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Diphenylether compound, its preparation and use

A technology for compounds and uses, applied in the fields of diphenyl ether compounds and their preparation and use, can solve unseen problems and the like

Inactive Publication Date: 2007-01-17
OCEAN UNIV OF CHINA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The present inventor found that the crude extract of Aspergillus sp.B-F-2 (Aspergillus sp.B-F-2) liquid fermentation product after ultrasonic crushing has good tumor cell proliferation inhibitory activity, then its active components were studied and found The new diphenyl ether compounds have anti-tumor activity, and there are no reports on the chemical structure, cell cycle inhibition, cell proliferation inhibition, and apoptosis-inducing activity of the compound, so there is no relevant information on the market. drug

Method used

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  • Diphenylether compound, its preparation and use
  • Diphenylether compound, its preparation and use
  • Diphenylether compound, its preparation and use

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Fermentative production and separation and purification of embodiment 1 compound 1

[0025] 1 Fermentation production

[0026] Fermentation culture of production bacteria: According to the conventional method for culturing microorganisms, take an appropriate amount of Aspergillus sp.B-F-2, inoculate it on the PDA slant medium, and cultivate it in an incubator at 28 degrees Celsius for 4 days.

[0027] Take an appropriate amount of Aspergillus sp.B-F-2 (Aspergillus sp.B-F-2) cultured on a slant for 4 days, and inoculate it into 120mL culture medium [medium composition (g / L): maltose 3.0, yeast extract 3.0, peptone 5.0, glucose 20.0, pH 7.0] in a 500mL Erlenmeyer flask, cultured on a shaker at 28°C and 120 rpm for 48 hours to obtain a seed culture solution of Aspergillus sp.B-F-2. The seed culture solution was respectively inoculated into a 1000 mL Erlenmeyer flask containing 300 ml of production culture solution [substrate composition (g / L): maltose 3.0, yeast extract 3...

Embodiment 2

[0035] The test of embodiment 2 antitumor activity

[0036] 1 Experimental samples and experimental methods

[0037] Preparation of the test sample solution: the test sample is the pure compound 1 isolated and refined in the above-mentioned Example 1. Accurately weigh an appropriate amount of sample and prepare a solution with the required concentration with DMSO for activity testing.

[0038]Cell line and subculture of cells: K562 cell line was used for activity test. All kinds of cells were subcultured in RPMI-1640 medium containing 10% FBS in an incubator with 5% carbon dioxide at 37°C.

[0039] Cell Proliferation Inhibitory Activity Test Method (MTT Method)

[0040] The invention adopts the MTT method to test and evaluate the inhibitory activity of the tested sample on the proliferation of cancer cells. The dehydrogenase in the mitochondria of living cells can metabolize and reduce the yellow bromide 3-(4,5-dimethylthiazole)-2,5-diphenyltetrazolium to blue-purple water...

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Abstract

A diphenyl-ether compound, its production and use are disclosed. The process is carried out by separating from marine sampler to obtain aspergillus-B-F-2(Aspergillus sp.B-F-2) and producing the final product. It can be used as cell periodic inhibitor, cell multiplication inhibitor and antineoplastic preparation.

Description

Technical field: [0001] The present invention relates to the preparation of diphenyl ethers by using Aspergillus sp.B-F-2 (Aspergillus sp.B-F-2), which was preserved in Wuhan China Culture Collection Center on December 16, 2005 (preservation number: CCTCC M 205148) The method of the compound; the present invention also relates to the use of the compound in the preparation of cell cycle inhibitors, cell proliferation inhibitors or antitumor agents. Background technique: [0002] Diphenyl ether compounds are derivatives of salicylic acid. Salicylic acid is the first non-protein endothelin (ET) binding inhibitor discovered so far. These compounds are a common class of fungal metabolites. It is generally believed that such compounds are derived from anthraquinones with the help of sulochrin and grisandienes (such as geodin). There have been some reports in the literature that this type of compound shows many unique biological activities, such as the ability to inhibit angioge...

Claims

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Application Information

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IPC IPC(8): C07C43/257C07C217/78C07C233/00C07C69/00C12P7/00C12P13/00C12P13/02A61K31/075A61K31/13A61K31/16A61K31/215A61P35/00
Inventor 朱天骄刘睿顾谦群朱伟明刘红兵方玉春张亚鹏
Owner OCEAN UNIV OF CHINA
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