Swertiamarin thermal conversion product, as well as preparation method, preparation and application thereof

A technology of licoricein and transformation product, which is applied in the directions of digestive system, organic chemistry, antiviral agent, etc., can solve the problems of long production cycle, complex structure, low content and the like, and achieves low cost, easy industrial production and operation. easy effect

Inactive Publication Date: 2015-04-08
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

The content of this kind of ingredients in plants is very low, and it does not have industrial production and commercial application value. Because of its complex structure, it cannot be obtained by chemical synthesis.
[0003] Chinese patent (Application No. 201010587969.5) "Swerterolactone H-K, its pharmaceutical composition and its use" discloses the preparation method and application of four swertirolactone compounds: dry and pulverize the whole herb of A. Ethanol is easy to reflux for extraction, and the extract is concentrated under reduced pressure and then suspended in water, followed by extraction with petroleum ether, ethyl acetate and n-butanol, and the ethyl acetate part is repeatedly subjected to silica gel column chromatography to separate and obtain 4 swertrolactone compounds , the amount of compound obtained is small, and the production cycle is long, so it is difficult to industrialize production

Method used

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  • Swertiamarin thermal conversion product, as well as preparation method, preparation and application thereof
  • Swertiamarin thermal conversion product, as well as preparation method, preparation and application thereof

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preparation example Construction

[0021] The preparation method of the thermal conversion product of swertiamarin of the present invention comprises the following steps:

[0022] A. Take the raw material swertiamarin, add 1 to 20 times the weight of water, and reflux at above 80°C for 5 to 7 hours until the swertiamarin completely disappears to obtain a transformation liquid;

[0023] B. Cool the conversion liquid and filter to obtain filtrate and filter residue. Add 80-120 mesh silica gel with a weight ratio of 0.1-2 times the filter residue to the filter residue to mix the sample, put it on a silica gel column, and use petroleum ether with a volume ratio of 15:1-3:1 -Acetone solution for gradient elution, and then chloroform-methanol solution with a volume ratio of 20:1~0:1 for gradient elution, TLC monitoring and collection of eluent, and concentration under reduced pressure to obtain the target compound.

[0024] The temperature of reflux described in step A is 90~100°C.

[0025] The complete disappearanc...

Embodiment 1

[0030] Take 20kg of swertiamarin, add 15 times the weight of water, heat up to 95°C to carry out the conversion reaction, after the detection of swertiamarin completely disappears, the reaction stops, cool to room temperature, and filter to obtain the filter residue; add 1.5 times to the filter residue Mix the sample with a weight of silica gel, dry it and put it into a silica gel column, first use petroleum ether-acetone (15:1-3:1) gradient elution, and then use chloroform-methanol (20:1-0:1) for gradient elution Remove, collect the target components, concentrate, and dry to obtain the thermal conversion product of swertiamarin. After testing, swertrolactone accounts for 76% of the total thermal conversion product, which contains swertirolactone G, swertia Lactone I, swertirolactone J, swertirolactone K; red-platinolactone accounted for 6% of the total thermal conversion products.

Embodiment 2

[0032] Take 30kg of swertiamarin, add 20 times the weight of water, heat up to 100°C to carry out the conversion reaction, after the detection of swertiamarin completely disappears, the reaction stops, cool to room temperature, filter to obtain the filter residue; add 2 times to the filter residue Mix the sample with a weight of silica gel, dry it and put it into a silica gel column, first use petroleum ether-acetone (15:1-3:1) gradient elution, and then use chloroform-methanol (20:1-0:1) for gradient elution Remove, collect the target components, concentrate, and dry to obtain the thermal conversion product of swertiamarin. After testing, swertrolactone accounts for 80% of the total thermal conversion product, which contains swertirolactone A, swertia Lactone C, swertrolactone J, swertrolactone K, swertrolactone M; red-platinolactone accounted for 4% of the total thermal conversion products.

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Abstract

The invention discloses a swertiamarin thermal conversion product, as well as a preparation method and an application thereof. The swertiamarin thermal conversion product is prepared from swertiamarin as a raw material through heating conversion, elution, separation and purification; and the swertiamarin thermal conversion product contains false Chinese swertia herb lactone composition with the weight percent being over 60%. The method disclosed by the invention is simple and convenient to operate and low in cost; the problems that a false Chinese swertia herb lactone component is low in content in plants, and cannot be greatly obtained easily through chemical synthesis due to a complicated molecular structure are solved. Compared with swertiamarin, the swertiamarin thermal conversion product obtained by the method is relatively high in hepatoprotective activity and anti-HBV activity, and can be applied to prevention and treatment of related hepatitis diseases.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a thermal conversion product of swertiamarin and its preparation method and application. Background technique [0002] Swerterolide is a kind of multi-chiral, highly oxidized, highly condensed natural product with complex structure, most of which have anti-hepatitis B virus activity, and have been isolated from the anti-hepatitis drug Folium bile in recent years. The content of such components in plants is very low, which has no industrial production and commercial application value, and cannot be obtained by chemical synthesis due to its complex structure. [0003] Chinese patent (Application No. 201010587969.5) "Swerterolactone H-K, Its Pharmaceutical Composition and Its Use" discloses the preparation method and application of four swertirolactone compounds: dry and pulverize the whole herb of A. Ethanol is easy to reflux for extraction, the extract is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/22A61K31/366A61P31/20A61P1/16
CPCC07D493/22
Inventor 周志宏杨树德淤泽浦谭文红马晓霞
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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