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Dioxygen piperazidine compounds and preparation method and usage thereof

A technology of compound and use, applied in the field of use in the preparation of cell proliferation inhibitors or anti-tumor agents, capable of solving problems such as drugs that have not yet been seen

Inactive Publication Date: 2008-01-30
OCEAN UNIV OF CHINA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that the shown dioxopiperazine compounds have antitumor activity, and there is no report on the antitumor active ingredients of the strain, the chemical structure of the compound and the inhibitory activity of cell proliferation, so there is no report on the market. related drugs

Method used

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  • Dioxygen piperazidine compounds and preparation method and usage thereof
  • Dioxygen piperazidine compounds and preparation method and usage thereof
  • Dioxygen piperazidine compounds and preparation method and usage thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Fermentation production and separation and purification of compounds I and II

[0023] 1 Fermentation production

[0024] Fermentation culture of producing bacteria: According to the conventional method of culturing microorganisms, take an appropriate amount of Aspergillus effuses H1-1 (Aspergillus effuses H1-1) (the deposit number is: CCTCC M 206066), inoculate it on the PDA solid slant medium, and at 28 degrees Celsius Incubator for 4 days.

[0025] Take an appropriate amount of Aspergillus effuses H1-1 (Aspergillus effuses H1-1) cultured on the slant for 4 days, inoculate it with 120 mL of culture medium [medium composition (g / L): maltose 20.0, mannitol 20.0, monosodium glutamate 10.0, KH 2 PO 4 0.5, MgSO 4 ·H 2 O0.3, yeast extract 3.0, corn steep liquor 1, natural pH] in a 500 mL Erlenmeyer flask, cultured in a shaker at 28°C and 120 rpm for 4 days to obtain a seed culture solution of Aspergillus sparse. According to 10% inoculation amount, the seed c...

Embodiment 2

[0039] Example 2 Test of antitumor activity

[0040] 1 Experimental samples and experimental methods

[0041] Preparation of the tested sample solution: The test sample is the pure compound I-II isolated and purified in the above Example 1. Accurately weigh an appropriate amount of sample and prepare a solution of the required concentration with DMSO for the activity test.

[0042]Cell Lines and Subculture of Cells: P388, A-549, HL60 and BEL7402 cell lines were used for viability assays. Various cells were subcultured in RPMI-1640 medium containing 10% FBS at 37°C in an incubator with 5% carbon dioxide.

[0043] 1-1MTT method activity test method

[0044] The present invention adopts the MTT method to test and evaluate the inhibitory activity of the tested samples on the proliferation of P388 and HL60 cancer cells. Dehydrogenase in the mitochondria of living cells can metabolize and reduce yellow 3-(4,5-dimethylthiazole)-2,5-diphenyltetrazolium bromide to blue-purple water...

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Abstract

The invention relates to preparation methods and uses of two dioxypiperazine compounds. The invention adopts aspergillus effuses H1-1 from root mud of Fujian mangrove forest to product novel structural dioxypiperazine compounds. Tests prove that: the compounds can be used as cellular breeding depressant or anti-tumor agent.

Description

Technical field: [0001] The present invention relates to using Aspergillus effuses H1-1 (Aspergillus effuses H1-1) (the strain has been preserved in the China Type Culture Collection Center on July 13, 2006, the preservation number is: CCTCC M 206066) to produce dioxygen Methods for piperazine compounds; the present invention also relates to the use of such compounds in the preparation of cell proliferation inhibitors or antitumor agents. Background technique: [0002] There are many reports about dioxypiperazines in the literature, but no reports on the two new structures of dioxypiperazines. The inventors found out that the crude extract of the liquid fermentation product of Aspergillus effuses H1-1 after ultrasonication has a good lethal activity to sea shrimp, so the active ingredient was studied. Studies have found that the dioxypiperazine compounds shown have anti-tumor activity, and there is no report on the research on the anti-tumor active components of the strain,...

Claims

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Application Information

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IPC IPC(8): C07D403/06A61K31/499A61P35/00C12P17/16C12R1/66C07D209/00C07D241/00
Inventor 顾谦群刘为忠朱伟明朱天骄方玉春
Owner OCEAN UNIV OF CHINA
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