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Preparation method and application of diphenylmethane compound

A technology of diphenylmethane and compound, which is applied in the field of screening out active components against breast cancer cells, can solve the problems of undiscovered pharmacological activity research reports, etc., and achieve enhanced ability of anti-breast cancer cell activity, good reproducibility, and easy operation. simple effect

Inactive Publication Date: 2017-04-26
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • 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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  • Preparation method and application of diphenylmethane compound
  • Preparation method and application of diphenylmethane compound
  • Preparation method and application of diphenylmethane compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Method for preparing monomer compound from Euphorbia chamaejasme

[0034] 30 kg of dried Euphorbia chamaejasme medicinal materials were crushed and soaked in 80% (ethanol: water 80:20) ethanol for reflux extraction twice for 2 hours each time, and the solvent dosage was 180L and 150L respectively. Combine the extracts, filter while hot, combine and concentrate until no ethanol remains, and concentrate the volume to 8L. Dilute 2L of the concentrated solution with 1L of water, and extract 3 times with petroleum ether, ethyl acetate and n-butanol in turn. Each extraction solvent is 3L. The solvent is recovered under reduced pressure to obtain 60g of petroleum ether and 160g of ethyl acetate. , 20g of n-butanol.

[0035] 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.

[0036] Take 12gFr.2 and pass it through a normal phase column, ...

Embodiment 2

[0058] Example 2: In vitro anti-breast cancer cell experiment

[0059] The MTT method was used to evaluate cytotoxicity, and six types of breast cancer cells were selected for research. They were triple-negative breast cancer MDA-MB-231, Sum149, LuminalA type MCF-7, LuminalB type ZR-75-1, Her 2 positive type SKBr3, BT474. Paclitaxel is the positive control drug. Adjust the density of the above 6 types of breast cancer cells to 5×10 4 Pcs / ml, inoculate into 96-well culture plate, inoculate 100μL cell suspension per well, place at 37℃, 5% CO 2 Cultivate overnight in an incubator. After observing that the cells adhere to the wall and grow well, set up a positive control group, a tumor cell control group and an experimental group of different concentrations of drugs. The experimental group was added with 8 sample solutions of gradient concentration, the concentration of the mother solution of compound 1 and 2 was 5mM, the concentration of paclitaxel mother solution was 3.5mM, and th...

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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 field of medical technology, and specifically is to screen out active ingredients against breast cancer cells from natural products. Background technique [0002] Breast cancer is one of the most common malignant tumors in women, and its high incidence and rising mortality have always been a disease of global concern. According to the 2011 Global Cancer Statistics Report, in 2008, the number of new cases of breast cancer worldwide reached 1.384 million, 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 the world population in some more developed countries It is 66.4 per 100,000, while that of developing countries is 27.3 per 100,000. The domestic female breast cancer incidence rate occupies the first place in the female cancer incidence rate, and the mortality rate occupies the sixth place in the female cancer mort...

Claims

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Application Information

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Patent Type & Authority Applications(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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