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Compound with tumor inhibition activity and extraction method thereof

A compound, ethyl acetate extraction technology, applied in the fields of organic active ingredients, organic chemistry, anti-tumor drugs, etc., can solve the problems of waste disposal and less research on active ingredients

Inactive Publication Date: 2020-06-19
HEILONGJIANG UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, domestic and foreign studies on Schisandra mainly focus on the chemical components and activities of Schisandra fruit. According to the existing technology, Schisandra fruit contains various chemical components such as schisandrin, lignans, organic acids, volatile oils, amino acids, tannins and polysaccharides. ; and the active ingredients in Schisandra leaves, which are the main components of Schisandra chinensis, are less studied, and they are usually thrown away as waste

Method used

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  • Compound with tumor inhibition activity and extraction method thereof
  • Compound with tumor inhibition activity and extraction method thereof
  • Compound with tumor inhibition activity and extraction method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: the isolation of compound 54

[0023] Dried schisandra leaves 14.0Kg, 80% ethanol reflux extraction 2 times, 2h / time, recover solvent to get extract 3.5Kg. Suspend extract and water 1:1 evenly, successively use petroleum ether, ethyl acetate, n-butyl Alcohol was extracted to obtain 381.0 g of petroleum ether layer, 603.0 g of ethyl acetate layer, and 526.0 g of n-butanol layer. Take 263.8 g of the ethyl acetate layer, adopt silica gel column chromatography, and carry out gradient elution with dichloromethane-methanol (1:0-0:1) as the mobile phase, and combine the obtained eluents after TLC analysis and identification, Finally, 9 fractions were obtained, Fr.A-I. Fr.D (22.6g) was separated by MCI column chromatography, methanol-water gradient elution (30:70-80:20, 1:0) to obtain 14 fractions, Fr.D1~Fr.D14. Fr.D8 (1.8g) was separated by SephadexLH-20 Sephadex column chromatography and eluted with methanol to obtain 10 fractions, Fr.D8-1~Fr.D8-10. Fr.D5 (20...

Embodiment 2

[0031] Example 2 Compound 54 Activity Screening and Results

[0032] 2.1 Experimental method

[0033] Caco2 colonic epithelial cells were purchased from the Cell Resource Center of Shanghai Academy of Biological Sciences, Chinese Academy of Sciences and cultured in DMEM containing 20% ​​FBS and 1% PS at 37°C, 5% CO 2 Cell culture chamber.

[0034] The Caco2 cells in the logarithmic growth phase were inoculated in a 96-well culture plate at a density of 1×104 cells / mL, and after 24 hours of complete attachment of the cells, they were cultured with high-glucose medium containing 20% ​​fetal bovine serum, and different concentrations of Nortriterpene compound 54 solution (0-1000 μg / mL), add 200 μL to each well, set up six duplicate wells, and set up blank control group at the same time, at 37 ° C, 5% CO 2 Conditioned for 24h. Add 10 μL of CCK-8 solution to each well, continue to incubate for 1 h, measure the absorbance (A) at 450 nm with a microplate reader, and calculate the ...

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Abstract

The invention relates to a novel compound with tumor inhibition activity and a method for extracting and separating the compound from schisandra chinensis leaves. Activity experiments show that the compound provided by the invention has excellent inhibitory activity on Caco2 colonic epithelial cells.

Description

technical field [0001] The present invention relates to a new compound with anti-tumor activity and an extraction method thereof, in particular to extracting and separating the compound with anti-tumor activity from Schisandra cotyledon leaves. Background technique [0002] Schisandra chinensis is the dry and mature fruit of Schisandra chinensis, a plant of Magnoliaceae, which has the effects of astringing the lungs and relieving cough, nourishing astringent essence, and stopping diarrhea and sweating. At present, domestic and foreign studies on Schisandra mainly focus on the chemical components and activities of Schisandra fruit. According to the existing technology, Schisandra fruit contains various chemical components such as schisandrin, lignans, organic acids, volatile oils, amino acids, tannins and polysaccharides. ; and the active ingredients in Schisandra leaves, which are the main components of Schisandra chinensis, are less studied, and they are usually discarded a...

Claims

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Application Information

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IPC IPC(8): C07D493/22A61K31/365A61P35/00
CPCA61P35/00C07D493/22
Inventor 杨炳友刘艳夏永刚匡海学
Owner HEILONGJIANG UNIV OF CHINESE MEDICINE
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