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A kind of diterpenoid compound and its preparation method and application

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

Inactive Publication Date: 2017-05-03
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • A kind of diterpenoid compound and its preparation method and application
  • A kind of diterpenoid compound and its preparation method and application
  • A kind of diterpenoid compound and its preparation method and application

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preparation example Construction

[0036] The preparation method of the diterpenoid compound of the present invention is to use the root of Angelica sinensis as a raw material, and obtain it through extract extraction, organic solvent extraction, silica gel column chromatography, and high-pressure liquid chromatography, specifically:

[0037] 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;

[0038] 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, every kin...

Embodiment 1

[0052] The preparation of embodiment 1 compound

[0053] Source of material: Heiguo soil angelica was collected in Kunming, Yunnan, and was identified as Aralia dumetorum Hand.-Mazz, the specimen is preserved in the Herbarium of the School of Medicine for Nationalities, Yunnan University for Nationalities.

[0054] Take the following steps:

[0055] 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;

[0056] 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 60Kg of 80% ethanol, combined ethanol extract, for subsequent use ;

[0057] C, concentration: the ethanol extract that step b makes is filtered through 80-120 micron filter paper and carries out decompression concentration with rotary evaporator at the temperature of 50 ℃, and w...

Embodiment 2

[0060] The preparation of embodiment 2 compound

[0061] Take the following steps:

[0062] 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;

[0063] 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 60Kg 84% ethanol, combined ethanol extract, for subsequent use ;

[0064] C, concentration: the ethanol extract that step b is made is filtered through 80-120 micron filter paper and carries out decompression concentration with rotary evaporator at the temperature of 50 ℃, and when specific gravity is 1.2, extractum 1340g is obtained, for subsequent use;

[0065] d, extraction: suspending 1340g extract in 4000ml water, extracting successively with 4000ml sherwood oil, 4000ml ethyl acetate and 4000ml n-butanol, extracting 4 times with ea...

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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 Patents(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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