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Application of desloratadine and pharmacologically acceptable salt of desloratadine in preparing drug for treating alzheimer's disease

A technology for Alzheimer's disease and desloratadine, which is applied to the application field of desloratadine and its pharmaceutically acceptable salts in the preparation of medicines for treating Alzheimer's disease, and achieves good neuronal efficiency. Protective effect, high safety effect

Inactive Publication Date: 2018-03-20
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on its protective effect on neurons and / or increasing Aβ clearance and / or inhibiting Tau protein phosphorylation, thereby playing an anti-Alzheimer's disease (AD) role

Method used

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  • Application of desloratadine and pharmacologically acceptable salt of desloratadine in preparing drug for treating alzheimer's disease
  • Application of desloratadine and pharmacologically acceptable salt of desloratadine in preparing drug for treating alzheimer's disease
  • Application of desloratadine and pharmacologically acceptable salt of desloratadine in preparing drug for treating alzheimer's disease

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Effect test

Embodiment 1

[0016] Embodiment 1: Desloratadine (Desloratadine) protects SH-SY5Y cell experiment

[0017] The present invention detects the protective effect of desloratadine on cell damage caused by streptozotocin in SH-SY5Y cells, and the experiment shows that desloratadine has obvious protective effect on neurons.

[0018] 1. Experimental principle

[0019] This experiment is based on the fact that streptozocin (STZ) is widely used for in vivo and in vitro oxidative stress-mediated apoptosis, so SH-SY5Y cells were treated with STZ to simulate neurons in AD state in vitro. In the present invention, STZ and different concentrations of desloratadine were added to SH-SY5Y cell culture medium and incubated for a certain period of time, and then the changes in cell viability were measured by MTT assay to evaluate the protective effect of desloratadine on SH-SY5Y cells.

[0020] In this experiment, the neuroprotective effect of desloratadine was evaluated by MTT assay. The principle is that s...

Embodiment 2

[0026] Embodiment 2: Desloratadine (Desloratadine) increases the experiment of Aβ clearance

[0027] In the present invention, the experiments on the removal of exogenous Aβ by cells are carried out in SH-SY5Y cells to detect the effect of desloratadine on the removal of Aβ. The experiment shows that desloratadine has the effect of obviously increasing the removal of Aβ.

[0028] 1. Experimental principle

[0029] This experiment is based on the fact that SH-SY5Y cells can transfer exogenous Aβ into cells through endocytosis, etc., and then degrade exogenous Aβ through related pathways. The inventors of the present invention added exogenous Aβ and different concentrations of desloratadine into the SH-SY5Y cell culture medium to incubate for a certain period of time, then removed the cell culture medium, washed the cells and lysed them, and obtained and determined the cell culture medium. Aβ content within. The reduction of the final intracellular Aβ content indicates the abi...

Embodiment 3

[0037] Embodiment 3: Desloratadine (Desloratadine) inhibits the phosphorylation experiment of Tau protein

[0038] Neurofibrillary tangles caused by hyperphosphorylation of Tau protein are one of the important pathogenic factors in AD pathology. Therefore, the present invention further studies the regulating effect of the compound desloratadine on the phosphorylation level of Tau protein by Western blot experiment. The results showed that in SH-SY5Y cells, desloratadine could significantly reduce the phosphorylation levels of 396, 231 and 199 of tau protein.

[0039] 1. Experimental principle

[0040] Western blot experiment: Tau protein is widely expressed in the nervous system, and it is also expressed in SH-SY5Y cells. The level of its phosphorylation will directly affect the important role of tubulin in assembling into microtubules and maintaining the structure of microtubules. Therefore, the phosphorylated antibody at position 396 of Tau protein, the antibody at positio...

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Abstract

The invention discloses novel application of desloratadine and a pharmacologically acceptable salt of desloratadine in preparing a drug for treating alzheimer's disease and novel application in preparing a drug for treating and protecting nerve cells and / or increasing Abeta, clearing and / or inhibiting Tau protein phosphorylation related neurodegenerative diseases such as Parkinson's disease. According to a great number of experiments, the desloratadine and the pharmacologically acceptable salt of desloratadine have obvious effects of protecting nerve tool cells SH-SY5Y from STZ injuries, promoting removal of exogenous Abeta by SH-SY5Y cells, and also can obviously inhibit phosphorylation level of Tau proteins in the SH-SY5Y cells. Therefore, desloratadine and the pharmacologically acceptable salt of desloratadine can be used for treating the alzheimer's disease and nerve cell damages and / or Abeta and / or Tau protein related diseases, and is of significant meaning in developing novel clinical applicability of desloratadine.

Description

technical field [0001] The present invention relates to the new application of drug therapy, in particular to the application of desloratadine and its pharmaceutical composition in the preparation of medicines for treating Alzheimer's disease, more specifically, the present invention relates to desloratadine and its pharmaceutical composition. Its pharmaceutically acceptable salt or its pharmaceutical composition can protect neurons and / or increase Aβ clearance and / or inhibit Tau protein phosphorylation and is used in the preparation of drugs for the treatment of neurodegenerative diseases such as Alzheimer's disease . Background technique [0002] Alzheimer's disease (AD) is a progressive neurodegenerative disease characterized by extraneural amyloid deposition caused by Aβ aggregation, neurofibrillary tangles caused by hyperphosphorylation of tau protein, and neuronal cell apoptosis etc. as its main symbol. AD is highly age-dependent. As age increases, the incidence of A...

Claims

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Application Information

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IPC IPC(8): A61K31/4545A61P25/28A61P25/16
Inventor 沈旭王佳颖卢健许瑞
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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