Application of dapsone to preparation of alpha-secretase enhancer

A technology of dapsone and secretase, applied in the directions of organic active ingredients, medical preparations containing active ingredients, nervous system diseases, etc., can solve the problem that dapsone has no regulatory effect, and achieve the effect of improving the level

Inactive Publication Date: 2014-08-13
崔德华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported that dapsone has no regulatory effect on β-secretase and γ-secretase

Method used

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  • Application of dapsone to preparation of alpha-secretase enhancer
  • Application of dapsone to preparation of alpha-secretase enhancer
  • Application of dapsone to preparation of alpha-secretase enhancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1N2

[0018] The cultivation of embodiment 1N2a-APP cell

[0019] N2a-APP cells are mouse neuroblastoma cells stably expressing APPsw and PS1, cultured in DMEM high-glucose medium, containing 10% fetal bovine serum, and placed in 95% humidity and 5% CO 2 in a 37°C incubator.

Embodiment 2

[0020] Example 2 Effects of different concentrations of dapsone on the level of sAPPα in N2a-APP cells

[0021] Dapsone was dissolved in dimethyl sulfoxide (DMSO, Sigma), the stock solution concentration was 100mmol / L, and it was directly diluted in the medium when used, and the final concentration of DMSO was not more than 0.3%, and the serially diluted dapsone ( 0, 20, 50, 100, 200 μM) were co-cultured with N2a-APP cells for 12 hours, the medium was collected respectively, and the cell protein was extracted for Western blot analysis.

[0022] Experimental results: The effect of dapsone on sAPPα is concentration-dependent. Within 0-100μM, as the concentration of dapsone increased, the level of sAPPα gradually increased, while at 200μM, it decreased, but still significantly increased compared with the blank group. Compared with the blank group *pfigure 1 As shown in A.

Embodiment 3

[0023] Example 3 Effects of different treatment times of dapsone on sAPPα of N2a-APP cells.

[0024] Dapsone was dissolved in dimethyl sulfoxide (DMSO, Sigma), and the stock solution concentration was 100mmol / L. When used, it was directly diluted in the culture medium. The final concentration of DMSO was not more than 0.3%. -APP cells were co-cultured for 0, 6, 12 and 24 hours, the medium was collected respectively, and the cell protein was extracted for Western blot analysis.

[0025] Experimental results: With the prolongation of the incubation time of dapsone and cells, the level of sAPPα gradually increased in a time-dependent manner. Compared with the blank group, *pfigure 1 Shown in B.

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Abstract

The invention relates to an application of dapsone (Chemical name: 4,4'-diamino diphenyl sulfone) to preparation of an alpha-secretase enhancer. By adopting dapsone, the level of alpha-secretase ADAM10 (A-Disintegrin And Metalloprotease 10) of N2a-APP cells is raised, so that the level of soluble APPalpha (sAPPalpha) is raised. By using the compound provided by the invention, the density of intracerebral synapse of a mouse can be increased, and the cognizing function is improved. Moreover, the compound provided by the invention can be combined with pharmaceutically-acceptable medicinal auxiliary materials or carriers, and can be applied orally or through rectum. The structural formula is shown in the specifications.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to the new application of dapsone in improving the activity of α-secretase. Background technique [0002] Amyloid Precursor Protein (APP) is a type I transmembrane protein with a single transmembrane domain, which is highly expressed in neurons and can be hydrolyzed by α-secretase, B-secretase and γ-secretase. APP is hydrolyzed by β-secretase and γ-secretase to produce toxic Aβ, and hydrolyzed by α-secretase to produce soluble APPα (sAPPα) with synaptic protective effect. [0003] APP is hydrolyzed into soluble APPα under the action of α-secretase ADAM10. sAPPα can promote neurogenesis and synapse growth, and can also regulate the differentiation of neural stem cells, which is beneficial to the nervous system. Based on in vivo experiments, it is also found that sAPPα can improve the cognitive and learning functions of animal models. [0004] Dapsone is currently used to treat ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/145A61P25/00A61P25/28
Inventor 崔德华童亚伟张韬王贺成付瑶蕴
Owner 崔德华
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