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Application of liver X receptor activator in anti-nerve inflammatory reaction

A receptor activator, anti-neuritis technology, applied in nervous system diseases, amide active ingredients, drug combinations, etc., to achieve the effect of small side effects

Inactive Publication Date: 2013-02-13
XINXIANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In spinal cord injury, experimental cerebral apoplexy and other diseases have the effect of inhibiting inflammatory response, but the effect of LXR activator on inflammatory response in senile dementia has not been reported

Method used

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  • Application of liver X receptor activator in anti-nerve inflammatory reaction
  • Application of liver X receptor activator in anti-nerve inflammatory reaction
  • Application of liver X receptor activator in anti-nerve inflammatory reaction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1T0901317

[0028] Example 1 Effect of T0901317 on the Deposition of Senile Plaques and Aβ Levels in the Brain of APP / PS1 Transgenic Mice

[0029] APP / PS1 transgenic Alzheimer's model mouse knock-in mouse / human APP695 cDNA (Swedish K595M / N596L) and human PS1 (exon 9-deleted variant) were purchased from the Laboratory of Neurobiology and Genetics, Rockefeller University, in the laboratory Breeding and rearing. The mice were kept in a clean cage with sufficient feed and drinking water, the room temperature was kept at about 23°C, and the light was maintained for 12 hours a day (6:00AM-6:00PM) with a fluorescent lamp. Forty 8-month-old adult male APP / PS1 transgenic mice were randomly divided into ① treatment group (T0901317 group) and ② control group (Vehicle group). Experimental mice were intervened by intragastric administration at regular times every day. The treatment group was intragastrically administered with LXR activator T0901317 (30 mg / kg / day body weight) (the drug concentration ...

Embodiment 2T0901317

[0037] Example 2 T0901317 reduces the protein expression of microglial inflammatory factors COX-2 and iNOS by inhibiting the NF-κB inflammatory signaling pathway

[0038] Experimental process: Isolation and purification of primary microglial cells: the brains of newborn mice were removed under aseptic conditions, washed repeatedly with D-Hanks solution to remove blood stains; meninges and blood vessels were removed under a dissecting microscope, and rinsed with D-Hanks solution; repeated Pipette 3 times, 10min each time, filter through a 200-mesh sieve, and centrifuge; add complete culture medium, culture in a culture bottle coated with poly-lysine in advance, place in a 37°C incubator, replace the culture medium on the second day, remove Non-adherent cells; after that, replace the culture medium every 3 days, culture until the 9th to 10th day, observe under the microscope, microglial cells are round, small cells with strong refraction attached to astrocytes; Digest with 12mM ...

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Abstract

The invention provides application of a liver X receptor activator in anti-nerve inflammatory reaction. The liver X receptor activator is T0901317. The invention also relates to application of T0901317 in preparation of a medicament for treating senile dementia. The liver X receptor activator T0901317 can directly pass through a blood brain barrier, and has the characteristic of low side effect; and the effect of the anti-nerve inflammatory reaction of the liver X receptor activator is systematically analyzed, the liver X receptor activator is expected to be used as a specific medicament for clinically treating the intra-cephalic inflammatory reaction of the senile dementia, and experimental data are provided for clinical treatment of the senile dementia.

Description

technical field [0001] The present invention relates to the new application of the liver X receptor activator, in particular to the application of the liver X receptor activator in anti-neurinflammation reaction. Background technique [0002] With the aging of the world's population, senile dementia has become one of the most powerful killer diseases that seriously threaten the lives of the elderly in today's society. In developed countries, senile dementia has become the fourth human disease after heart disease, cancer and stroke. cause of death. Therefore, overcoming senile dementia and improving the quality of life of the elderly is one of the major topics in the field of biomedical research today. So far, there is no specific treatment method and drug for the inflammatory response in the brain of senile dementia. [0003] Alzheimer's disease is a common degenerative disease of the nervous system, and its pathological features are the deposition of senile plaques, neuro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/18A61P25/28
Inventor 崔卫刚邓晓慧任铭新宋海岩孙春莉
Owner XINXIANG MEDICAL UNIV
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