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Diterpenoid compound and preparing method and application thereof

A technology for compounds and diterpenoids, applied in the field of diterpenoids and their preparation, can solve the problems of less pharmacological activity and the like, and achieve the effects of high purity, good anti-inflammatory activity and wide source of raw materials

Inactive Publication Date: 2015-12-09
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are few research reports on the phytochemical constituents and pharmacological activities of Angelica sinensis

Method used

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  • Diterpenoid compound and preparing method and application thereof
  • Diterpenoid compound and preparing method and application thereof
  • Diterpenoid compound and preparing method and application thereof

Examples

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preparation example Construction

[0036] The preparation method of the diterpenoid compound of the present invention is obtained by extracting extract, organic solvent extraction, silica gel column chromatography, and high pressure liquid chromatography from the root of Angelica sinensis as the raw material, specifically:

[0037] A. Extraction of extract: Air-dry and crush the root of Angelica sinensis to obtain particles with a particle size of 0.05 to 0.15 cm. Add 4 to 8 times the weight ratio of Angelica sinensis root to a volume percentage of 80-95% ethanol solution. Reflux and extract 3~5 times at 65~74℃, 1~3h each time, combine the extracts, filter the extracts, concentrate the extracts under reduced pressure to a specific gravity of 1.1-1.3 to obtain extract a;

[0038] B. Organic solvent extraction: Add 2~4 times the weight of water to extract a, and then use the same volume of petroleum ether, ethyl acetate and n-butanol for extraction. Each solvent is extracted 4~6 times. The solvent is evaporated to obt...

Embodiment 1

[0052] Preparation of Example 1 Compound

[0053] Source of material: Angelica sinensis was collected in Kunming, Yunnan, and was identified by Associate Professor Yang Qingsong, School of Ethnic Medicine, Yunnan Nationalities University Araliadumetorum Hand.-Mazz, specimens are kept in the Herbarium of the School of Ethnic Medicine, Yunnan Nationalities University.

[0054] Take the following steps:

[0055] a. Crushing: 10Kg of black fruit soil angelica root is dried and crushed into particles with a particle size of 0.1cm to obtain black fruit soil angelica powder for use;

[0056] b. Reflux extraction: the black fruit angelica powder prepared in step a was refluxed and extracted at a temperature of 65°C for 4 times, each for 2 hours, with 60Kg of 80% ethanol each time, and the ethanol extracts were combined for use;

[0057] c. Concentration: the ethanol extract obtained in step b is filtered through 80-120 micron filter paper and concentrated under reduced pressure with a rotary ev...

Embodiment 2

[0060] Example 2 Preparation of compound

[0061] Take the following steps:

[0062] a. Crushing: 10Kg of black fruit soil angelica root is dried and crushed into particles with a particle size of 0.1cm to obtain black fruit soil angelica powder for use;

[0063] b. Reflux extraction: the black fruit angelica powder prepared in step a was refluxed and extracted 3 times at a temperature of 67° C., each 2.5 hours, each time with 60Kg of 84% ethanol extraction, combined with the ethanol extracts for use;

[0064] c. Concentration: the ethanol extract obtained in step b is filtered through 80-120 micron filter paper and concentrated under reduced pressure with a rotary evaporator at a temperature of 50°C. When the specific gravity is 1.2, 1340g of extract is obtained for use;

[0065] d. Extraction: Suspend 1340g extract in 4000ml water, and extract with 4000ml petroleum ether, 4000ml ethyl acetate and 4000ml n-butanol successively. Extract each solvent 4 times, and then use a rotary evapor...

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Abstract

The invention discloses a diterpenoid compound and the preparing method and application thereof. The diterpenoid compound is obtained by using aralia melanocarpa roots as the raw material through extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation. The molecular formula of the diterpenoid compound is C20H30O3. The name of the diterpenoid compound is 14-oxygen-ent-8(9),15-(14-oxo-ent-pimara-8(9),15-diene-19-oic acid). The structural formula is as shown in the specification. According to the preparing method, aralia melanocarpa roots are used as the raw material, and extractum extraction, organic solvent extraction, column chromatography on silica gel and high pressure liquid chromatography separation are conducted to generate the diterpenoid compound. The diterpenoid compound can be applied to preparation of anti-inflammatory drugs for prevention and / or treatment. The diterpenoid compound is subjected to in-vitro anti-inflammatory activity testing, and experimental results show a good lipopolysaccharide (LPS) restraining effect and a good effect of inducting pulmonary alveolar macrophages (RAW264.7) to generate NO. A new compound or lead compound with high application value can be provided for the medical industry.

Description

technical field [0001] The invention belongs to the technical field of extraction of plant active ingredients, and in particular relates to a diterpenoid compound and its preparation method and application. Background technique [0002] At present, the treatment of acute and chronic inflammation is mainly based on antibiotics and hormone drugs. Although the treatment of these drugs can receive good results, due to the continuous increase of drug-resistant strains, there are more and more cases despite the use of antibiotics. The condition cannot be effectively controlled, and it is not uncommon for antibiotics to produce side effects in clinical application. Some inflammatory diseases are caused by viral infections, and antibiotics are basically ineffective. In recent years, researchers at home and abroad have gradually turned their attention to resource-rich, pure natural Chinese herbal medicines and ethnic medicines, hoping to find new anti-inflammatory drugs from them. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C62/38C07C51/42A61P29/00
CPCC07C51/42C07C62/38
Inventor 黄相中李艳红江志勇孙静贤夏福婷
Owner YUNNAN MINZU UNIV
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