of anti-tubercle bacillus drugs
  • Application of celecoxib derivative OSU-03012 in preparation of anti-tubercle bacillus drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The C57BL / 6 mouse peritoneal primary macrophages were divided into 1*10 5 Each cell / well was inoculated in a 48-well cell culture plate. After about 2 hours for the cells to adhere to the wall, the complete medium 1640 was removed, and then fresh complete medium was added to culture overnight. The next day, 1 h before infection, replace with fresh 1640 containing 10% serum without double antibody, and add AR-12 at a final concentration of 1uM in the cell culture supernatant; use DMSO as a control well, place the cells in After culturing in the incubator for 1 h, the tubercle bacillus (H37Rv) was infected at a dose of MOI=5. After 2-3 hours of infection, discard the supernatant, then culture the cells with amikacin-containing medium for 2 hours, discard the supernatant and replace with 1640 containing 10% serum without double antibody and continue at 37°C for 5 %CO 2 Cells were cultured in the incubator for 24 h. Discard the supernatant and wash the cells with PBS, th...

Embodiment 2

[0030] The C57BL / 6 mice were divided into two groups, 6 in each group, and infected with Mycobacterium tuberculosis (H37Rv) by intraperitoneal injection, the dose was 2*10 6 Bacteria / mouse, 1 week after infection, orally administered 25 mg / kg and PBS as a control, and administered continuously for 3 weeks. The mice were sacrificed by dislocation of the cervical spine, and one lobe of the lung was taken out, fixed with 4% paraformaldehyde, paraffin sectioned, and H&E staining was performed to observe the pathological damage of the lung.

[0031] see figure 2 , given AR-12 at a dose of 100-200 mg / kg, after three weeks of oral administration, the pathological damage of the lungs of mice was significantly reduced; therefore, the experimental results of this example show that AR-12 can effectively reduce the damage of the lungs of mice. Pathological damage.

Embodiment 3

[0033] Take one-third of the mouse lung tissue administered three weeks after infection in Example 2, and grind it with 1 ml of PBS containing 1% triton-100, serially dilute, and take 10 -3 、10 -4Spread 100ml of tissue suspension evenly on Middle Brook 7H10 agar culture plate containing amphotericin B, then place it in a 37°C incubator for 2-3 weeks, and count the colonies. The results are as follows: image 3 shown.

[0034] The experimental results of this example show that AR-12 significantly reduces the bacterial load of Mycobacterium tuberculosis in the lungs of mice.

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PUM

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Abstract

The invention relates to the technical field of pharmaceutical chemistry, and in particular, relates to an application of a celecoxib derivative OSU-03012 in preparation of anti-tubercle bacillus drugs, and an application of the celecoxib derivative OSU-03012 in preparation of drugs for treatment of pulmonary tuberculosis, and also relates to an anti-tubercle bacillus drug composition. The celecoxib derivative OSU-03012 has anti-tubercle bacillus and anti-drug-resistant tubercle bacillus activities, so the celecoxib derivative OSU-03012 can be used as a leading compound in treatment of tubercle bacillus infectious diseases (such as pulmonary tuberculosis). Of course, the celecoxib derivative OSU-03012 itself can also be used for preparing the drugs for treating tuberculosis, thereby havinggood clinical application prospects.

Description

technical field [0001] The present invention relates to the technical field of medicinal chemistry, in particular to the application of celecoxib derivative OSU-03012 in the preparation of anti-tuberculosis drugs, and the application of celecoxib derivative OSU-03012 in the preparation of drugs for treating pulmonary tuberculosis , also relates to an anti-tuberculosis pharmaceutical composition. Background technique [0002] Mycobacterium tuberculosis (M.tuberculosis) is referred to as tubercle bacilli or Mycobacterium tuberculosis. As early as 1882, German bacteriologist Robert Koch (Robert Koch, 1843-1910) had proved that Mycobacterium tuberculosis is the pathogenic bacteria of tuberculosis. The bacteria can invade various tissues and organs of the whole body, but the most common infection is the lungs. [0003] Mycobacterium tuberculosis does not produce endotoxins and exotoxins, and its pathogenicity may be related to inflammation caused by bacteria multiplying in tiss...

Claims

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Application Information

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IPC IPC(8): A61K31/415A61P31/06A61P11/00
CPCA61K31/415A61P11/00A61P31/06
Inventor 戈宝学陈建霞刘峰李蒿蒿刘海鹏郑瑞娟刘忠华
Owner SHANGHAI PULMONARY HOSPITAL
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