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Harpertrioate A, medicine for treating and resisting Alzheimer's disease, preparation method and application

A technology of trilactone and trilactone, applied in the field of anti-Alzheimer's medicine and preparation, trilactone A, which can solve the problem of no activity of trilactone A compound question

Active Publication Date: 2021-04-02
KUNMING INST OF BOTANY - CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, up to now, there is no report of auratrilactone A compound and its activity in the prior art

Method used

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  • Harpertrioate A, medicine for treating and resisting Alzheimer's disease, preparation method and application
  • Harpertrioate A, medicine for treating and resisting Alzheimer's disease, preparation method and application
  • Harpertrioate A, medicine for treating and resisting Alzheimer's disease, preparation method and application

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preparation example Construction

[0039] The present invention also provides the preparation method of the auratrilactone A shown in the formula I structure in the above scheme, comprising the following steps:

[0040] 1) using an aqueous ethanol solution with a volume fraction of 90% to 95% to carry out reflux extraction on the branches of the tendon fruit, and collect the extract; concentrate the extract to obtain an extract; resuspend the extract in water to obtain crude extract;

[0041] 2) using petroleum ether to carry out the first extraction of the crude extract, remove the petroleum ether extraction part, and collect the residue; use ethyl acetate to carry out the second extraction of the residue, collect the ethyl acetate part, and obtain ethyl acetate ester extract;

[0042] 3) The ethyl acetate extract is subjected to small-pore resin chromatographic separation, and the first gradient elution is carried out. The procedure of the first gradient elution is: sequentially adopt methanol aqueous soluti...

Embodiment 1

[0081]1) The plant sample of beef tendon fruit is collected from 100 kg of beef tendon fruit sprigs. Drying and pulverizing the twigs of the beef tendon fruit into 80-100 mesh powders and then extracting by heating and refluxing with 95% aqueous ethanol solution by volume fraction, the extraction temperature is 60°C, the volume of the aqueous ethanol solution used for each extraction is 100L, and extracting by heating and refluxing three times, Combine the extracts.

[0082] 2) Concentrating the obtained extract under reduced pressure, recovering the solvent, the condensation temperature is 4° C., the pressure is 0.2-0.25 MPa, and the extract is obtained after concentration. Suspend and disperse the concentrated crude extract with 50L of water, extract three times with 50L petroleum ether, remove the petroleum ether extraction part, collect the residue, and extract the residue three times with 50L ethyl acetate to obtain ethyl acetate extract .

[0083] 3) After the ethyl ac...

Embodiment 2

[0114] The auratrilactone A prepared in advance by the method of Example 1 is added water for injection respectively according to the auxiliary agent used in conventional injections, finely filtered, potted and sterilized to make injections.

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Abstract

The invention provides Harpertrioate A, a medicine for treating and resisting Alzheimer's disease, a preparation method and application, and belongs to the technical field of medicines. The Harpertrioate A can influence the metabolic pathway of amyloid precursor protein (APP), not only can reduce the expression capacity of beta-amyloid proteins Abeta42 and Abeta40, but also can promote the conversion of the APP to a non-Abeta metabolic pathway, shows a certain capacity of resisting the generation of beta amyloid protein Abeta, and has the activity of preventing and treating Alzheimer's disease.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to auratrilactone A, medicines for treating and resisting Alzheimer's disease, preparation methods and applications. Background technique [0002] Harrisonia perforata (Bl.) Merr. is a plant of the genus Harrisonia (Simarubaceae) in the family Simarubaceae. There are four species of this genus in the world, and they are distributed in tropical Africa, tropical Asia and Oceania. In China, beef tendon fruit is mainly distributed in Fujian, Guangdong and Hainan; it is often found in shrubs and open forests at low altitudes. Beef tendon fruit has the effect of clearing away heat and cutting off malaria. The root is used as medicine, which is bitter in taste and cold in nature, and is often used for malaria. However, so far, there is no report on the auratrilactone A compound and its activity in the prior art. Contents of the invention [0003] The object of the present invention i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/20A61K31/366A61P25/28
CPCC07D493/20A61P25/28
Inventor 郝小江姚永刚邸迎彤罗荣灿唐小涵
Owner KUNMING INST OF BOTANY - CHINESE ACAD OF SCI