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Preparation method of chimonanthus inhibited acetylcholinesterase active part and application thereof

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

Inactive Publication Date: 2012-09-26
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
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Effect test

Embodiment 1

[0020] 1. Preparation of alkaloids from active parts of Chimonanthus

[0021] a. Weigh the Chimonanthus leaves as the raw material, dry, pulverize, and extract 3 times with a 60% volume percent ethanol solution. The quality of the ethanol solution used for each time is 10 times, 8 times and the quality of the raw material of the Chimonanthus leaves. 8 times, 10 hours each time, filter the three extracts with gauze and combine;

[0022] b. The above-mentioned combined extracts are concentrated under reduced pressure at a temperature of 45°C to recover the ethanol until there is no alcohol taste to obtain an ethanol extract, which is dried at 40°C to form an extract for later use;

[0023] c. Weigh 250 g of Chimonanthus praecox extract, disperse it with 10% acetic acid aqueous solution, and extract with ethyl acetate, 500 mL each time, extract 10 times, collect acid water phase, ethyl acetate phase and insoluble precipitate.

[0024] d. The above acid aqueous phase is alkalized with sod...

Embodiment 2

[0038] 1. Preparation of flavonoids from active parts of Chimonanthus

[0039] The processing of the leaves of Chimonanthus plant and the extraction of the extract are the same as the preparation steps a, b, and c of the active site alkaloids in Example 1. The subsequent preparation steps are as follows;

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

[0041] e. Acidify the collected alkaline water layer with hydrochloric acid to a solution pH of 6.0. After acidification, a large amount of precipitate will precipitate, centrifuge and collect the precipitate;

[0042] f. Take the precipitate and dissolve it in ethanol, develop it by TLC (petroleum ether: ethyl acetate = 7: 3), spray aluminum trichloride solution, it will show yellow fluorescence under ultraviolet long wave, and it is preliminarily determined that the precipitate is a flavonoid.

[0043] 2. Determination of ...

Embodiment 3

[0051] 1. Preparation steps of coumarins from the active part of Chimonanthus

[0052] The processing of the leaves of Chimonanthus plant and the extraction of the extract are the same as the preparation steps a, b, c, d of the active site alkaloids in Example 1. The subsequent preparation steps are as follows;

[0053] e. Acidify the collected alkaline aqueous layer with hydrochloric acid to a solution pH of 6.0. After acidification, a large amount of precipitation will precipitate. Centrifuge to collect the supernatant. The supernatant is extracted with ethyl acetate, 500 mL each time, 6 times, and ethyl acetate is collected phase;

[0054] f. After the ethyl acetate phase is developed by TLC (petroleum ether: ethyl acetate=6:4), spray 5% potassium hydroxide ethanol solution, the blue fluorescence enhancement phenomenon appears under ultraviolet, confirm the ethyl acetate phase is fragrant Legumes;

[0055] 2. Determination of acetylcholinesterase inhibitory activity of coumarins i...

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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 byacetylcholine 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 Chimonanthus plants, and 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 medicine for preventing and treating senile dementia. Background technique [0002] Chimonanthus praecox (L.) Link is a Calycanthaceae plant of the Chimonanthus family, which is distributed in Central China, South China, East China and the Yunnan-Guizhou Plateau. Its flowers and leaves have aromatic oils that emit fragrance, which has extremely high medicinal and edible value . The current research on Chimonanthus plants focuses on the volatile oil components of leaves, including cineole, linalool, α-pinene, β-pinene, camphene, camphor, and camphor and other main components; while for...

Claims

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Application Information

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Patent Type & Authority Patents(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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