Diterpenoid compounds, and preparation method and application thereof

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, easy industrial production, and good anticancer activity

Inactive Publication Date: 2015-12-23
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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  • Diterpenoid compounds, and preparation method and application thereof
  • Diterpenoid compounds, and preparation method and application thereof
  • Diterpenoid compounds, and preparation method and application thereof

Examples

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preparation example Construction

[0034] 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:

[0035] 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;

[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 water successively, every kin...

Embodiment 1

[0049] The preparation of embodiment 1 compound

[0050] 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.

[0051] Take the following steps:

[0052] (1) Dry and crush 10Kg of Angelica sinensis roots 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;

[0053] (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 1380g of extract for later use;

[0054] (3) Suspend 1380g of the extract in (2) in 4500ml of wat...

Embodiment 2

[0056] The preparation of embodiment 2 compound

[0057] Take the following steps:

[0058] (1) Dry and crush 10Kg of Angelica sinensis roots 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;

[0059] (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;

[0060] (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 diterpenoid compounds, and a preparation method and application thereof. The diterpenoid compounds are prepared by the following steps: by using Aralia melanocarpa root as a raw material, carrying out extract leaching, organic solvent extraction, silica gel column chromatography and high pressure liquid chromatography separation. The molecular formula of the compounds is C20H28O2 which is named ent-pimar-6,8(14),15-trien-19-oic acid disclosed as the structural formula in the specification. The preparation method comprises the following steps: by using the Aralia melanocarpa root as the raw material, carrying out extract leaching, organic solvent extraction, silica gel column chromatography and high pressure liquid chromatography separation. The invention also discloses application of the diterpenoid compounds in preparing drugs for preventing and / or treating tumor and in preparing drugs for preventing and / or treating human lung adenocarcinoma, human prostatic cancer or human acute medullary system leukaemia. The diterpenoid compounds have obvious inhibiting actions when being applied to drugs for human lung adenocarcinoma, human prostatic cancer or human acute medullary system leukaemia, which indicates that the diterpenoid compounds have favorable anticancer activity and can be used as an anticancer active component or 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 diterpenoid compound and its preparation method and application. Background technique [0002] Aralia ( Aralia ) There are more than 40 species in the world, mainly distributed in Asia and North America. There are 28 species in my country, 20 of which are available for medicinal purposes, distributed almost all over the country, and rich in resources. The root and bark of this genus are mainly used as medicine, which has the functions of expelling wind and dampness, diuresis and swelling, promoting blood circulation and relieving pain. For hepatitis, swollen lymph nodes, nephritis edema, diabetes, leucorrhea, stomach pain, rheumatic joint pain, low back pain, bruises. The research on the chemical constituents and pharmacology of Aralia plants is mainly concentrated in Liaodong Aralia ( A. elata (Miq.) Seem.), Aralia ( A.decaisnea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C61/35C07C51/42A61P35/00A61P35/02
CPCC07C51/42C07C61/35
Inventor 田凯黄相中江志勇李艳红孙静贤夏福婷王韦
Owner YUNNAN MINZU UNIV
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