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Tetracyclic diterpenoid compound and preparation method as well as application thereof

A technology for tetracyclic diterpenoids and compounds, applied in the field of tetracyclic diterpenoids and their preparation, can solve problems such as poor water solubility, toxic and side effects, and achieve the effects of easy industrial production, high purity, and good anticancer activity

Inactive Publication Date: 2015-12-30
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chemically synthesized anticancer drugs, such as metal complex platinum complexes, organic germanium compounds, etc., have strong anticancer properties, but they have defects such as toxic side effects and poor water solubility.

Method used

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  • Tetracyclic diterpenoid compound and preparation method as well as application thereof
  • Tetracyclic diterpenoid compound and preparation method as well as application thereof
  • Tetracyclic diterpenoid compound and preparation method as well as application thereof

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preparation example Construction

[0038] The preparation method of the tetracyclic diterpenoids of the present invention is to use the root of Angelica sinensis as a raw material, and obtain through extraction from extract, organic solvent extraction, silica gel column chromatography, and high-pressure liquid chromatography, specifically:

[0039] A, extraction of extract: dry and pulverize the roots of Angelica sinensis to obtain 0.05 ~ 0.15cm particle size, add 80 ~ 95% ethanol solution with a volume percentage concentration of 4 ~ 8 times of root weight ratio of Angelica sinensis in Reflux extraction at 65~74°C for 3~5 times, each time for 1~3h, combine the extracts, filter the extracts, concentrate the extracts under reduced pressure until the specific gravity is 1.1~1.3 to obtain the extract a;

[0040] B, organic solvent extraction: add the water of 2~4 times of weight ratio in extract a, carry out extraction with sherwood oil, ethyl acetate and n-butanol solvent of equal volume to water successively, eve...

Embodiment 1

[0054] The preparation of embodiment 1 compound

[0055] Source of material: Heiguo soil angelica was collected in Kunming, Yunnan, and was identified as Aralia du Metorum Hand.-Mazz, the specimen is preserved in the Herbarium of the School of Medicine for Nationalities, Yunnan University for Nationalities.

[0056] Take the following steps:

[0057] a. Pulverization: dry and pulverize 10Kg of Heiguotu Angelica root into particles with a particle diameter of 0.1cm to obtain Heiguotu Angelica powder for subsequent use;

[0058] B. reflux extraction: reflux extraction of the Angelica sinensis powder prepared in step a at a temperature of 65° C. for 4 times, each time for 2 hours, each extraction with 60Kg80% concentration of ethanol, combined ethanol extract, for subsequent use;

[0059] c. Concentration: filter the ethanol extract prepared in step b through 80-120 micron filter paper and concentrate under reduced pressure with a rotary evaporator at a temperature of 50°C unti...

Embodiment 2

[0062] The preparation of embodiment 2 compound

[0063] Take the following steps:

[0064] a. Pulverization: dry and pulverize 10Kg of Heiguotu Angelica root into particles with a particle diameter of 0.1cm to obtain Heiguotu Angelica powder for subsequent use;

[0065] B. reflux extraction: reflux extraction of the Angelica sinensis powder prepared in step a at a temperature of 67°C for 3 times, each time for 2.5 hours, each extraction with 60Kg84% concentration of ethanol, combined ethanol extract, for subsequent use;

[0066] c. Concentration: filter the ethanol extract prepared in step b through 80-120 micron filter paper and concentrate under reduced pressure with a rotary evaporator at a temperature of 50°C until the specific gravity is 1.2 to obtain 1340g of extract, which is set aside;

[0067] d, extraction: 1340g medicinal extract is suspended in 4000ml water, extract with 4000ml sherwood oil, 4000ml ethyl acetate and 4000ml n-butanol successively, every kind of so...

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Abstract

The invention discloses a tetracyclic diterpenoid compound and a preparation method as well as application thereof. The tetracyclic diterpenoid compound is obtained through extractum extracting, organic solvent leaching, column chromatography on silica gel and high pressure liquid chromatography separation by taking Araliadumetorum Hand.-Mazz roots as a material. The compound has a molecular formula of C20H30O3, is named as dumetorumane B, and has the following structural formula as shown in the description. The preparation method means that the tetranuclear diterpenoid is obtained through extractum extracting, organic solvent leaching, column chromatography on silica gel and high pressure liquid chromatography separation by taking the Araliadumetorum Hand.-Mazz roots as the material. The application is application of the tetranuclear diterpenoid to preparation of drugs for preventing and / or treating tumour and to preparation of drugs for preventing and / or treating human lung adenocarcinoma, human acute promyelocytic leukemia or human breast cancer. The tetranuclear diterpenoid has a remarkable inhibiting effect on cell strains of human lung adenocarcinoma, human acute promyelocytic leukemia or human breast cancer, has good antitumor activity indicatively, and can serve as an antitumor activity component or a lead compound.

Description

technical field [0001] The invention belongs to the technical field of extraction of plant active ingredients, and in particular relates to a tetracyclic diterpenoid compound and its preparation method and application. Background technique [0002] At present, the incidence of cancer in the world is severe, and the morbidity and mortality continue to rise. The World Health Organization released a report in February 2014, predicting that global cancer cases will show a rapid growth year by year, from 14 million in 2012 to 19 million in 2025 and 24 million in 2035. Statistics from the organization also show that there are about 3.5 million new cancer cases in China every year, and about 2.5 million people die from it. Therefore, finding effective anticancer drugs has become a top priority. In the research of anticancer drugs, the research and clinical application of chemotherapy drugs have made great progress. Chemically synthesized anticancer drugs, such as metal complex p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J61/00A61P35/00A61P35/02
Inventor 田凯黄相中江志勇孙静贤夏福婷李艳红王韦
Owner YUNNAN MINZU UNIV
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