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c 24 h 24 no 6 o 2 the s 3 Use in the preparation of anti-tuberculosis drugs

An anti-tuberculosis and drug technology, applied in antibacterial drugs, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve problems such as the prevention or treatment of tuberculosis without mentioning the compound BPTES, and achieve huge market potential. The effect of in vivo survival and broad clinical application prospects

Active Publication Date: 2021-07-27
SHANGHAI PULMONARY HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] It can be seen that the prior art only discloses the effect of the compound BPTES on tumor suppression, but does not mention that the compound BPTES can be used for the prevention or treatment of tuberculosis

Method used

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  • c <sub>24</sub> h <sub>24</sub> no <sub>6</sub> o <sub>2</sub> the s <sub>3</sub> Use in the preparation of anti-tuberculosis drugs
  • c <sub>24</sub> h <sub>24</sub> no <sub>6</sub> o <sub>2</sub> the s <sub>3</sub> Use in the preparation of anti-tuberculosis drugs
  • c <sub>24</sub> h <sub>24</sub> no <sub>6</sub> o <sub>2</sub> the s <sub>3</sub> Use in the preparation of anti-tuberculosis drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Db / Db (leptin receptor (Lepr) mutant) peritoneal primary macrophages of C57BL / 6 mice and DB / db mice were mixed with 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 hour before infection, replace with fresh 1640 containing 10% serum without double antibody, and treat the cells with DMSO and compound BPTES (150nM) for 1 hour before infection with Mycobacterium tuberculosis, and then infect with a dose of MOI=5 Mycobacterium tuberculosis (H37Rv). After 2-3 hours of infection, discard the supernatant, then culture the cells with the medium containing amikacin for 2 hours, then discard the supernatant and replace with 1640 containing 10% serum without double antibody and continue at 37°C, 5%CO 2 Cells were cultured in the incubator for 24 h. Discard the supernatant and wash the c...

Embodiment 2

[0036] The C57BL / 6 mice were divided into two groups, and the Db / db mice were divided into two groups, with 6 mice in each group, which were infected with Mycobacterium tuberculosis (H37Rv) by intranasal drip at a dose of 200 CFU / mouse for 1 week. Afterwards, the compound BPTES was administered continuously for 3 weeks by 5 mg / kg / day dose, and pure water was used as negative control. 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.

[0037] see figure 2 , it can be seen that the pathological damage of the lungs of mice treated with the compound BPTES was significantly reduced; therefore, the experimental results of this embodiment show that the compound BPTES (ie C 24 h 24 N 6 o 2 S 3 ) can effectively reduce the pathological damage of mouse lung.

Embodiment 3

[0039] Take one-third of the mouse lung tissue administered one month after infection in Example 2, and grind it with 1 ml of PBS containing 1% triton-100, serially dilute, and take 10 -3 、10 -4 100ml of the tissue suspension was spread evenly on the MiddleBook 7H10 agar culture plate containing amphotericin B, then placed in a 37°C incubator for 2-3 weeks, and the colony counting was completed. The results were as follows: image 3 shown.

[0040] The experimental results of this embodiment show that the compound BPTES (i.e. C 24 h 24 N 6 o 2 S 3 ) significantly reduced the load of Mycobacterium tuberculosis in the lungs of mice.

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Abstract

The present invention provides C 24 h 24 N 6 o 2 S 3 The invention has a new application in preparing anti-tuberculosis drugs, and provides a pharmaceutical composition for preventing or treating pulmonary tuberculosis. C 24 h 24 N 6 o 2 S 3 It can replenish α-KG to inhibit the expression of macrophage autophagy-related genes, restore the autophagy function of macrophages, and effectively inhibit the survival of Mycobacterium tuberculosis in vivo, so it can effectively inhibit the infection of Mycobacterium tuberculosis. Therefore, C 24 h 24 N 6 o 2 S 3 Can be used as a lead compound for the treatment of pulmonary tuberculosis and / or extrapulmonary tuberculosis, and C 24 h 24 N 6 o 2 S 3 It is also particularly suitable for preparing medicines for preventing or treating tuberculosis, thus having broad clinical application prospects and huge market potential.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to C 24 h 24 N 6 o 2 S 3 The use in preparing anti-tuberculosis drugs also relates to a pharmaceutical composition for preventing or treating pulmonary tuberculosis. 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. Mycobacterium tuberculosis does not produce endotoxins and exotoxins, and its pathogenicity may be related to inflammation caused by bacteria multiplying in tissue cells, toxicity of bacterial components and metabolites, and immune damage to bacterial components. Mycobacterium tuberculosis c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/433A61P31/06A61K45/06
CPCA61K31/433A61K45/06A61P31/06
Inventor 戈宝学陈建霞刘峰刘海鹏李蒿蒿王菲刘忠华唐芬黄晓辰王洁
Owner SHANGHAI PULMONARY HOSPITAL
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