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Palmatine derivatives and application thereof to preparation of anti-alzheimer-disease medicament

A technology for Alzheimer's disease and derivatives, which is applied in the field of preparation of palmatine derivatives, can solve the problem that there are no literature reports on the anti-Alzheimer's effect of palmetine derivatives, and no discovery of palmetine derivatives Application reports and other issues

Inactive Publication Date: 2016-04-20
JILIN AGRICULTURAL UNIV
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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 were no reports in the literature that palmatine derivatives had an anti-Alzheimer's disease effect, and no report on the application of palmetine derivatives in the preparation of anti-Alzheimer's disease drugs was found.

Method used

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  • Palmatine derivatives and application thereof to preparation of anti-alzheimer-disease medicament
  • Palmatine derivatives and application thereof to preparation of anti-alzheimer-disease medicament
  • Palmatine derivatives and application thereof to preparation of anti-alzheimer-disease medicament

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 palatine (compound 1) preparation method

[0043] 5kg of the medicinal material of Huangteng is crushed into a coarse powder, extracted 3 times with 70% ethanol containing 2% glacial acetic acid, 2 hours each time, combined the 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, centrifuge, take supernatant, pass through D101 macroporous resin, first use 10% ethanol to elute 5 times resin volume, then use 60% ethanol to elute 5 times resin volume , collect the ethanol eluent, recover the solvent, and dry under reduced pressure to obtain the crude product of palmetine. The crude product of palmetine was dissolved in methanol, passed through an ODS atmospheric pressure chromatographic column, eluted with acetonitrile-0.4% phosphoric acid solution (32:68) as the mobile phase, and the palmetine componen...

Embodiment 2

[0044] Embodiment 2 compound 2 preparation method

[0045] 2.00g of palmatine, pyrolyzed at 160-180°C for 20min under vacuum condition, cooled to room temperature, separated and purified with silica gel column (chloroform:methanol:ammonia water=8:1:0.1) to obtain 1.45g of crystals, yield 72.5 %. Dark red powder, molecular formula C 20 h 20 NO 4 , molecular weight 338.5.

Embodiment 3

[0046] Embodiment 3 compound 3 preparation method

[0047] Compound 20.33g was dissolved in 25mL of CH 2 Cl 2 0.5 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 first eluted with diethyl ether, and then separated and purified by silica gel column (chloroform:methanol=8:1) to obtain compound 3 with a yield of 85.37%, yellow powder, molecular formula C 27 h 24 NO 5 , molecular weight 442.7.

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Abstract

The invention discloses a series of derivatives prepared by extracting from Fibraurea recisa Pierre. and carrying out separation and purification to obtain palmatine, using the palmatine as a lead compound, and performing corresponding chemical reactions. Enzymology and cell tests prove that the palmatine derivatives have good effects of inhibiting acetylcholin esterase and protecting neuroblastoma cells so as to achieve an effect of protecting and treating the alzheimer disease. Further research shows that the palmatine derivatives have higher activity than the lead compound.

Description

technical field [0001] The present invention relates to a preparation method of palmatine derivatives obtained from natural Chinese medicines, to be precise, a series of derivatives are prepared with the chemical components extracted from Chinese medicines as lead compounds, so as to have anti-Alzheimer's disease activity Structural modification for the purpose 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. The aggravation of the global Alzheimer's disease 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 entering clin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03A61P25/28
CPCC07D455/03
Inventor 何忠梅祝洪艳宗颖杨鹤刘双利吕娜张连学南敏伦
Owner JILIN AGRICULTURAL UNIV
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