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Preparation and application of two hepatoprotective triterpenoids in Chizhi

A technology of triterpene compounds and compounds, applied in the field of preparation of triterpene compounds, can solve the problems of unsatisfactory drug efficacy and lack of hepatoprotective drugs, and achieve the effects of good liver protection, good application prospects, and simple operation

Active Publication Date: 2021-07-30
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the efficacy of some hepatoprotective drugs is unsatisfactory. We still lack hepatoprotective drugs with high efficiency and no obvious side effects. However, the research on the hepatoprotective activity of natural medicines has shown broad application prospects.

Method used

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  • Preparation and application of two hepatoprotective triterpenoids in Chizhi
  • Preparation and application of two hepatoprotective triterpenoids in Chizhi
  • Preparation and application of two hepatoprotective triterpenoids in Chizhi

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preparation example Construction

[0025] The preparation method of the two triterpene compounds is that the sub-entity of the Erqhiba is a raw material, extracted with a solvent, extracted, and then separated by a positive phase column after MCI, and finally use semi-prepared HPLC to obtain Compound I and Compound II. .

[0026] The method specifically includes the following steps:

[0027] (1) Organic solvent ultrasound extraction: dried the burricantge entity, smashed to 60-100 mesh, extract 2-4 times after soaking with the first organic solvent at room temperature, 20-40 minutes, combined with extracts, After concentration, you get the red lucidum dipper a.

[0028] (2) Organic Solvent Extraction: Pour the dipper cream into the separatory funnel, adding the water and the second organic solvent weight of the extract weight, stir well, stir well, completely reoperable Take an organic solvent layer, repeated 3 times, combined with the organic solvent layer, and distilled to the Red Hero dip cream B;

[0029] (3) P...

Embodiment 1

[0042] Ganoderma lucidums from Yunnan West Dai Dai Autonomous Prefecture were pulverized to 60 mesh, using 92% of industrial ethanol to extract 3 times at room temperature, 30 minutes each time, concentrated ethanol solution to obtain 0.7 kg.

[0043] Pour the dipper into the separatory funnel, add water 1.2L, stir evenly, add 1.2 l of ethyl acetate, oscillate, then completely stand, wait for water and organic solvent to pull out ethyl acetate, repeated process 3 times, combined Ethyl acetate extracts the solution, and the reduced pressure is distilled to obtain 0.4 kg. Dissolve the dipolor after adding 480 ml of ethyl acetate to the dipper, and then 0.8 kg of silica gel (80-100 mesh) was mixed well and dried at room temperature. Weigh 8kg silica gel (100-200 mesh) mounting silica gel column chromatography, with petroleum ether: acetone (volume ratio 1: 0, 9: 1, 7: 1, 4: 1, 2: 1, 1: 1, and 0: 1) Elution to the eluent to obtain a total of 6 components of AF. The component D (149 g)...

Embodiment 2

[0045] Ganoderma lucidum sub-entity produced from Fuyang, Hubei, was pulverized to 80 mesh, extracted twice with 90% industrial methanol room, 20 minutes each time, concentrated methanol solution 1.2 kg.

[0046] Pour the dipper into the separatory funnel, add 1.5 L of water and 1.5 l-dichloromethane, stir well, and then allowed to stand, and then collect dichloromethane extract, repeated 3 times, combined with dichloromethane extract, The reduced pressure was concentrated to get 0.6 kg of Cauca dipper. After dissolved with 600 ml of dichloromethane, the silica gel was dissolved and stirred evenly, dried at room temperature, separated by the positive phase column of the silica gel column of 18 kg 150, from 1: 0, 9: 1, respectively. 7: 1, 4: 1, 2: 1, 1: 1 and 0: 1 Petroleum ether: Acetone is eluted as the eluent system to obtain a total of 6 components of AF. The group D (330 g) was taken from MCI column chromatography, and the component D1-D5 was obtained by dissolving with 43% -8...

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Abstract

The invention discloses the preparation method and application of two kinds of triterpene compounds with hepatoprotective activity in the medicinal fungus Chizhi. The preparation method of the two kinds of triterpenoids is to use the fruiting body of Chizhi Zhizhi as raw material, extract and extract with chemical solvents, undergo preliminary separation by normal phase column chromatography, decolorize by MCI chromatography, separate by normal phase column chromatography, and then separate by semi-preparative HPLC get. The application is the use of the above two triterpene compounds in the preparation of liver protection drugs. The present invention separates triterpene methylganoderic acid C and 3β,7β-dihydroxy-11,15,23-tricarbonyl-lanostane-8,16-diene-26-carboxylic acid from Chizhi for the first time. The method is simple and the degree of purification is high; in addition, the present invention discovers for the first time that the above-mentioned triterpenoids have good hepatoprotective activity, which provides a basis and a new idea for the extraction and medicinal research of such triterpenoids.

Description

Technical field [0001] The present invention belongs to the field of chemical technology, and therefore involves the preparation method and application of two triterpene compounds having a protective liver activity in August. Background technique [0002] Due to environmental pollution, excessive diet, excessive drinking, food additive abuse such as liver disease increasing increase, leading to higher incidence of hepatitis, fatty liver, hepatic fibrosis, cirrhosis or even liver cancer, and severely threaten human health . So far, some drug-effective drug effects cannot be satisfactory. We still lack high-efficiency, no obvious side effects, and natural drugs have a vast use of prospects. Therefore, the development activity is better, and the treatment of liver disease for liver disease is a problem that researchers need to solve. [0003] Ganoderma lucidum is a famous Chinese medicine in my country. It has a history of medicinal history, which is used to treat various diseases. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/575A61P1/16
CPCA61P1/16C07J9/005
Inventor 周敏刘文星
Owner YUNNAN MINZU UNIV
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