A kind of swertirolactone compound and its preparation method, preparation and application

A technology of sorghum lactone and compound, which is applied in the field of sorghum lactone compound and its preparation, can solve the problems of thermal instability of alkenyl ether bond, occurrence of decomposition, transformation, hidden danger of clinical safety medication, etc., and achieves easy access to raw materials. The effect of obtaining, simple process and strong operability

Active Publication Date: 2017-04-05
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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Problems solved by technology

However, the ene ether bond in the structure of swertiamarin is extremely unstable when heated, and will decompose and transform when heated. Therefore, swertiamarin has not been detected in the Qingyedan ​​injection prepared by the thermal extraction method. Not only has it brought difficulties to the production and inspection of Qingyedan ​​Injection, but it has also brought hidden dangers to clinical safety medication

Method used

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  • A kind of swertirolactone compound and its preparation method, preparation and application
  • A kind of swertirolactone compound and its preparation method, preparation and application
  • A kind of swertirolactone compound and its preparation method, preparation and application

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preparation example Construction

[0024] The preparation method of swertiger lactone compound of the present invention comprises the following steps:

[0025] A. Take swertiamarin, add water with a weight ratio of 3 to 5 times, and reflux at 90 to 100°C for 5 to 7 hours until the swertiamarin completely disappears to obtain the water-soluble part a and the fat-soluble part b;

[0026] B. Take the water-soluble part a, carry out gradient elution with methanol-water solution with a volume ratio of 5:95~100:0 through a reverse column, and collect in sections;

[0027] C. Take the eluate under the methanol-water solution section with a volume ratio of 15:85~30:70, concentrate under reduced pressure to obtain extract a, and extract a through a macroporous adsorption resin column for adsorption, with a volume ratio of 0:100 ~100:0 methanol-water solution for gradient elution, the extract b concentrated under reduced pressure of the eluent, and the extract b is packed with 4~5 times the amount of 160~200 mesh silica ...

Embodiment 1

[0035]Take 5.8 kg of swertiamarin, add 3 times the weight of water, heat to 90°C, and keep the temperature constant for 6 hours, the swertiamarin completely disappears, and the water-soluble part and the fat-soluble part are obtained. The water-soluble part was collected in sections by reverse medium-pressure column, gradient elution with methanol-water (5:95~100:0). Take methanol-water as the eluent under the polar section (15:85~30:70), concentrate under reduced pressure to obtain the extract, and the obtained extract is adsorbed by HPD-100 macroporous adsorption resin, and methanol-water (0: 100-100:0) for gradient elution; and then silica gel column chromatography, using petroleum ether-ethyl acetate (8:1-2:1) for gradient elution to obtain the crude extract of the target compound. After concentration, the crude extract was adsorbed by MCI-gel, and gradient eluted with methanol-water (20:80~100:0), followed by thin-layer chromatography to collect the target components, and...

Embodiment 2

[0037] Take 10 kg of swertiamarin, add 5 times the weight of water, heat to 95°C, keep the temperature for 5 hours, the swertiamarin completely disappears, and the water-soluble part and the fat-soluble part are obtained. The water-soluble part was collected in sections by reverse medium-pressure column, gradient elution with methanol-water (5:95~100:0). Take methanol-water as the eluent under the polar section (15:85~30:70), concentrate under reduced pressure to obtain the extract, and the obtained extract is adsorbed by HPD-300 macroporous adsorption resin, and methanol-water (0: 100-100:0) for gradient elution; and then silica gel column chromatography, using petroleum ether-ethyl acetate (8:1-2:1) for gradient elution to obtain the crude extract of the target compound. After concentration, the crude extract was adsorbed by MCI-gel, and gradient eluted with methanol-water (20:80~100:0), followed by thin-layer chromatography to collect the target components, and the eluate w...

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Abstract

The invention discloses a lactone compound of false Chinese swertia herb, as well as a preparation method, a preparation and an application of the lactone compound. The lactone compound of the false Chinese swertia herb is prepared from swertiamarin as a raw material. A molecular formula of the lactone compound is C18H20O6. The lactone compound has the following structural formula as shown in the specification. The preparation method comprises the steps of separating and purifying a swertiamarin thermal conversion product by a reverse medium-pressure column method, an MCI-GEL method, a silica gel method and the like to prepare the lactone compound. Pharmacological studies show that the lactone compound has a significant liver protection effect and hepatits B virus activity resistance at the same time. The preparation method has the advantages that a raw material is sufficient in source and easy to obtain, the technology is simple, and the method can be used for industrial production.

Description

technical field [0001] The invention belongs to the technical field of phytochemistry, and in particular relates to a swertirolactone compound and its preparation method, preparation and application. Background technique [0002] Swertia mileensis TN HO et WL. Shih is a traditional anti-hepatitis medicine in China. Its original plant is Swertia mileensis (S.mileensis). It is only distributed in Yunnan and is commonly used by Hani and Yi people in Honghe, Yunnan. Anti-hepatitis drugs. The main water-soluble anti-hepatitis component and marked component in Folium Folium is swertiamarin, which contains as high as 12% in the medicinal material of Folium Folium, and accounts for more than 50% of its cold-soaked extract. Aglycone belonging to the group of secoiridoid glycosides. However, the ene ether bond in the structure of swertiamarin is extremely unstable when heated, and will decompose and transform when heated. Therefore, swertiamarin has not been detected in the Qingyeda...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/22A61K31/366A61P1/16A61P31/20
CPCC07D493/22
Inventor 周志宏马晓霞杨竹雅陈海丰淤泽浦
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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