Preparation method for compound 3 alpha-Akebonolic acid and application of compound to preparation of glycosidase inhibitor drug

A technology of glycosidase inhibitors and compounds, which is applied in the field of natural medicinal chemistry, can solve problems such as no separation reports, and achieve the effects of abundant material sources, easy operation, and good economic benefits

Inactive Publication Date: 2014-03-12
SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no research report on its glycosidase inhibitor activity so far, and there is no literature on its isolation from other plants of the genus Akebia.

Method used

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  • Preparation method for compound 3 alpha-Akebonolic acid and application of compound to preparation of glycosidase inhibitor drug
  • Preparation method for compound 3 alpha-Akebonolic acid and application of compound to preparation of glycosidase inhibitor drug
  • Preparation method for compound 3 alpha-Akebonolic acid and application of compound to preparation of glycosidase inhibitor drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Preparation of 3α-Akebonolic acid in Akebia clover fruit

[0023] 1.1 Plant source and identification

[0024] The fruit samples of Akebia trifolia (Thumb.) Koidz., a plant material for extraction, were collected from Hunan Province in September 2009 and identified by Xing Fuwu, a researcher at South China Botanical Garden, Chinese Academy of Sciences.

[0025] 1.2 Extraction and separation

[0026] The sample (dried fruit of Akebia trifoliata, weighing 1.0 kg) was crushed and extracted three times with 95% ethanol at room temperature, the combined filtrate was concentrated under reduced pressure to remove the organic solvent ethanol, and the crude extract of the total extract was obtained. Suspend the crude extract of the total extract in 500ml of water, extract three times with an equal volume of petroleum ether, and concentrate the extract under reduced pressure to obtain the total extract of petroleum ether (16g). Dissolve the petroleum ether total extr...

Embodiment 2

[0030] Example 2: Preparation of 3α-Akebonolic acid in Akebia quinata fruit

[0031] 2.1 Plant source and identification: same as Example 1

[0032] 2.2 Extraction and separation

[0033] The sample (Akebia fruit, dry weight 1.0 kg) was crushed and extracted three times with 95% ethanol at room temperature, the combined filtrate was concentrated under reduced pressure to remove the organic solvent ethanol, and the crude extract of the total extract was obtained. Suspend the crude extract of the total extract in 500ml of water, extract three times with an equal volume of petroleum ether, and concentrate the extract under reduced pressure to obtain the total extract of petroleum ether (12g). Dissolve the petroleum ether total extract with acetone (150mL), add normal phase silica gel (80-100 mesh) to mix the sample at a weight ratio of 1:1.5, evaporate to dryness, and dry the column (200-300 mesh, 300g) to dry Samples were loaded using petroleum ether / acetone=100:0, 20:1, 5:1, ...

Embodiment 3

[0035] Take the stems and leaves of Akebia clover, Akebia clover, or the stems, leaves or fruits of Akebia syringae, Akebia bainosa, and Akebia syringae as samples, and finally purify according to the extraction and separation methods described in Example 1 to obtain the formula ( I) The pure compound 3α-Akebonolic acid.

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PUM

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Abstract

The invention discloses a preparation method for a compound 3 alpha-Akebonolic acid and the application of the compound in the preparation of a glycosidase inhibitor drug. According to the invention, an alpha-glucosaccharase inhibitor is extracted and separated from akebia plants; the source of the plant material is abundant, the extraction and preparation method is easy to operate, and the plants can be utilized for a long term without being damaged through adopting fruits for extraction, so that the economic benefit can be improved, and the monomeric compound is environmentally friendly, stable, and easy to store. Pharmacology experiments show that the activity of the alpha-glucosaccharase inhibitor of the compound 3 alpha-Akebonolic acid is higher than that of the first-line diabetes drug acarbose, so that the compound 3 alpha-Akebonolic acid is expected to be developed into a drug for preventing and treating type 2 diabetes mellitus, and has excellent application and development prospects.

Description

Technical field: [0001] The invention belongs to the field of natural medicinal chemistry, and in particular relates to a method for separating and preparing a nortriterpene compound 3α-Akebonolic acid, and the use of the compound or its pharmaceutically acceptable salt or its esterified derivative in the preparation of glycosidase inhibitor drugs application. Background technique: [0002] Diabetes is a common clinical endocrine and metabolic disorder disease, which has an important correlation with the annual increase of cardiovascular diseases and cancers, and is an important killer of human health. With the progress of society and the improvement of people's living standards, the incidence of diabetes is increasing worldwide. In my country, the prevalence of diabetes is more than 100 million, and it shows a trend of increasing year by year. Diabetes is causing more and more serious losses to our people's health and national economy. [0003] Diabetes in western medicin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P3/10C07J63/00
Inventor 谭建文王晶徐巧林周忠玉罗应
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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