Application of echinatin serving as inhibitor

A technology of licorice chalcone and inhibitor, applied in the field of biomedicine and medicine

Active Publication Date: 2020-02-11
THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no clinical application of related drugs in the treatment of NLRP3 inflammasome or other inflammasome-related diseases. Therefore, the development of NLRP3 inflammasome inhibitors to inhibit the abnormal activation of NLRP3 inflammasome will help alleviate the above-mentioned inflammatory diseases. diseases and new avenues for treatment

Method used

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  • Application of echinatin serving as inhibitor
  • Application of echinatin serving as inhibitor
  • Application of echinatin serving as inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] This example is used to illustrate that licorice chalcone can significantly inhibit the processing, maturation and release of IL-1β after ATP-induced NLRP3 inflammasome activation.

[0048] 1. Cultivation and differentiation of mouse bone marrow-derived macrophages (BMDMs): Take C57BL / 6 mice about 10-12 weeks old, kill them by dislocation, separate the bilateral femurs of the mice on an ultra-clean table, and absorb DMEM with a fine needle for culture Bone marrow cells were washed out from the base, and the cells were repeatedly blown away, then transferred to a 50mL centrifuge tube, centrifuged at room temperature, and the supernatant was removed, and the cells were resuspended in DMEM medium with 10% fetal bovine serum (FBS) and 1% double antibody. At the same time, macrophage colony-stimulating factor (M-CSF) was added at a final mass concentration of 25 ng mL -1 , BMDMs were obtained after 5 days of cell culture.

[0049] 2. The NLRP3 inflammasome activation model ...

Embodiment 2

[0053] This example is used to illustrate that licorice chalcone can inhibit the enzymatic activity of caspase-1 p20 in NLRP3 inflammasome.

[0054] 1. Acquisition and collection of BMDMs: BMDMs cell culture supernatants induced by LPS-stimulated ATP and niridinectin respectively, the same as steps 1 and 2 of Example 1. The cell culture supernatant was 1 Inflammasome Assay detection kit was used to measure caspase-1p20 enzyme activity, and the detection was carried out according to the instructions of the kit, and finally detected by PromegaGloMax 20 / 20 luminescence detector, the results were as follows Figure 5 and 6 .

[0055] in conclusion: 1Inflammasome Assay detection kit is an effective tool for detecting caspase-1p20 enzyme activity at present. Figure 5-6 The results showed that licorice chalcone can inhibit caspase-1p20 enzyme activity in a dose-dependent manner.

Embodiment 3

[0057] This example is used to illustrate that licorice chalcone inhibits ASC multimerization.

[0058] 1. Seed BMDMs cells in a 6-well plate (at a density of 8.5×10 5 well), after overnight, 50ng / mL LPS was induced for 4 hours, licochalcone 40uM was added to act for 1 hour, and then different NLRP3 inflammasome stimulating factors were added to act for the corresponding time. Aspirate the supernatant, add 500 μL pre-cooled Triton lysate [50mM Tris-HCl (pH 7.5), 150mM NaCl, 0.5% Triton X-100, and EDTA-free protease inhibitor cocktail (Roche)] to each well, and let it stand for 15 Minutes later, centrifuge at 6000g for 15 minutes, discard the supernatant, add pre-cooled PBS to wash twice, then resuspend in 200 μL of PBS, directly add suberic acid bis(N-hydroxysuccinimide ester) to make it final The concentration was 2 mmol / L, and the reaction was carried out at 37 degrees Celsius for 30 minutes. Then centrifuge at 6000g for 15 minutes, remove the supernatant, add 30 μL of 2× ...

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Abstract

The invention discloses application of echinatin serving as an inflammation inhibitor. The echinatin can serve as an inflammasome inhibitor, and can inhibit formation of apoptosis-associated speck-like protein (ASC) spots as well as subsequent activation of caspase-1 p20 and secretion of IL-1beta. The echinatin can serve as a potential drug for treating of diseases related to abnormal activation of inflammasomes.

Description

technical field [0001] The invention belongs to but not limited to the fields of biomedicine and medicine, and particularly relates to the use of licochalcone as an inflammasome inhibitor and its application in the treatment of related diseases. Background technique [0002] The inflammasome is mainly composed of receptor protein, apoptosis-associated speck-like protein (ASC) and pro-caspase-1. Protein complexes; among them, receptor proteins include a variety of NOD-like receptor protein families such as NOD-like receptor family 3 (NLRP3), NOD-like receptor family caspase activation recruitment domain 4 (NLRC4), melanoma Lack of factor 2 (AIM2) protein and pyrin. When cells are stimulated by pathogen associated molecular pattern (pathogen associated molecular pattern, PAMP) or danger associated molecular pattern (danger-associated molecular pattern, DAMP), it will promote the assembly and activation of inflammasome, pro-caspase-1 self-cleavage to generate activity Caspase...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P19/06A61P9/10A61P1/16A61P31/00A61P25/00A61P37/00A61P25/28A61P25/16A61P31/04
CPCA61K31/122A61P1/16A61P9/10A61P19/06A61P25/00A61P25/16A61P25/28A61P31/00A61P31/04A61P37/00
Inventor 柏兆方肖小河徐广付书彬
Owner THE FIFTH MEDICAL CENT OF CHINESE PLA GENERAL HOSPITAL
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