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Novel applications of tranilast

A disease and inflammasome technology, applied in the field of medicinal chemistry, can solve problems such as ineffective treatment, and achieve the effect of preventing and treating type 2 diabetes

Inactive Publication Date: 2018-12-07
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although these drugs targeting IL-1 have curative effect on some diseases (Dinarello et al., 2013, SeminImmunol), IL-1 is not the only effector molecule produced after activation of NLRP3 inflammasome, nor is it induced by NLRP3 inflammasome Therefore, drugs targeting IL-1 cannot effectively treat all NLRP3 inflammasome-related diseases

Method used

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  • Novel applications of tranilast
  • Novel applications of tranilast
  • Novel applications of tranilast

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. TR inhibits the activation of macrophage NLRP3 inflammasome in vitro

[0039] 1. TR inhibits the secretion of IL-1β

[0040] 1. On the first day, the mouse bone marrow was taken, and cultured and differentiated in DMEM medium containing 20% ​​L929 cell (mouse fibroblast) culture supernatant for 4 days;

[0041] 2. On the fifth day, divide the BMDM cells into twelve-well plates, each well 6×10 5 cells;

[0042] 3. On the sixth day, the supernatant was removed, and 500 μL of opti-MEM medium containing bacterial lipopolysaccharide (LPS) (50 ng / ml) was added to each well. After three hours of treatment, they were divided into five groups for different treatments, and each group had six replicates. Holes, the specific grouping process is as follows:

[0043] Group 1: Add 0.5 μL DMSO to each well for half an hour;

[0044] The second group: Add 0.5 μL DMSO to each well for half an hour, then add Nigericin to a final concentration of 5 μM, and then treat for hal...

Embodiment 2

[0092] Example 2, TR inhibits the acute inflammation induced by urate crystals

[0093] 1. TR inhibits urate crystal (MSU) accumulation-induced peritonitis

[0094] 1. Select 10-week-old wild mice and divide them into three groups, with three mice in each group. The specific grouping process is as follows:

[0095] The first group: 50 μL DMSO was injected intraperitoneally first, and 300 μL PBS was injected half an hour later;

[0096] The second group: 50 μL DMSO was injected intraperitoneally first, and MSU was injected half an hour later, and the injection dose was 0.5 mg per mouse;

[0097] The third group: 200mg / kg TR was injected intraperitoneally first, and MSU was injected half an hour later, and the injection dose was 0.5mg per mouse;

[0098] 2. After six hours, inject 10ml PBS into the abdominal cavity of each group of mice, and take the peritoneal lavage fluid and centrifuge;

[0099] 3. The supernatant of the peritoneal lavage fluid obtained in step 2 was used ...

Embodiment 3

[0114] Example 3, TR can alleviate metabolic disorder syndrome

[0115] 1. TR prevents high-fat food-induced metabolic disorders

[0116] 1. Select 8-week-old C57BL / 6J WT wild mice and divide them into four groups, with 9 mice in each group. sodium);

[0117] The second group: use 60% high-fat diet to feed the mice, and give 300 μ L placebo (sodium cellulose) by intragastric administration every day;

[0118] The third group: mice were fed with 60% high-fat food, and TR was given by intragastric administration every day at a dose of 25 mg / kg;

[0119] The fourth group: mice were fed with 60% high-fat food, and TR was administered orally every day at a dose of 50 mg / kg;

[0120] 2. Monitor the body weight and food intake of the mice, and record and test the blood sugar, glucose tolerance and insulin sensitivity of the mice. See the results in Figure 8 .

[0121] from Figure 8 The results showed that mice fed with 60% high-fat food had faster body weight gain than normal f...

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Abstract

The invention belongs to the field of pharmaceutical chemistry, and provides novel applications of tranilast, and especially applications of tranilast in preparation of medicines used for treating NLRP3 inflammasome related diseases. It is shown by experiments that tranilast is capable of reducing IL-1beta and IL-18 maturation secretion, blocking obesity development, and preventing type II diabetes through specific inhibition on NLRP3 inflammasome activation, and treating peritonitis and gout caused by NLRP3 inflammasome stimulant urate crystal (MSU) accumulation, and Muckle Wells syndromes caused by NLRP3 mutation preferably at the same time.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a new application of Tranister, in particular to the application of Tranister in the preparation of drugs for preventing or treating diseases related to NLRP3 inflammasomes. Background technique [0002] NLRP3 is an important member of the NOD-like receptors (NLRs) family of intracellular pattern recognition receptors. It contains three domains, namely the LRR domain, the NATCH domain and the PYD domain. When stimulated by exogenous pathogen-associated molecular patterns (such as bacteria, fungi) or danger-related molecular patterns (such as urate crystals, saturated fatty acids), NLRP3 recruits the adapter protein ASC (apoptosis-associated speck-like protein containing CARD) and The pro-caspase-1 forms a multimeric complex called the NLRP3 inflammasome. After the NLRP3 inflammasome is assembled, it undergoes self-cleavage to form a shear-activated caspase-1, which...

Claims

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Application Information

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IPC IPC(8): A61K31/196A61P25/16A61P25/24A61P25/28A61P19/06A61P17/16A61P17/00A61P9/10A61P11/00A61P1/16A61P29/00A61P31/00A61P3/00A61P3/10A61P3/04
CPCA61K31/196
Inventor 周荣斌江维黄亿
Owner UNIV OF SCI & TECH OF CHINA
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