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Application of piperlongumine in inhibition of NLRP3 inflammasome activation

A technology of inflammasome and piperamide, which is applied in the directions of anti-inflammatory agents, non-central analgesics, active ingredients of heterocyclic compounds, etc., can solve the problems of insignificant effects on normal cells and unreported effects

Pending Publication Date: 2022-02-22
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, many studies have found that perylene amide can selectively kill a variety of tumor cells, but has no obvious effect on normal cells, and the mechanism of action has been deeply explored. However, there is no report on the effect of perylene amide on the activation of NLRP3 inflammasome.

Method used

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  • Application of piperlongumine in inhibition of NLRP3 inflammasome activation
  • Application of piperlongumine in inhibition of NLRP3 inflammasome activation
  • Application of piperlongumine in inhibition of NLRP3 inflammasome activation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0049] This example is used to illustrate that perylene amide does not affect the activation of NLRC4 inflammasome and AIM2 inflammasome

[0050] (1) Cultivation and differentiation of mouse bone marrow-derived macrophages (BMDMs): same as step (1) of Example 1.

[0051] (2) Inoculate the differentiated cells into a 24-well plate, 2×10 per well 5 the cell density. After culturing overnight, the medium was replaced with opti-MEM, and 100ng / mL LPS was added for pretreatment for 3 hours, and then they were divided into two groups, which were treated with different concentrations of PL (0μM, 10μM) for 1 hour, and then The cells treated with PL were divided into three groups according to each group, and each group was as follows: no stimulation as the control group; stimulation with 5 μM nigericin for 30 minutes; cleaning after 0.5 h infection with Salmonella typhimurium BNCC124795 (Bei Na Biology) , and then add opti-MEM medium containing 50 μg / mL gentamicin to stimulate for 4 h...

Embodiment 7

[0068] This example is used to illustrate the inhibitory effect of perylene amide on the oligomerization of NLRP3 itself.

[0069] (1) Cultivation and differentiation of mouse bone marrow-derived macrophages (BMDMs): same as step (1) of Example 1.

[0070] (2) Inoculate the differentiated cells into a 12-well plate, 5×10 per well 5 the cell density. After culturing overnight, the medium was replaced with opti-MEM, and 100ng / mL LPS was added for pretreatment for 3 hours. After pretreatment, they were divided into three groups: one group was not treated as control, and one group was stimulated with 5 μM nigericin. For 30 minutes, one group was treated with 10 μM PL for 1 hour and then stimulated with 5 μM nigericin for 30 minutes. Using semi-denaturing agarose gel electrophoresis (SDD-AGE), the method is as follows: Discard the cell culture medium, add SDD-AGE cell lysate 100μl / well, lyse on a shaker at 4°C for 30min, centrifuge at 10,000rpm at 4°C for 10min, take Transfer th...

Embodiment 8

[0072] This example is used to illustrate that perylene amide can inhibit peritonitis induced by urate crystals

[0073] (1) Choose 7-8 weeks old C57BL / 6 male mice (with similar body weight) and divide them into three groups: the first group was injected with dimethyl sulfoxide (DMSO) first, and then injected with PBS one hour later as the control group; The first group was injected with DMSO, and then 0.5 mg of urate crystals (MSU, Themor Scientific Company, U 2875) was injected one hour later; the third group was first injected with 50 mg / kg perylene amide, and then 0.5 mg of MSU was injected one hour later.

[0074] (2) After 6 hours, the eyeballs were removed to take blood, and after the blood was taken, the mice were treated with cervical dislocation; 1mL PBS was injected into the abdominal cavity, and the abdominal cavity was gently filled to make it evenly filled, and then sucked out, and the sucked liquid was centrifuged at 3000rpm for 3 Minutes, the supernatant was us...

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Abstract

The invention discloses an application of piperlongumine in inhibition of NLRP3 inflammasome activation. It is found that piperlongumine can inhibit NLRP3 inflammasome activation induced by nigericin in mouse macrophages and human mononuclear macrophages, in addition, piperlongumine not only can inhibit classical NLRP3 inflammasome activation caused by nigericin, urate crystals, aluminum and other different NLRP3 inflammasome activators, but also can inhibit activation of non-classical NLRP3 inflammasome caused by intracellular LPS, can relieve peritonitis induced by urate crystallization, and can be used for treating NLRP3 inflammasome-related inflammatory diseases such as type II diabetes atherosclerosis, gout, rheumatic arthritis, rheumatoid arthritis and the like. The invention provides an effective way for treating Parkinson's multiple sclerosis, Alzheimer's disease and the like.

Description

technical field [0001] The invention relates to the fields of biology and medicine, in particular to the application of perylene amide in inhibiting the activation of NLRP3 inflammasome. Background technique [0002] Innate immunity is the body's first line of defense against pathogenic infection, which mainly triggers inflammation and protects the body through a series of pattern recognition receptors. When some pattern recognition receptors are activated by pathogenic microorganisms or "danger signals", they will act as sensor molecules and interact with the adapter protein ASC (apoptosis-associated speck-like proeincontaining a CARD, apoptosis-associated speck-like protein) and cysteine The acid protease caspase-1 constitutes the cytoplasmic protein complex, that is, the inflammation body (Inflammation). The activated inflammasome mediates the self-cleavage activation of caspase-1. On the one hand, the activated caspase-1 promotes the maturation and secretion of pro-infl...

Claims

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Application Information

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IPC IPC(8): A61K31/36A61P29/00A61P9/10A61P19/06A61P19/02A61P25/16A61P25/28
CPCA61K31/36A61P29/00A61P9/10A61P19/06A61P19/02A61P25/16A61P25/28
Inventor 温龙平赵晓敏张云娇刘榴
Owner SOUTH CHINA UNIV OF TECH
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