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Application of BMS470539 to preparation of medicine for treating Alzheimer's disease

A 1. BMS470539, Alzheimer's disease technology, applied in the direction of drug combination, pharmaceutical formula, plant raw materials, etc., can solve the problem of lack of BMS470539 research, and achieve the effect of increasing the level of rigidity, delaying the development of the disease, and increasing memory ability. Effect

Inactive Publication Date: 2021-09-03
DALI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the problem of the lack of BMS470539 in the research of Alzheimer's disease medicine in the prior art, and the proposed application of BMS470539 in the preparation of Alzheimer's disease medicine

Method used

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  • Application of BMS470539 to preparation of medicine for treating Alzheimer's disease
  • Application of BMS470539 to preparation of medicine for treating Alzheimer's disease
  • Application of BMS470539 to preparation of medicine for treating Alzheimer's disease

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Drugs containing BMS470539, Hovenia japonica extract, Jujube seed extract, lemon extract, industrial hemp flower and ginkgolide can be used in human melanoma cells, BMS470539 is a potent and selective melanocortin-1 (MC1) receptor agonist, the IC50 value of BMS470539 is 120nm;

[0020] BMS470539 inhibited TNF-induced activation of NF-κB transcription factor in a dose-dependent manner when the drug was administered to MC-1R human melanoma cells;

Embodiment 2

[0022] Drugs containing BMS470539, Hovenia citrus extract, Jujube seed extract, lemon extract, industrial hemp flower and ginkgolide can be used in the microcirculation of cremaster muscle caused by platelet activating factor inflammation, and BMS470539 is an effective and selective Sexual melanocortin-1 (MC1) receptor agonist, the IC50 value of BMS470539 is 120nm;

[0023] BMS470539 inhibits cell migration, but does not affect cell adhesion when the drug is used in the microcirculation of cremaster muscle caused by platelet activating factor inflammation;

Embodiment 3

[0025] Drugs containing BMS470539, Hovenia japonica extract, Jujube seed extract, lemon extract, industrial hemp flower and ginkgolide can be used in the mouse model of LPS (lipopolysaccharide)-induced cytokine accumulation, and BMS470539 is an effective And a selective melanocortin-1 (MC1) receptor agonist, the IC50 value of BMS470539 is 120nm;

[0026] When the drug was used in a mouse model of LPS (lipopolysaccharide)-induced cytokine accumulation, when the dose of BMS470539 was 11 μmol / kg, TNF-α decreased by 65% ​​in a dose-dependent manner; when the dose of BMS470539 was 33 μmol / kg, TNF-α decreased by 82% in a dose-dependent manner;

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Abstract

The invention discloses an application of BMS470539 to preparation of a medicine for treating Alzheimer's disease. The medicine internally contains BMS470539, a raisin tree seed extract, a spina date seed extract, a lemon extract, industrial hemp flowers and bilobalide, and the BMS470539 is an effective and selective melanocortin-1 (MC1) receptor agonist. Research finds that the compound has a certain effect in human melanoma cells, a mouse model in which LPS (lipopolysaccharide) induces cell factor accumulation, a mouse pneumonia model, a delayed hypersensitivity reaction model and other disease models in experiments. Laboratory research finds that the BMS470539 can significantly improve pathological symptoms and improve the memory level in an Alzheimer's disease animal model, the application effect of the BMS470539 in Alzheimer's diseases is obtained through a large number of experiments, particularly, the BMS470539 can significantly improve the memory ability of Alzheimer's disease mice in conditional fear experiments, the stiffness level is significantly increased, and the application potential in treatment of the Alzheimer's disease is shown.

Description

technical field [0001] The invention relates to the technical field of Alzheimer's disease medicines, in particular to the application of BMS470539 in the preparation of medicines for treating Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD) is a neurodegenerative disease with insidious onset and progressive development. Clinically, it is characterized by comprehensive dementia such as memory impairment, aphasia, apraxia, agnosia, impairment of visuospatial skills, executive dysfunction, and personality and behavior changes. The etiology is still unknown. Those with onset before the age of 65 are called Alzheimer's disease; those with onset after the age of 65 are called senile dementia; [0003] The onset of the disease is slow or insidious, and patients and family members often cannot tell when the onset occurs. It is more common in the elderly over 70 years old (average 73 years old for men, 75 years old for women). A small number of patients ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/454A61K36/752A61P25/28A61K31/365
CPCA61K31/454A61K31/365A61K36/72A61K36/725A61K36/752A61K36/60A61P25/28A61K2300/00
Inventor 龚志婷王晓兵姜乐
Owner DALI UNIV
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