Cycloviral buxicine d derivatives and their medicinal uses

A technology of cyclovirbuxin and its derivatives, which is applied in the field of medicine, and can solve problems such as the report of the application of cyclovirbuxine D derivatives that have not been found.

Active Publication Date: 2018-01-30
JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Before the completion of the present invention, there was no literature report on the anti-Alzheimer's disease effect of cycloviral buxicine D derivatives, nor was there any report on the application of cycloviral buxicine D derivatives in the preparation of anti-Alzheimer's disease drugs

Method used

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  • Cycloviral buxicine d derivatives and their medicinal uses
  • Cycloviral buxicine d derivatives and their medicinal uses
  • Cycloviral buxicine d derivatives and their medicinal uses

Examples

Experimental program
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Effect test

Embodiment 1

[0036] Example 1 Preparation method of Cycloviral Buxicine D

[0037] 5 kg of Euonymus microphylla medicinal material is crushed into coarse powder, extracted 3 times with 70% ethanol containing 1% glacial acetic acid, each time for 2 hours, combined extracts, added 0.2% active carbon of the liquid volume, stirred, filtered, and the filtrate decompressed to recover ethanol Obtain extractum, add water to dissolve, make every 1ml contain 1g medicinal material, adjust pH to 10 with sodium hydroxide, extract with chloroform to obtain total alkaloids; alkaloids are first separated by silica gel column (chloroform-methanol=5: 1) to obtain the crude product of Cyclovirin buxillus D. Take the crude product of cyclovir buxaxin D and dissolve it in methanol, pass it through an ODS atmospheric pressure chromatographic column, elute with acetonitrile-water (25:75) as the mobile phase, combine the components of cyclovir buxaxin D, and recrystallize to obtain cyclovir buxaxin D . white c...

Embodiment 2

[0038] Example 2 Preparation method of compound 1

[0039] Cyclovitamin D 0.42g dissolved in 25mL of CH 2 Cl 20.5 mL of benzoyl chloride was slowly added dropwise, then 0.5 mL of triethylamine was added, and stirred at room temperature. After the reaction was complete, the solvent was recovered under reduced pressure and dried to obtain a crude product. The crude product was separated and purified by silica gel column (petroleum ether: ethyl acetate = 5:2) to obtain compound 1 with a yield of 75.32%, white powder.

Embodiment 3

[0040] The preparation method of embodiment 3 compound 2-12

[0041] The preparation method is the same as in Example 2, and the yields are all greater than 60%, white powder.

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Abstract

The invention discloses a series of derivatives prepared from cyclovirobuxine D as a lead compound through corresponding chemical reaction. The cyclovirobuxine D is extracted and separated from Buxus micr ophylla Sieb.et Zucc.var.sinica Rehd.et Wils. and congener plants. Zymologic and cell experiments prove that the cyclovirobuxine D derivatives have a relatively strong inhibiting effect on acetylcholin esterase as well as an excellent protection effect on neuroblastoma celland so as to be capable of preventing and treating the Alzheimer's disease. Further researches present that certain cyclovirobuxine D derivatives have stronger activities than lead compounds.

Description

technical field [0001] The present invention relates to a preparation method of cyclovir buxicine D derivatives obtained from natural Chinese medicines, to be precise, a series of derivatives are prepared with chemical components extracted from Chinese medicines as lead compounds to resist Alzheimer's disease. Structural modification for the purpose of disease activity belongs to the field of medicine. Background technique [0002] Alzheimer's disease (AD) is a common degenerative disease of the central nervous system characterized by progressive memory loss, cognitive dysfunction, and personality changes in middle-aged and elderly people. Intensified, the global number of Alzheimer's patients has exceeded 35 million, which will bring many social and economic problems. Therefore, the prevention and treatment of AD has become a very urgent social and medical problem. At present, there are many kinds of drugs for the treatment of AD. The drugs that have been marketed or are ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J53/00A61K31/57A61K31/58A61P25/28
CPCC07J53/004
Inventor 南敏伦赫玉芳赵昱玮吕娜何忠梅马吉胜赵全成
Owner JILIN ACAD OF TRADITIONAL CHINESE MEDICINE
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