Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Application of Q-U50 and 488H in preparation of medicine for inhibiting activation of macrophage inflammasome

A technology of macrophages and inflammasomes, applied in the field of medicine, can solve problems such as difficulty passing through the blood-brain barrier, reduce addiction, high water solubility, etc., and achieve a good effect of macrophage inflammasome activation

Pending Publication Date: 2022-05-31
AIR FORCE MEDICAL UNIV
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Quaternized U50,488H is a new drug modified by κ-OR selective agonist U50,488H. Compared with U50,488H, it has higher water solubility and is not easy to pass through the blood-brain barrier, so it greatly reduces its addiction. It can relax blood vessels and inhibit vascular remodeling by activating κ-OR in cardiopulmonary tissue, but whether there is κ-OR on macrophages and whether activating this receptor can inhibit the activation of its inflammasome, thereby inhibiting the inflammatory response of HPH , progress in remission of HPH has not been reported so far

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Application of Q-U50 and 488H in preparation of medicine for inhibiting activation of macrophage inflammasome
  • Application of Q-U50 and 488H in preparation of medicine for inhibiting activation of macrophage inflammasome
  • Application of Q-U50 and 488H in preparation of medicine for inhibiting activation of macrophage inflammasome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The following experiments illustrate the effect of κ-opioid receptor agonist Q-U50,488H on inhibiting macrophage infiltration and inflammasome activation in HPH mice.

[0040] The κ-opioid receptor agonist Q-U50,488H is obtained by quaternary amination of U50,488H.

[0041] 1. Establishment and grouping of mouse HPH model

[0042] The mice were treated with hypoxia for 4 weeks. After the experiment, the mice were anesthetized, placed in the supine position, and the hemodynamics were detected for the RVSP and RV / (S+LV) of the mice. Experimental groups: normoxia group; normoxia+Q-U50, 488H; hypoxia group; hypoxia+Q-U50,488H; hypoxia+nor-BNI+Q-U50,488H, etc. n=5, ** P&& P## P<0.01 vs. Hypoxia+Q-U50 group (hypoxia group+Q-U50, 488H); the nor-BNI means κ-opioid receptor blocker.

[0043] 2. Immunofluorescence and H&E staining to detect the proliferation and hypertrophy of pulmonary small vessels, n=5, ** P&& P## P<0.01 vs. Hypoxia+Q-U50 group.

[0044] 3. Immunofluoresc...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicine, and relates to application of Q-U50 and 488H in preparation of a medicine for inhibiting activation of macrophage inflammasome, research shows that the Q-U50 and the 488H are kappa-opioid receptor stimulants, and the action mechanism of the kappa-opioid receptor stimulants Q-U50 and 488H in inhibition of activation of the macrophage inflammasome is as follows: the kappa-opioid receptor stimulants Q-U50 and 488H in inhibition of activation of the macrophage inflammasome by reducing PFKFB3 expression; further, the glycolysis level is inhibited, so that LPS-induced macrophage inflammasome activation is inhibited, and a research result provides a potential drug target and a treatment strategy for clinical treatment of pulmonary arterial hypertension inflammatory infiltration.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to the use of Q-U50,488H in preparing medicines for inhibiting macrophage inflammasome activation. Background technique [0002] Pulmonary artery constriction and remodeling are the main pathological changes in hypoxic pulmonary hypertension (HPH). Chronic inflammation has been shown to be the main cause of persistent pulmonary artery constriction and stenotic remodeling. Among them, the inflammatory response mediated by macrophages is an important part of chronic pulmonary inflammatory response. Excessive activation of inflammatory response mediated by macrophages can lead to apoptosis of pulmonary artery endothelial cells and proliferation of smooth muscle cells, resulting in remodeling of vascular structure, eventually leading to the occurrence of HPH. Depletion of macrophages significantly blocked hypoxia-induced lung chronic inflammatory response and progression of HPH. Altho...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K31/40A61P29/00A61P11/00A61P9/12A61P9/00
CPCA61K31/40A61P29/00A61P11/00A61P9/12A61P9/00
Inventor 李娟裴建明张敏王巧娟牛津张淑苗付锋李军刘亚莉冯娜顾晓明贾敏刘银姬
Owner AIR FORCE MEDICAL UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com