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Caffeoylquinic acid derivative and application of caffeoylquinic acid derivative as medicine for repairing and protecting neurons

A technology of caffeoylquinic acid and derivatives, applied in the field of biopharmaceuticals, can solve problems such as unreported, and achieve the effect of significant neuron repair and protection activity

Active Publication Date: 2017-02-22
GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the effect of caffeoylquinic acid derivatives in burdock root on neurons.

Method used

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  • Caffeoylquinic acid derivative and application of caffeoylquinic acid derivative as medicine for repairing and protecting neurons
  • Caffeoylquinic acid derivative and application of caffeoylquinic acid derivative as medicine for repairing and protecting neurons
  • Caffeoylquinic acid derivative and application of caffeoylquinic acid derivative as medicine for repairing and protecting neurons

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1: Preparation of caffeoylquinic acid derivatives A and B.

[0031] 10.0 kg of burdock root medicinal material, soaked in 8-20 times the mass percentage of 55% ethanol aqueous solution overnight, heated and refluxed for 3 times, the first time for 2 hours, and the last two times for 1 hour. The extracts were combined, and the solvent was recovered under reduced pressure to obtain a concentrated extract. The extract was dispersed in appropriate amount of water, and extracted with petroleum ether, dichloromethane, ethyl acetate and n-butanol successively. The solvent was recovered under reduced pressure to obtain petroleum ether extract (15.6 g), dichloromethane extract (43.1 g), ethyl acetate extract (256.8 g) and n-butanol extract (843.2 g). After testing, the ethyl acetate layer had the best activity. The ethyl acetate extract (256.8 g) was passed through a silica gel column, and eluted with dichloromethane-methanol (100:1-1:100) to obtain 15 fractions. Frac...

Embodiment 2

[0034] Example 2: Study on the repair and protection activity of caffeoylquinic acid derivatives on nerve cells in vitro.

[0035] The present invention adopts MTT and LDH activity test methods to measure the protective effect of caffeoylquinic acid derivatives on SH-SY5Y cell damage mediated by hydrogen peroxide, and the results show that caffeoylquinic acid derivatives have a significant effect of repairing nerve cells , so it can be used in the research and development of drugs for the treatment of neurodegenerative diseases, stroke and traumatic brain injury.

[0036] (1) Instruments and reagents: DMEM medium was purchased from Hyclone Company, and fetal bovine serum was Hyclone product; CKX31 inverted microscope (Olympus, Japan); constant temperature CO2 incubator (Thermo, USA); 5810R desktop high-speed and low-temperature Centrifuge (Eppendorf, Germany); Fully automatic microplate reader (Biotek Group, USA); Hydrogen peroxide (Sinopharm Chemical Reagent Co., Ltd.); LDH k...

Embodiment 3

[0045] Embodiment 3: the preparation of pharmaceutical composition

[0046] Compound A 6.5g

[0047] Dextrin 80g

[0048] According to a conventional method, after the above-mentioned substances are mixed uniformly, 1000 equal parts are respectively packed into ordinary gelatin capsules to obtain 1000 capsules.

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PUM

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Abstract

The invention discloses a caffeoylquinic acid derivative, a medicine composition containing the derivative, action of series derivatives as a medicine for repairing and protecting neurons and application of the caffeoylquinic acid derivative for preparing the medicine for treating neurodegenerative diseases, traumatic brain injury and stroke. A dicaffeoylguinic acid derivative has remarkable neurons repairing and protection activity, can be developed for treating diseases including the neurodegenerative diseases, the traumatic brain injury and stroke diseases and supplies potential opportunity for treating similar diseases.

Description

[0001] Technical field: [0002] The invention belongs to the field of biopharmaceuticals, in particular to a caffeoylquinic acid derivative, which has the effect of repairing and protecting neurons. [0003] Background technique: [0004] Neurodegenerative disease is a disease state in which cells and neurons of the brain and spinal cord are lost. The brain and spinal cord are made up of neurons that have different functions, such as controlling movement, processing sensory information, and making decisions. Cells in the brain and spinal cord generally do not regenerate, so excessive damage can be devastating and irreversible. Neurodegenerative diseases are caused by the loss of neurons or their myelin sheath, which worsens over time, leading to dysfunction. Initial treatment depends on the diagnosis of the specific disease. Currently, only a few drugs are available for some neurodegenerative diseases. Therefore, it is urgent to find safe and effective therapeutic drugs. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/732C07C67/48A61K31/216A61P25/28
CPCA61K31/216C07C67/48C07C69/732
Inventor 赵庆春蒋晓文田星白俊鹏
Owner GENERAL HOSPITAL OF THE NORTHERN WAR ZONE OF THE CHINESE PEOPLES LIBERATION ARMY