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Compound for preventing and treating Alzheimer disease as well as preparation method and application thereof

A technology for Alzheimer's disease and a compound, which is applied in the field of drug research for the prevention and treatment of Alzheimer's disease, can solve problems such as high cost of care, and achieve the effect of good resistance to Alzheimer's disease and improvement of learning and memory index.

Active Publication Date: 2015-05-20
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

People with AD suffer from cognitive deficits and memory loss, as well as behavioral problems such as anxiety, and often require comprehensive care from assisted living agencies or family members, which can be very costly

Method used

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  • Compound for preventing and treating Alzheimer disease as well as preparation method and application thereof
  • Compound for preventing and treating Alzheimer disease as well as preparation method and application thereof
  • Compound for preventing and treating Alzheimer disease as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Extraction of 2-[(2,5-dihydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester

[0027] Take 8Kg of air-dried beef flat (A. barbatum var. puberulum) roots, and extract with 4 L of 60% ethanol (v / v, ethanol / water) under reflux for 2 hours, twice in a row. The extracts were combined, ethanol was removed in vacuo, the residue was dispersed in water, and then extracted three times with ethyl acetate and n-butanol successively (10 L of ethyl acetate and n-butanol were used for each extraction). The n-butanol extract was subjected to silica gel column chromatography with CHCl 3 -MeOH-H 2 O (volume ratios are 100:0:0, 98:2:0, 95:5:0, 90:10:0, 80:20:0, 60:40:8, 0:100:0) for gradient For elution, the volume of each gradient elution solution is 82mL of eluent per 1g of dry sample of n-butanol extract. Take CHCl 3 -MeOH-H 2 O (volume ratio 98:2:0) fraction, further cross ODS column chromatography, use MeOH-H 2 O (volume ratio 10:90, 30:70, 50:50, 70:30, 90:10, ...

Embodiment 2

[0029] Example 2: Biological test of methyl 2-[(2,5-dihydroxybenzoyl)amino]-5-hydroxybenzoate

[0030] (1) Preparation of transgenic Drosophila disease model

[0031] According to the method of Koichi Iijima and Hsin-Ping Liu et al. (Dissecting the pathological effects of human Aβ40 and Aβ42in Drosophila: A potential model for Alzheimer's disease. PNAS, 2004, 101(17): 6623-6628), will carry the elav promoter gene The parent fruit fly of the parent fruit fly is crossed with the parent fruit fly carrying the Aβ42 protein gene, and the offspring disease fruit fly integrated with the elav promoter gene and the Aβ42 protein factor is obtained. This Drosophila model can be used to evaluate the effect of drug treatment and prevention of neurodegenerative diseases, especially the effect of treatment and prevention of Alzheimer's disease, such as the therapeutic effect of AD drugs.

[0032] (2) Biological activity evaluation method

[0033] The experiment of biological determination se...

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Abstract

The invention belongs to the field of research of medicines for preventing and treating Alzheimer disease and discloses a compound for preventing and treating Alzheimer disease as well as a preparation method and application thereof. The compound is 2-[(2,5-dyhydroxybenzoyl)amido]-5-hydroxymethyl benzoate. The preparation method comprises the step of extracting and separating the compound from aconitum ochranthum root to obtain the compound. The 2-[(2,5-dyhydroxybenzoyl)amido]-5-hydroxymethyl benzoate is applied to preparation of the medicine for preventing and treating Alzheimer disease. The result proves that the 2-[(2,5-dyhydroxybenzoyl)amido]-5-hydroxymethyl benzoate can improve the learning and memory index of transgenic drosophila under low concentration, and the compound has good effect of resisting the Alzheimer disease and is particularly suitable for the Alzheimer disease.

Description

technical field [0001] The invention belongs to the research field of drugs for preventing and treating senile dementia, in particular to a compound for preventing and treating senile dementia, its preparation method and application. Background technique [0002] Alzheimer's disease (AD) is the most common form of senile dementia. It is a progressive and fatal neurodegenerative disease associated with aging. Deterioration, progressive decline in the ability of daily living, and various neuropsychiatric symptoms and behavioral disturbances. AD patients suffer from cognitive deficits and memory decline, as well as behavioral problems such as anxiety, and often require comprehensive care from assisted living agencies or family members, which can be very costly. AD is an increasingly serious medical problem as the elderly population and its proportion of the total population increase. [0003] The pathology of AD is characterized by neurofibrillary tangles produced by hyperpho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C235/64C07C231/24A61K31/609A61P25/28
Inventor 姚新生钟毅高昊刘振宇穆祯强杜书文肖高铿
Owner JINAN UNIVERSITY