A kind of ketone compound and its preparation method and application

A kind of mouthshanone and compound technology, applied in the field of mouthshanone compound

Inactive Publication Date: 2018-03-13
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention has isolated a kind of ketanone compound with 5α-reductase inhibitory activity from black violet swertia, which has not been reported so far

Method used

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  • A kind of ketone compound and its preparation method and application
  • A kind of ketone compound and its preparation method and application
  • A kind of ketone compound and its preparation method and application

Examples

Experimental program
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preparation example Construction

[0028] The preparation method of the ketone compound of the present invention is to use dried black swertia herb 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: take the dried whole herb of Swertia chinensis as raw material, crush it, extract it with 95% ethanol at room temperature for 3~5 times, each time for 3 days, combine the extracts, filter, concentrate and extract under reduced pressure solution, let it stand, filter out the precipitate, and concentrate 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 80-100 mesh silica gel with a weight ratio of 8-10 times for sili...

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 japonica, dried and crushed, extracted 4 times with 95% ethanol at room temperature, 3 days each time, 3.5 L of extract each time, combined the extracts, filtered, and concentrated under reduced pressure to obtain an extract , to obtain extract 121g. The extract was decolorized with an MCI column, and the elution condition was methanol / water 90:10. The decolorized extract was dissolved in 240 grams of chloroform / methanol mixed solvent, and then 120 grams of 100-mesh silica gel was added to mix the sample. After mixing the sample, use 600 grams of 100-mesh silica gel to dry-pack the column; use chloroform / The acetone solution is used for gradient elution, the gradient eluate is collected, concentrated, and the same parts are combined, wherein the volume ratio of the eluate is 7:3 and the part of the eluate is passed into the reversed-phase C18 ...

Embodiment 2

[0043] The raw material is black and purple waterweed from Diqing area, Yunnan Province. Sampling 2.0kg of the whole herb of Swertia chinensis, drying and pulverizing, extracting 3 times with 95% ethanol at room temperature, 3 days each time, 3.0L of extracting solution each time, combining the extracting solutions, filtering, and concentrating under reduced pressure to form an extract , to obtain extract 105g. The extract was decolorized with an MCI column, and the elution condition was methanol / water 90:10. The decolorized extract was dissolved in 200 grams of chloroform / methanol mixed solvent, and then 100 grams of 80-mesh silica gel was added to mix the sample. After mixing the sample, use 500 grams of 80-mesh silica gel to dry-pack the column; use chloroform / The acetone solution is used for gradient elution, the gradient eluate is collected, concentrated, and the same parts are combined, wherein the volume ratio of the eluate is 7:3 and the part of the eluate is passed ...

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Abstract

The invention discloses a xanthone compound (1) capable of inhibiting 5 alpha-reductase. The xanthone compound is extracted from Swertia atroviolacea, the molecular formula is C18H18O5, the compound is named as: 6-(2-hydroxyethyl) -1,7-dimethoxy-3-methyl-xanthone, the xanthone compound has the structural formula which is defined in the description. The preparation method of the xanthone compound comprises the following steps: using the Swertia atroviolacea as the raw material, subjecting the raw material to extracting, MCI decoloration, silica gel column chromatography and high-pressure liquid chromatography to obtain the xanthone compound. The 5 alpha-reductase activity test on the xanthone compound shows that the xanthone compound has relatively good inhibition effect on the 5 alpha-reductase and the compound can be used as a lead compound for preparing a 5 alpha-reductase inhibitor.

Description

technical field [0001] The invention belongs to the technical field of phytochemistry, and in particular relates to a ketanone compound extracted for the first time from Swertia chinensis. At the same time, the invention also relates to the preparation method of the compound and its 5α-reductase inhibitory activity. 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. B...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/86A61P35/00A61P9/00A61P3/10A61P39/06A61P31/00
CPCA61K36/51C07D311/86
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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