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29-noroleananoic acid compound and its preparation method and application in the preparation of glycosidase inhibitor medicine

A technology for reducing oleanberries and compounds, which is applied in the directions of steroids, drug combinations, organic chemistry, etc., can solve the problems of insufficient pharmacological activity and ingredients, and achieve the effects of good market prospects, rich material sources, and easy operation.

Active Publication Date: 2015-09-09
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

It has been reported in the literature that the plants of the genus Akebia have anti-inflammatory, diuretic and other pharmacological functions, and are rich in compounds such as triterpenes and nortriterpenes, but the research on pharmacological activities and components is generally not deep enough

Method used

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  • 29-noroleananoic acid compound and its preparation method and application in the preparation of glycosidase inhibitor medicine
  • 29-noroleananoic acid compound and its preparation method and application in the preparation of glycosidase inhibitor medicine
  • 29-noroleananoic acid compound and its preparation method and application in the preparation of glycosidase inhibitor medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1: Preparation of 2,3,20-trihydroxy-29-norolean-12-ene-28-acid in Akebia clover fruit

[0025] 1.1 Instruments and reagents

[0026] The decompression concentration adopts N-1000 rotary evaporator of Tokyo Physical and Chemical Company, CCA-1110 circulating cooling box and SB-1000 electric heating constant temperature water bath; HPLC adopts Japan Shimadzu Company LC-20AT liquid chromatograph, SPD-M20A detection and Shim-PackPRC-ODS chromatographic column (particle size 5μm, pore size 12nm, 250mm×20mm); electrospray mass spectrometry (ESIMS) adopts MDS SCIEX API2000LC / MS / MS instrument from Applied Biosystems, USA, and methanol is used as solvent for direct injection Determination; 1 H NMR spectrum and 13C NMR spectrum was determined by Bruker DRX-400 nuclear magnetic resonance instrument, and tetramethylsilane was used as internal standard. The color development method adopts 10% sulfuric acid ethanol solution or sulfuric acid vanillin treatment, and then hea...

Embodiment 2

[0038] Example 2: Preparation of 2,3,20-trihydroxy-29-norolean-12-ene-28-acid in the stems and leaves of Akebia trifoliata

[0039] 2.1 Instruments and reagents: same as Example 1

[0040] 2.2 Plant source and identification: Same as Example 1

[0041] 2.3 Extraction and separation

[0042] The sample (Akebia trifoliate stems and leaves, dry weight 1.0 kg) was crushed and extracted three times with 95% ethanol at room temperature, and the combined filtrate was concentrated under reduced pressure to remove the organic solvent ethanol to obtain the crude extract of the total extract. The total extract crude extract is suspended in 500ml water, after extracting with an equal volume of sherwood oil, then extracted three times with an equal volume of ethyl acetate, and the ethyl acetate extract is concentrated under reduced pressure to obtain the total extract of ethyl acetate ( 52g). Dissolve the total extract of ethyl acetate with chloroform / methanol (150mL) with a volume rati...

Embodiment 3

[0044] Take the stems, leaves or fruits of Akebia lanceolata, Akebia changxu, Akebia basilicate and Akebia clover as samples, and finally purify according to the extraction and separation methods described in Example 1 to obtain pure compounds of formula (I) 2,3 ,20-Trihydroxy-29-norolean-12-ene-28-oic acid.

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Abstract

The invention discloses a compound 2,3,20-trihydroxy-29-noroleanolic acid, as well as a preparation method and application thereof in preparing glycosidase inhibitor medicines. According to the preparation method, a powerful alpha-glycosidase inhibitor is extracted and separated from akebia plants, the plant material is rich in source, the extracting preparation method is easy to operate, and the plant cannot be destroyed and can be utilized for a long time when the plant fruits are adopted for extraction, so that the economical benefit can be increased, and the environment is protected. The monomeric compound is stable and easy to store. Pharmacological experiments indicate that the activity of the alpha-glycosidase inhibitor of the compound 2,3,20-trihydroxy-29-noroleana-12-ene-28-oic acid is stronger than that of the first line diabetes drug acarbose, and the compound is expected to be developed into a medicine for treating II-type diabetes in clinical application, and has good prospect.

Description

Technical field: [0001] The invention belongs to the field of natural medicinal chemistry, and specifically relates to a new 29-noroleanane acid compound, namely 2,3,20-trihydroxy-29-norolean-12-ene-28-acid, And the method for separating and preparing the compound from the plants of the genus Akebia, and the application of the compound or its pharmaceutically acceptable salt or its esterification derivative in the preparation of glycosidase inhibitor drugs. Background technique: [0002] Diabetes is a common clinical endocrine and metabolic disorder disease, which has an important correlation with the annual increase in cardiovascular diseases and cancers, and is a potentially 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 m...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61P3/10
Inventor 谭建文王晶周忠玉任慧徐巧林
Owner SOUTH CHINA BOTANICAL GARDEN CHINESE ACADEMY OF SCI
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