Preparation method and application of guaiacane-type sesquiterpene

A technology of guaiacane and guaiac wood, which is applied in the field of medicine

Inactive Publication Date: 2011-11-30
FUJIAN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, except that our laboratory has studied the chemical components of the petroleum ether extraction part...

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  • Preparation method and application of guaiacane-type sesquiterpene
  • Preparation method and application of guaiacane-type sesquiterpene
  • Preparation method and application of guaiacane-type sesquiterpene

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Embodiment 1

[0007] Embodiment 1: Extraction, separation and structural identification of compounds of the present invention

[0008] (1), extraction: take 5.5kg of the dried whole plant of Pancarina chinensis, grind it, soak it in 95% ethanol at room temperature and extract it 4 times, each time for 7 days. After concentrated under reduced pressure to remove alcohol, 320 g of extract was obtained. The extract was suspended in water and then extracted with petroleum ether, ethyl acetate and n-butanol in sequence to obtain 60 g of petroleum ether, 80 g of ethyl acetate and 130 g of n-butanol.

[0009] (2) Separation: The n-butanol layer was mixed with an equal amount of silica gel and subjected to silica gel column chromatography, eluted with a polar gradient of ethyl acetate-methanol (1:0~0:1), and finally flushed with methanol and combined A total of 8 components (Fr I ~ Fr VIII) were obtained after the same part of the composition. FrⅢ passed through SephadexLH-20 column, chloroform-me...

Embodiment 2

[0014] Example 2: Inhibitory effect of compounds of the present invention on human tumor cell lines

[0015] Methods: The human tumor cell lines K-562, HL-60, MOLT-4 and NB4 cells in the logarithmic growth phase were respectively inoculated on 96-well culture plates, and the inoculation volume in each well was 6000 / 150 μL and 6000 / 150 μL respectively. , 12000 / 150μL and 12000 / 150μL. The experiment consisted of a drug test group, a negative control group and a blank control well. Add 50 μL of the compound of the present invention in different concentrations to each hole of the drug experimental group, and make 3 replicate holes for each concentration; add 50 μL of nutrient solution to each hole of the negative control group, and set 6 replicate holes in total; only add 200 μL of nutrient solution to the blank control wells, and use Zero the instrument. After 72 hours of action, centrifuge to discard the supernatant, add 150 μL of dimethyl sulfoxide (DMSO) to each well, and sha...

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Abstract

The invention belongs to the medical technical field, and concretely relates to a preparation method and an application of guaiane-type sesquiterpene. A guaiane-type sesquiterpene compound is 15-hydroxy-2-oxygen-guaiacum-3-alkene-1alpha, 5alpha, 6beta, 7alpha, 10alpha, 11beta hydrogen-12, 6-lactone (15-hydroxy-2-oxo-guaia-3-en-1alpha, 5alpha, 6beta, 7alpha, 10alpha, 11betaH-12, 6-olide, a compound 1), and can be extracted and separated from a whole plant of prenanthes macrophylla franch. Indicated by the research of experiments, the compound has favorable inhibitory activity for a plurality of tumor cells of human body, therefore, the guaiane-type sesquiterpene can be used for preparing antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a guaiac-type sesquiterpene compound isolated from the plant Pancarina: 15-hydroxy-2-oxo-guaiac-3-ene- 1α, 5α, 6β, 7α, 10α, 11βH-12,6-lactone (15-hydroxy-2-oxo-guaia-3-eh-1α, 5α, 6β, 7α, 10α, 11βH-12,6- Olide, the preparation method and application of compound 1). Background technique [0002] Prenanthes macrophylla Franch. is a plant of the genus Prenanthes in the Compositae family, and is a unique plant in China. There are about 40 species of this genus in the world, mainly distributed in tropical and temperate regions. There are about 16 species in my country, one of which can be used as medicine, and has the effects of treating carbuncle, sores, swollen toxins, promoting blood circulation and stopping bleeding. At present, there are few reports on the phytochemical constituents of this genus, which mainly contain triterpenes, sesquiterpenes, and phytosterols. ...

Claims

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Application Information

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IPC IPC(8): C07D307/93A61P35/00A61K31/365
Inventor 张永红谢捷明陈永胜
Owner FUJIAN MEDICAL UNIV
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