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Germacrane sesquiterpene compound extracted from carpesium cernuum and applications thereof

A technology of tobacco pipe grass and gimane type, which is applied in the field of medicine, can solve the problems of unextracted gimane type sesquiterpenes, etc., and achieve the effects of inhibiting the formation of clones, inhibiting migration, and promoting production and accumulation

Active Publication Date: 2018-12-07
ANSHUN PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, in the prior art, there is no research report on the extraction of gemane-type sesquiterpene Carpescernolides A from natural plants and its activity

Method used

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  • Germacrane sesquiterpene compound extracted from carpesium cernuum and applications thereof
  • Germacrane sesquiterpene compound extracted from carpesium cernuum and applications thereof
  • Germacrane sesquiterpene compound extracted from carpesium cernuum and applications thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] (1) Get 20kg of dry branches and leaves in the tobacco pipe head grass, use 95% industrial ethanol to refluxing extract it at a temperature of 80°C for 3 times, and then reclaim the ethanol alcohol to concentrate to obtain the extract, the extract is miscible with water and becomes turbid, and passes through acetic acid Extract with equal volume of ethyl ester and concentrate to obtain 0.960 kg of ethyl acetate layer extract;

[0028] (2) The ethyl acetate layer extract was subjected to 300-400 mesh silica gel column chromatography, and was eluted with a gradient eluent with a volume ratio of petroleum ether and acetone of 60:1 to 0:1, and merged into 7 Parts: Fr 1–7;

[0029] (3) Carry out MCI column chromatography on Fr 6 in step 2, adopt the gradient elution of the eluent whose volume ratio of methanol to water is 4:6~10:0, and be divided into 4 sub-fractions again: Fr 6a, Fr 6b, Fr 6c and Fr 6d, Fr 6b were purified by semi-preparative high-performance liquid chroma...

Embodiment 2

[0034] Ampoule: 2 mg of the compound Carpescernolides A obtained in Example 1, 10 mg of sodium chloride;

[0035] Preparation method: Dissolve the compound and sodium chloride in an appropriate amount of water for injection, filter the resulting solution, and fill it into an ampoule bottle under sterile conditions.

Embodiment 3

[0037]Capsules: 10 mg of Carpescernolides A obtained in Example 1, 187 mg of lactose, and 3 mg of magnesium stearate;

[0038] Preparation method: mix Carpescernolides A with auxiliary agents, sieve, mix evenly, put the obtained mixture into hard gelatin capsules, each capsule weighs 200 mg, and the active ingredient is 10 mg.

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Abstract

Disclosed is a germacrane sesquiterpene Carpescernolides A compound extracted from carpesium cernuum. The compound is isolated and extracted from a whole plant of the carpesium cernuum. The structuralformula of the compound is represented as the formula (I) which is shown in the description. A preparation method of the germacrane sesquiterpene compound includes the steps of ethanol extraction, extract concentration, silica gel column chromatography, gradient elution, gel column chromatography, semi-preparative high performance liquid chromatography purification and the like. The germacrane sesquiterpene Carpescernolides A compound disclosed by the invention is firstly extracted and isolated for the carpesium cernuum produced in Zhenning, Anshun, Guizhou Province, and the structural formula of the germacrane sesquiterpene Carpescernolides A compound is determined. The compound has a therapeutic effect on human hepatoma SMMC-7721 cells, can induce apoptosis of the SMMC-7721 cells, dose-dependently promotes the production and accumulation of endogenous ROS, inhibits the migration of tumor cells, inhibits the formation of tumor cell cloning, and can be applied in the preparation of medicine for treatment of liver cancer. The compound can be used as a lead compound of medicine for treating liver cancer.

Description

technical field [0001] The invention belongs to the field of medicaments, and in particular relates to a gemane-type sesquiterpene Carpescernolides A compound extracted from tobacco pipe grass and its preparation method and application. Background technique [0002] Tobacco pipe grass (Carpesium cernuum) is a plant of the genus Tianmingjing in the family Compositae. The medicinal part is the whole plant, pungent, cool and bitter. It is slightly poisonous. It mainly survives in areas with an altitude of 60 meters to 3,000 meters, mainly grows in hills, wastelands and ravines, and is distributed in Asia and Europe. There are rich species in Southwest China, Central Plains, North China and other places. Through the method of extracting aromatic oil, tobacco pipe grass is often prepared as a raw material of essence. Used as a national medicine, Yi medicine can treat toothache, mumps, bronchitis, asthma, urinary tract infection, mastitis, snake bites, etc.; Baiyao can treat d...

Claims

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Application Information

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IPC IPC(8): C07D493/22A61K31/365A61P35/00A61P35/04
CPCA61P35/00A61P35/04C07D493/22
Inventor 晏晨张云东孙茂张卫青梁伟王天元
Owner ANSHUN PEOPLES HOSPITAL
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