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Application of 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester

A technology of methyl hydroxybenzoate and hydroxybenzoyl, which is applied in the direction of medical preparations containing active ingredients, sugar derivatives, sugar derivatives, etc., can solve the problems of high cost of care, and achieve good anti-Alzheimer's effect , Improve the effect of learning and memory index

Active Publication Date: 2013-08-21
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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  • Application of 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1: Preparation of 2-[(2-O-glucosyl-5-hydroxybenzoyl)amino]-5-hydroxybenzoic acid methyl ester

[0027] Take 8.5Kg of dried rhizomes of Niubian, and reflux extraction with 8 times the amount of 60% ethanol (v / v, ethanol / water) for 2 hours, twice in a row. The extracts were combined, ethanol was removed in vacuo, the residue was dispersed in water, and extracted three times with ethyl acetate and n-butanol successively. The amount of ethyl acetate used is to use 3.5mL ethyl acetate per 1g of burdock root; the amount of n-butanol used is to use 3.5mL of n-butanol per 1g of burdock root.

[0028] 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 elution volume of each gradient is 82mL eluent per 1g dry sample of n-butanol extract. Take CHCl 3 -MeOH-H 2 O (volume ratio 80:20:0) fraction, further ODS column c...

Embodiment 2

[0030] Example 2: Biological test of methyl 2-[(2-O-glucosyl-5-hydroxybenzoyl)amino]-5-hydroxybenzoate

[0031](1) Preparation of transgenic Drosophila disease model

[0032] According to the method of Koichi Iijima and Hsin-Ping Liu et al. (Dissecting the pathological effects of human Aβ40 and Aβ42 in Drosophila: A potential model for Alzheimer's disease. PNAS, 2004, 101(17):6623-6628), the elav promoter gene 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.

[0033] (2) Biological activity evaluation method

[0034] The experiments of biological determination consisted of three groups ...

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Abstract

The invention discloses an application of 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester, belonging to the research field of drugs for preventing and treating senile dementia. The invention also discloses a method for extracting the 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester from aconitum ochranthum roots. The 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester is applied to the preparation of drugs for preventing and treating senile dementia. The drugs contain at least one of 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester as well as a medicinal salt and solvate of 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester. The 2-[(2-O-glucosyl-5-hydroxybenzoyl) amino]-5-hydroxybenzoic acid methyl ester can be used for improving the learning memory indexes of transgenic flies under low concentration condition, has a better senile dementia preventing effect 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, and in particular relates to the use of methyl 2-[(2-O-glucosyl-5-hydroxybenzoyl)amino]-5-hydroxybenzoate. Background technique [0002] Alzheimer's Disease (AD) is the most common form of Alzheimer's disease, and it is a fatal neurodegenerative disease with progressive development 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 produ...

Claims

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Application Information

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IPC IPC(8): A61K31/7034A61P25/28C07H15/203C07H1/08
Inventor 姚新生钟毅高昊刘振宇穆祯强杜书文肖高铿
Owner JINAN UNIVERSITY