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Biphenyl polyphenol compound with acetyl choline and butyrylcholine esterase inhibiting effect and use of compound

Technology of a compound, pyrogallol, applied in the field of medicine

Inactive Publication Date: 2013-10-30
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report about the cholinesterase inhibitory activity of these two compounds

Method used

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  • Biphenyl polyphenol compound with acetyl choline and butyrylcholine esterase inhibiting effect and use of compound
  • Biphenyl polyphenol compound with acetyl choline and butyrylcholine esterase inhibiting effect and use of compound
  • Biphenyl polyphenol compound with acetyl choline and butyrylcholine esterase inhibiting effect and use of compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Embodiment 1: the preparation of formula I

[0034] 1. Take 100 kg of Magnolia officinalis medicinal material, crush it into a coarse powder, add 70% ethanol to extract, the amount of ethanol is 8 times of the weight of the medicinal material, each extraction time is 2 hours, and the number of extractions is 3 times.

[0035] 2. Filtrate the extract, combine the filtrates, and concentrate under reduced pressure at 60°C to form an extract.

[0036] 3. Add 10 times the amount of 5% sodium hydroxide solution to the extract, stir to dissolve, let it stand until the solution is clear, filter, then add hydrochloric acid to adjust the pH value to 2-3, stand overnight, filter, and get acid precipitate .

[0037] 3. The acid precipitate was washed with deionized water until neutral, dried and pulverized to obtain the precipitate.

[0038] 4. Take the precipitate, add dichloromethane to reflux and extract, the amount of solvent used is 5 times of the weight of the precipitate, ...

Embodiment 2

[0046] Embodiment 2: the preparation of formula II

[0047] 1. Take 100 kg of Magnolia officinalis medicinal material, crush it into a coarse powder, add 70% ethanol to extract, the amount of ethanol is 8 times of the weight of the medicinal material respectively, the extraction time is 2 hours each time, and the extraction times are 3 times.

[0048] 2. Filtrate the extract, combine the filtrates, and concentrate under reduced pressure at 60°C to form an extract.

[0049] 3. Add 10 times the amount of 5% sodium hydroxide solution to the extract, stir to dissolve, let it stand until the solution is clear, filter, then add hydrochloric acid to adjust the pH value to 2-3, stand overnight, filter, and get acid precipitate .

[0050] 3. The acid precipitate was washed with deionized water until neutral, dried and pulverized to obtain the precipitate.

[0051] 4. Take the precipitate, add dichloromethane to reflux and extract, the amount of solvent used is 5 times of the weight o...

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Abstract

The invention discloses a biphenyl polyphenol compound. Separating dry tree bark, root bark and wig bark from magnolia biloba (Magnolia officinalis Rehd. et Wils.var.biloba Rehd.et Wils ) of traditional Chinese medicine schisandra sphenanthera mangnolia officinalis (Magnolia officinalis Rehd. et Wils) to obtain 3'-allyl-2,4'-,5- biphenyl triphenol (formula I) and 3'-allyl-5-2-(2-hydroxyl butanone group)-2,4'-biphenol (formula II), wherein the compound of the formula I is a novel compound. The compounds of the formula I and the formula II have an obvious acetyl choline and butyrylcholine esterase inhibiting effect, and show unique advantages in treating senile dementia diseases, and the formula I and the formula II are shown in the specification.

Description

technical field [0001] The invention relates to two natural biphenyl polyphenol compounds, which not only have strong acetylcholinesterase inhibitory activity, but also have strong butyrylcholinesterase inhibitory activity, and can be used for the treatment of learning and memory disorders and senile dementia Treatment belongs to the technical field of medicine. technical background [0002] With the aging of the world and China's population, the incidence of Alzheimer's disease is increasing rapidly. According to statistics, the annual incidence rate of the elderly aged 65-69 is 1.5‰, 17.7‰ in the age of 70-79, and increases to 45.0‰ at the age of 85. Senile dementia is a disease that seriously affects the quality of life and health of the elderly after cardiovascular and cerebrovascular diseases, malignant tumors, and diabetes. This disease can cause memory impairment, memory loss, often forgetting the names of relatives and friends including children; being unable to di...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C39/21C07C49/835A61K31/05A61P25/00A61P25/28
Inventor 陈世忠王弘张宝宝
Owner PEKING UNIV