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Tricyclic diterpenoid compound and preparation method and application thereof

A technology for tricyclic diterpenes and compounds, which is applied in the field of tricyclic diterpenoids and their preparation, can solve the problems of low pharmacological activity and the like, and achieve the effects of high purity, good anticancer activity and wide source of raw materials

Inactive Publication Date: 2015-12-16
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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  • Tricyclic diterpenoid compound and preparation method and application thereof
  • Tricyclic diterpenoid compound and preparation method and application thereof
  • Tricyclic diterpenoid compound and preparation method and application thereof

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preparation example Construction

[0034] The preparation method of the tricyclic diterpenoids of the present invention is obtained by extracting the stem of Angelica sinensis as a raw material, extracting from the extract, extracting with an organic solvent, silica gel column chromatography, and separating by high-pressure liquid chromatography, specifically:

[0035] A, extraction of extract: dry and pulverize the stems 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 stem 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;

[0036] 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 wa...

Embodiment 1

[0052] The preparation of embodiment 1 compound

[0053] Source of material: Angelica sinensis was collected in Kunming, Yunnan. It was identified as Araliadumetorum Hand.-Mazz by Associate Professor Yang Qingsong, School of Nationalities Medicine, Yunnan University for Nationalities, and the specimen was preserved in the Herbarium of School of Medicine for Nationalities, Yunnan University for Nationalities.

[0054] Take the following steps:

[0055] (1) Dry and crush 10Kg of Angelica sinensis stems into particles with a particle size of 0.1cm to obtain Angelica sinensis powder. Reflux the Angelica sinensis powder with 60Kg of 80% ethanol at a temperature of 65°C each time Extract 4 times, 2 hours each time, combine the ethanol extracts, and set aside;

[0056] (2) Filter the ethanol extract prepared in step (1) 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 obta...

Embodiment 2

[0059] The preparation of embodiment 2 compound

[0060] Take the following steps:

[0061] (1) Dry and crush 10Kg of Angelica sinensis stems into particles with a particle size of 0.1cm to obtain Angelica sinensis powder. Reflux the Angelica sinensis powder with 60Kg of 84% ethanol at a temperature of 67°C each time Extract 3 times, 2.5 hours each time, combine the ethanol extracts, and set aside;

[0062] (2) Filter the ethanol extract prepared in step (1) 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 for later use;

[0063] (3) Suspend 1340g of the extract in (2) in 4000ml of water, sequentially extract with 4000ml of petroleum ether, 4000ml of ethyl acetate and 4000ml of n-butanol, extract 4 times with each solvent, and then evaporate it with a rotary evaporator Solvent, respectively petroleum ether, ethyl acetate and n-butanol extrac...

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Abstract

The invention discloses a tricyclic diterpenoid compound and a preparation method and application thereof. The tricyclic diterpenoid compound is obtained by taking aralia melanocarpa stems as raw materials through extract leaching, organic solvent extraction, silica gel column chromatography and high pressure liquid chromatography separation. The molecular formula of the compound is C20H32O4, the compound is named dumetorumane A, and the structural formula of the compound is as shown in the specification. The preparation method comprises the following steps: by taking the aralia melanocarpa stems as the raw materials, carrying out extract leaching, organic solvent extraction, silica gel column chromatography and high pressure liquid chromatography separation so as to obtain the tricyclic diterpenoid compound. The tricyclic diterpenoid compound can be applied to preparation of medicines for preventing and / or treating tumors and can be applied to preparation of medicines for preventing and / or treating human lung adenocarcinoma, human acute promyelocytic leukemia or human breast cancer. The tricyclic diterpenoid compound has obvious inhibiting effects on human lung adenocarcinoma, human acute promyelocytic leukemia or human breast cancer cell strains, has favorable anti-cancer activity, and can serve as an anti-cancer active ingredient 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 tricyclic diterpene compound and its preparation method and application. Background technique [0002] Angelica with black fruit soil ( Aralia du Metorum Hand.-Mazz) is a plant of the genus Araliaceae (Araliaceae), and its root is used as medicine among the people, and it enters the spleen and stomach meridians. The plant has the effects of invigorating the middle and replenishing qi, expelling toxins, and reducing inflammation. It is used for lymphadenitis, chronic suppurative osteomyelitis, and boils and carbuncles. The phytochemical constituents of this genus mainly contain diterpenes, triterpene saponins, coumarins, flavonoids, lignans and sterols. It has been reported in the literature that diterpenoids have antitumor activity (ChangL.C., SongL.L., ParkE.J., LuyengiL., LeeK.J., FarnsworthN.R., PezzutoJ.M., and KinghornA.D. Bioa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C62/32C07C51/42C07C51/47A61K31/19A61P35/00
CPCC07C51/42C07C51/47C07C62/32
Inventor 黄相中李艳红孙静贤夏福婷
Owner YUNNAN MINZU UNIV
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