A kind of preparation method and application of diphenylmethane compound

A technology of diphenylmethane and compounds, which is applied in the field of screening out active ingredients of anti-breast cancer cells, can solve problems such as undiscovered pharmacological activity research reports, and achieve enhanced anti-breast cancer cell activity, simple operation, and high yield Effect

Inactive Publication Date: 2019-02-12
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Compound 2 euphordin A, 3,3'-diacetyl-2,4'-dimethoxy-2',4,6,6'-tetrahydroxy-5'-methyldiphenylmethane After reviewing the literature, no research reports on pharmacological activity have been found

Method used

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  • A kind of preparation method and application of diphenylmethane compound
  • A kind of preparation method and application of diphenylmethane compound
  • A kind of preparation method and application of diphenylmethane compound

Examples

Experimental program
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Embodiment 1

[0032] Embodiment 1: the method for preparing monomer compound from Euphorbia chamaejasma

[0033] 30kg of dried Euphorbia chamaejasma, crushed, soaked in 80% (ethanol: water 80:20) ethanol reflux extraction twice, each time for 2 hours, the amount of solvent was 180L and 150L respectively. Combine the extracts, filter while hot, combine and concentrate until no ethanol remains, and concentrate the volume to 8L. Take 2L of the concentrated solution and add 1L of water to dilute it, then extract 3 times with petroleum ether, ethyl acetate and n-butanol in sequence, each time the extraction solvent is 3L, and recover the solvent under reduced pressure to obtain 60g of petroleum ether and 160g of ethyl acetate , 20g of n-butanol.

[0034] The ethyl acetate part was passed through a normal phase silica gel column and eluted with petroleum ether: ethyl acetate 100:1, 50:1, 20:1, 15:1, 10:1, 5:1, 1:1 to obtain Fr. 1-Fr. 7.

[0035] Take 12g of Fr.2 to pass through the normal phas...

Embodiment 2

[0057] Embodiment 2: Anti-breast cancer cell experiment in vitro

[0058]MTT method was used to evaluate cytotoxicity, and 6 types of breast cancer cells were selected for research, namely triple negative breast cancer MDA-MB-231, Sum149, LuminalA type MCF-7, LuminalB type ZR-75-1, Her 2 positive type SKBr3, BT474. Paclitaxel was used as the positive control drug. Adjust the above six kinds of breast cancer cell density to 5 × 10 4 cells / ml, inoculate into 96-well culture plate, inoculate 100 μL cell suspension in each well, place at 37°C, 5% CO 2 Cultivate overnight in an incubator, observe that the cells adhere to the wall and grow well, and then set up a positive control group, a tumor cell control group and an experimental group with different concentrations of drugs. The experimental group added 8 sample solutions with gradient concentrations. The concentration of compound 1 and 2 mother solutions was 5mM, and the concentration of paclitaxel mother solution was 3.5mM. ...

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Abstract

The invention belongs to the technical field of medicine and relates to a preparation method of a diphenylmethane compound, in particular to two diphenylmethane compounds, ebracteolatain A and 3,3'-diacetyl-2,4'-dimethoxy-2',4,6,6'-tetrahydroxy-diphenyl methane extracted from euphorbia fischeriana. An extracting process is that petroleum ether, ethyl acetate and n-butyl alcohol are adopted to extract euphorbia fischeriana medicinal material powder, and then the parts are separated through a silica-gel column chromatography method. The preparation method is simple, quick, convenient, good in reproducibility and high in extracting purity. In the obtained compound, the diphenylmethane compound has the good effect of resisting breast cancer cell activity, and 2,4-dihydroxyl-6-methoxy-3-methyl-1-acetophenone has no obvious effect of resisting breast cancer cell activity. Thus it can be seen that the compound provided with a diphenylmethane mother nucleus can remarkably inhibit the breast cancer cell activity, and the type of compound has certain structure-function relationship.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically screens out active ingredients of anti-breast cancer cells from natural products. Background technique [0002] Breast cancer is one of the most common malignant tumors in women, and its high morbidity and rising mortality have always been a disease of global concern. According to the 2011 global cancer statistics report, the number of new cases of breast cancer in the world reached 1.384 million in 2008, accounting for 23.0% of the total number of new cases of malignant tumors, while the number of deaths was as high as 459,000. The age-standardized incidence rate of world population in some more developed countries It is 66.4 / 100,000, while it is 27.3 / 100,000 in developing countries. The incidence of female breast cancer in China ranks first in the incidence of female cancer, and its mortality rate ranks sixth in female cancer mortality. Since the current incidence of breast ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C45/78C07C49/84A61K31/12A61P35/00
CPCC07C45/78C07C49/84
Inventor 赵亮朱利君李洋曹青青李云青张国庆吕磊葛继云钱勇
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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