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Applications of small-molecular inhibitor MLN4924 in preparation of drug for inhibiting bleomycin-induced pulmonary fibrosis

A technology for small molecule inhibitors and pulmonary fibrosis, applied in the biological field, can solve problems such as little known effects

Inactive Publication Date: 2016-06-29
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous research reports on MLN4924 mostly focused on its anti-tumor properties by blocking the cancer cell cycle or causing apoptosis, but little is known about its role in the inflammatory response

Method used

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  • Applications of small-molecular inhibitor MLN4924 in preparation of drug for inhibiting bleomycin-induced pulmonary fibrosis
  • Applications of small-molecular inhibitor MLN4924 in preparation of drug for inhibiting bleomycin-induced pulmonary fibrosis
  • Applications of small-molecular inhibitor MLN4924 in preparation of drug for inhibiting bleomycin-induced pulmonary fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1 tracheal administration

[0054] In this study, animal disease models were established by tracheal instillation. First, lightly anesthetize the mouse with ether. The appropriate level of anesthesia is for the mouse to lose consciousness but keep breathing evenly. Grab the mouse with the right hand, stretch the neck, and expose the mouth. Use a 20 μL capillary blood collection needle along the tongue of the mouse. Insert 0.05mL of BLM (5mg / kg) down about 2cm, be careful not to go too deep so as not to damage the tissues around the throat. Judging from the symptoms, if the mouse has shortness of breath, rapid heartbeat, and the liquid level in the capillary blood collection needle drops rapidly, it means into the trachea. After the infusion was completed, the mouse was rotated upright for about 1 min, so that the instilled medicinal solution could be evenly distributed in both lungs.

Embodiment 2

[0055] Embodiment 2 intraperitoneal injection

[0056] In this study, MLN4924 intervention was carried out by intraperitoneal injection. After the mice were fixed by the grasping method described above, their abdomens were disinfected with alcohol cotton balls. Make it head down and belly up before injection to prevent the needle from piercing the internal organs. After stabbing the skin obliquely at a 45° angle with the beveled surface of the needle facing upwards, turn the needle straight down and pierce a little to enter the abdominal cavity. Contamination of the skin by leakage of the injected fluid or loss of the injected dose. The needle insertion site should not be too close to the upper abdomen or too deep to protect internal organs.

Embodiment 3

[0057] Example 3 Alveolar Lavage Fluid Collection and Total Protein Determination

[0058] 1. Collection of alveolar lavage fluid:

[0059] After sacrificing the mouse by neck dissection, cut the skin of the neck to expose the trachea, gently cut a small hole at the distal end, insert a venous indwelling needle for fixation, inject 1 mL of pre-cooled PBS buffer solution, and draw back after staying for 30 seconds. After lavage twice, the lavage fluid was centrifuged at 1500 rpm for 5 min, and the supernatant was taken to detect the total protein content and cytokines in BALF by BCA protein quantification method.

[0060] 2. Determination of total protein

[0061] The total protein content in the alveolar lavage fluid was determined by the BCA protein quantification method, and the specific operation was as follows:

[0062] (1) Take 1.2mL of the protein standard preparation solution in the kit and add it to a tube of protein standard, fully dissolve and prepare a 25mg / mL pro...

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Abstract

The invention discloses an application of a small-molecular inhibitor MLN4924 in preparation of a drug for inhibiting bleomycin-induced pulmonary fibrosis. The invention also discloses an application of the small-molecular inhibitor MLN4924 in preparation of a drug for inhibiting an early inflammation process of bleomycin-induced pulmonary fibrosis. The invention also discloses an application of the small-molecular inhibitor MLN4924 in preparation of a drug for inhibiting activation of NF-[kappa]B and MAPK signal pathways in inflammatory reactions.

Description

technical field [0001] The present invention relates to the field of biotechnology, in particular to the application of MLN4924, a small molecule inhibitor of NEDD8 activating enzyme, in the preparation of drugs for inhibiting bleomycin-induced pulmonary fibrosis, and the use of MLN4924 in the preparation of NF-κB and The application of drugs that activate the MAPK signaling pathway. Background technique [0002] Pulmonary fibrosis is a disease that seriously endangers human health. It is usually caused by severe external trauma, infection, spontaneous immune response, adverse drug side effects and other factors, causing permanent damage to the lungs, resulting in repeated damage to the extra-alveolar matrix and excessive repair. Reconstruct and deposit, eventually leading to changes in normal lung tissue structure and loss of function. Pulmonary fibrosis is a serious disease characterized by permanent damage to the lungs and associated with high mortality, for which there ...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P11/00A61P29/00
Inventor 王平邓琦张娇娇
Owner EAST CHINA NORMAL UNIV
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