Application of ethyl asterrate in preparation of anti-alzheimer medicine

A technology for senile dementia and drugs, applied in the field of medicine, can solve problems such as no reports of compounds

Inactive Publication Date: 2014-05-07
YICHUN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Compound ethyl asterrate in the present invention is the derivant of kodiic acid, has remarkable antibacterial activity (LI Y, SUN BD, CHE YS, et al.Bioactive Asterric acid derivatives from the Antarctic ascomycete fungus Geomyces sp. [J]. J Nat Prod, 2008, 71( 9): 1643~1646. ), but there is no report on the inhibitory activity of this type of compound on acetylcholinesterase

Method used

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  • Application of ethyl asterrate in preparation of anti-alzheimer medicine
  • Application of ethyl asterrate in preparation of anti-alzheimer medicine
  • Application of ethyl asterrate in preparation of anti-alzheimer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Example 1: Acetylcholinesterase inhibitory activity of the compound ethyl asterrate

[0012] (1) Drugs and reagents

[0013] Acetylcholinesterase (AChE, Sigma Company), 50 mmol / L, pH8.0 phosphate-buffered saline (PBS), 15 mmol / L 5,5-dithio-2-nitrobenzoic acid (dithiobis-nitrobenzoic acid , DTNB) solution (Sigma company) (prepared with 50mmol / L, pH 8.0 PBS), 15 mmol / L thioacetylcholine (Acetyl thiocholine, ATch, Sigma company, prepared with 50mmol / L, pH 8.0 PBS), 4% ten Sodium Dialkyl Sulfate (SDS, Sigma Company), positive control Huperzine A (National Institute for the Control of Pharmaceutical and Biological Products), 0.75mol / L MgCl 2 solution, methanol.

[0014] (2) Experimental method

[0015] Refer to the literature (Zhang Yi, Feng Yan, Li Xiaoming, et al. Research on the inhibition of acetylcholinesterase activity by seaweed components [J]. Ocean and Limnology, 2005, 36(5): 459-464.) and make appropriate improvements. The reference substance for the detectio...

Embodiment 2

[0023] (1) Experimental animals and test drugs

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Abstract

The invention discloses application of ethyl asterrate in preparation of an anti-alzheimer medicine, and in particular relates to application of diphenyl ether compound ethyl asterrate shown in the structural formula (I) in inhibition of the activity of acetylcholine esterase and preparation of an anti-alzheimer medicine. Experiments prove that the ethyl asterrate can remarkably inhibit the activity of acetylcholine esterase, can remarkably improve the memory and space exploration capability of an alzheimer rat model caused by D-galactose and AlCl3, can be applied to preparation of the anti-alzheimer medicine, and indicates an excellent market application prospect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a diphenyl ether compound, and its acetylcholinesterase inhibitory activity is studied. The compound can be applied to the preparation of anti-senile dementia drugs. Background technique [0002] Alzheimer's disease (AD) is a progressive neurodegenerative disease, which is mainly manifested as memory function attenuation and recognition impairment, accompanied by various neurological symptoms and behavioral disorders, and has a very high incidence rate. Currently, the market approves the treatment of AD Most of the drugs used are drugs that inhibit the activity of acetylcholinesterase, mainly including tacrine, donepezil, carbamates (such as rivastigmine, revosidamine), huperzine A, galantamine (galantamine) etc. With the arrival of the aging of the global population, the number of its incidence will continue to increase, and the demand for anti-senile dementia drugs will hav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/60A61P25/28
Inventor 颜日明朱笃汪涯张志斌汪娣
Owner YICHUN UNIVERSITY
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