Preparation method of chimonanthus inhibited acetylcholinesterase active part and application thereof

A technology of acetylcholinesterase and active parts, which is applied in the field of preparation of acetylcholinesterase inhibitory active parts, and achieves the effects of reasonable preparation process, easy industrialization and abundant sources

Inactive Publication Date: 2011-04-06
朱笃
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on the medicinal effect of Chimerus genus mainly focuses on antibacterial, antiviral, and influenza prevention. There are no reports on the literature and patents about its extract components inhibiting the activity of acetylcholinesterase. The report of the active site that inhibits acetylcholinesterase is isolated, and it also provides a new development idea for the development of new senile dementia drugs, especially acetylcholinesterase inhibitors, from traditional Chinese medicine resources

Method used

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  • Preparation method of chimonanthus inhibited acetylcholinesterase active part and application thereof
  • Preparation method of chimonanthus inhibited acetylcholinesterase active part and application thereof
  • Preparation method of chimonanthus inhibited acetylcholinesterase active part and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 1. Preparation of alkaloids from active parts of Chimerus genus

[0021] A. take waxy plum leaf as raw material, dry, pulverize, extract 3 times with the ethanol solution of volume percent concentration 60%, the quality of each used ethanol solution is successively 10 times, 8 times and 8 times of the waxy plum leaf raw material quality 8 times, extracting for 10 hours each time, filtering the three extracts with gauze and merging;

[0022] b. Concentrate the above-mentioned combined extract solution at a temperature of 45°C to recover ethanol until it has no alcohol smell, and obtain an ethanol extract, which is dried at 40°C to form an extract for later use;

[0023] c. take by weighing 250 grams of wax plum extract, disperse it with 10% acetic acid aqueous solution, extract with ethyl acetate, each 500mL, extract 10 times, collect acid aqueous phase and ethyl acetate phase and insoluble precipitation.

[0024] d. Alkalinize the above-mentioned acidic aqueous phase w...

Embodiment 2

[0038] 1. Preparation of flavonoids from active parts of Chimerus genus

[0039] The processing of the leaf material of Chimerus genus and the obtaining of the extract are the same as the preparation steps a, b, and c of the active site alkaloids in Example 1, and the subsequent preparation steps are as follows;

[0040] d. Extract the above-mentioned ethyl acetate phase with 10% aqueous sodium carbonate solution, 500 mL each time, extract 8 times, and collect the alkaline aqueous layer;

[0041] e. acidifying the collected alkaline water layer with hydrochloric acid to a solution pH of 6.0, after acidification, a large amount of precipitates are separated out, and the precipitates are centrifuged and collected;

[0042] f. Take the precipitate and dissolve it with ethanol, develop it by TLC (petroleum ether: ethyl acetate = 7: 3), spray aluminum trichloride solution, yellow fluorescence will appear under long-wave ultraviolet light, and the precipitate is preliminarily determ...

Embodiment 3

[0051] 1. The preparation steps of the active part coumarins of Chimerus genus

[0052] The processing of the leaf material of Chimerus genus and the obtaining of the extract are the same as the preparation steps a, b, c, and d of the active site alkaloids in Example 1, and the subsequent preparation steps are as follows;

[0053] e. Acidify the collected alkaline water layer with hydrochloric acid until the pH of the solution is 6.0. After the acidification, a large amount of precipitates precipitate out. The supernatant is collected by centrifugation. The supernatant is extracted with ethyl acetate, 500 mL each time, extracted 6 times, and the ethyl acetate is collected. Mutually;

[0054] f. After developing the ethyl acetate phase by TLC (petroleum ether: ethyl acetate = 6: 4), spray 5% potassium hydroxide ethanol solution, and the phenomenon of blue fluorescence enhancement appears under ultraviolet light, and it is determined that the ethyl acetate phase is fragrant. le...

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Abstract

The invention relates to the field of traditional Chinese medicine preparation and relates to a preparation method of a chimonanthus inhibited acetylcholinesterase active part and application thereof. The preparation method comprises the following steps of: ethanol lixiviation, low-polarity solvent extraction, acid-solution and alkali-isolation chloroform extraction or alkali-solution and acid-isolation, centrifugation and ethyl acetate extraction. The extracted active part includes three categories of substances, namely alkaloids, flavonoids and coumarins respectively. The active part has relatively strong inhabitation effect on the activity of acetylcholinesterase and has a wide application range in preparing medicaments for preventing and treating related symptoms or diseases caused by acetylcholine deletion, particularly the medicaments for preventing and treating senile dementia.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the separation and extraction of active parts from Chimerus genus plants, in particular to a preparation method for acetylcholinesterase inhibitory active parts. The obtained active parts have a strong inhibitory effect on acetylcholinesterase activity. It is expected to be used as a drug for preventing and treating senile dementia. Background technique [0002] Chimonanthus praecox (L.) Link is a Calycanthaceae plant of the Chimonanthus family. It is distributed in central, southern, eastern and Yunnan-Guizhou Plateau regions of China. Its flowers and leaves have aromatic oils that emit aroma, and have extremely high medicinal and edible values. . The current research on Chimerus plants focuses on the volatile oil components of leaves, including eucalyptol, linalool, α-pinene, β-pinene, camphene, camphor and borneol; while the non-volatile oil components In r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K36/185A61P25/28A61K125/00A61K127/00A61K131/00A61K133/00A61K135/00
Inventor 朱笃王凌云张志斌刘易鑫颜日明邹峥嵘
Owner 朱笃
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