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Phenylpropanoid compounds as well as preparation method and application thereof

A compound, the technology of phenylpropanoid, applied in the field of phytochemistry, can solve the problem of unreported reductase inhibitory activity

Inactive Publication Date: 2016-10-12
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

A kind with 5 was obtained by separation α - The reductase inhibitory activity of phenylpropanoids, which are related to the 5 α - Reductase inhibitory activity has also not been reported

Method used

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  • Phenylpropanoid compounds as well as preparation method and application thereof
  • Phenylpropanoid compounds as well as preparation method and application thereof
  • Phenylpropanoid compounds as well as preparation method and application thereof

Examples

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preparation example Construction

[0028] The preparation method of the phenylpropanoid compound described in the present invention is to use the dry whole herb of Swertia chinensis as raw material, through the steps of extraction from extract, MCI decolorization, silica gel column chromatography, and high-pressure liquid chromatography, specifically:

[0029] A. Extraction of extract: crush the whole herb of Swertia chinensis, extract 3~5 times at room temperature with 95% ethanol, 3 days each time, combine the extracts, filter, concentrate the extracts under reduced pressure, let stand, filter In addition to sediment, concentrated into extract a;

[0030] B. MCI decolorization: the extract a is decolorized with an MCI column, eluted with 80%-95% methanol / water, combined with the organic phase, concentrated under reduced pressure to obtain extract b;

[0031]C. Silica gel column chromatography: the extract b is dry-packed with 100-200 mesh silica gel with a weight ratio of 8-10 times for silica gel column chro...

Embodiment 1

[0041] The raw material is black and purple waterweed from Diqing area, Yunnan Province. Sampling 2.5 kg of the whole herb of Swertia chinensis and crushing it, extracting 4 times with 95% ethanol at room temperature, 3 days each time, 3.5 L of extracting solution each time, combining the extracting solutions, filtering, and concentrating under reduced pressure to form an extract. Obtained extract 86 g. The extract was decolorized with an MCI column and eluted with 90% methanol / water. The decolorized extract was dissolved in 55 g of chloroform / methanol mixed solvent, and then 52 g of 80-mesh silica gel was added to mix the sample. After mixing the sample, use 1 kg of 100-200 mesh silica gel to dry-pack the column; Chloroform / acetone solution was used for gradient elution, the gradient eluate was collected, concentrated, and the same fractions were pooled, the volume of which was 1 g of the 8:2 fraction; the 8:2 fraction was passed into the reverse phase C 18 Medium pressure ...

Embodiment 2

[0043] The raw material is black and purple waterweed from Diqing area, Yunnan Province. Sampling 2.5 kg of the whole herb of Swertia chinensis and crushing it, extracting 4 times with 95% ethanol at room temperature, 3 days each time, 3.5 L of extracting solution each time, combining the extracting solutions, filtering, and concentrating under reduced pressure to form an extract. Obtained extract 86 g. The extract was decolorized with an MCI column and eluted with 90% methanol / water. The decolorized extract was dissolved in 55 g of chloroform / methanol mixed solvent, and then 52 g of 80-mesh silica gel was added to mix the sample. After mixing the sample, use 1 kg of 100-200 mesh silica gel to dry-pack the column; Chloroform / acetone solution was used for gradient elution, the gradient eluate was collected, concentrated, and the same fractions were pooled, the volume of which was 1 g of the 8:2 fraction; the 8:2 fraction was passed into the reverse phase C 18 Medium pressure ...

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Abstract

The invention discloses phenylpropanoid compounds as well as a preparation method and an application thereof. The phenylpropanoid compounds are separated from Swertia atroviolacea, are named 3-hydroxy-1-(6-hydroxymethyl-1,3-dihydroisobenzofuran-5-yl)propan-1-one and have the structural formula shown in the specification, and a molecular formula of the phenylpropanoid compounds is C12H14O4. The preparation method of the phenylpropanoid compounds comprises the following steps: the Swertia atroviolacea is taken as the raw material and subjected to extract extraction, MCI decoloration, silica gel column chromatography and HPLC (high performance liquid chromatography) separation. 5 alpha-reductase activity tests prove that the phenylpropanoid compounds have better inhibition function on 5 alpha-reductase. The invention further discloses the preparation method and the application of the phenylpropanoid compounds. The compounds are simple in structure, have better 5 alpha-reductase inhibition function and can serve as lead compounds for preparing 5 alpha-reductase inhibitors.

Description

technical field [0001] The invention belongs to the technical field of phytochemistry, and in particular relates to a phenylpropanoid compound extracted for the first time from Swertia chinensis and its preparation method and application. Background technique [0002] Swertia ( Swertia ) is a genus of Gentianaceae, there are about 170 species in the world, and there are more than 80 species in my country, mainly distributed in Yunnan, Sichuan and other places. In my country, this genus has a long history of being used as medicine. There are 35 kinds of medicinal plants. It has the functions of clearing away heat and gallbladder, dehumidifying and detoxifying, and is often used to treat acute jaundice hepatitis, osteomyelitis and other diseases. The plants of this genus are rich in chemical components, mainly including compounds such as ketones, flavonoids, iridoids, triterpenes and alkaloids. Black and Purple Swertia ( Swertia atroviolacea ) is a perennial herbaceous pla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/87A61P13/08A61P17/10A61P17/14A61P17/00
CPCC07D307/87
Inventor 吴海燕李干鹏周敏蒋薇左马怡杨青松胡秋芬
Owner YUNNAN MINZU UNIV
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