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Specific penicillium ketone compounds, process for preparing same and use thereof

A specific penicillone and compound technology, applied in the field of use in the preparation of cell proliferation inhibitors or anti-tumor agents, can solve the problems of no research report on the structure of this type of compound, no research report on the activity of the compound and the like

Inactive Publication Date: 2006-09-27
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The formula I compound specific penicillinone (named as Notatone A in English) discovered by the present inventor is a brand-new skeleton, and there is no structure research report about this type of compound, and there is no activity research report about this type of compound

Method used

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  • Specific penicillium ketone compounds, process for preparing same and use thereof
  • Specific penicillium ketone compounds, process for preparing same and use thereof
  • Specific penicillium ketone compounds, process for preparing same and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Fermentative production and separation and purification of compound specific penicillin (Notatone A)

[0021] 1 Fermentation production

[0022] Fermentation culture of producing bacterium: according to the conventional method of cultivating microorganisms, get Penicillium notatum B-62 (Penicillium notatumB-62), this bacterial strain has been preserved in China Type Culture Collection Center on May 26, 2005 (preservation number is: CCTCCM205047) appropriate amount of fungus, inoculated on the PDA slant medium, and cultivated for 5 days in an incubator at 28 degrees Celsius.

[0023] Get an appropriate amount of Penicillium notatum B-62 (Penicillium notatum B-62) (preservation number is: CCTCCM205047) cultured on the slant for 5 days, and inoculate it into 150mL culture medium [the medium composition (%) is: NaCl 12%, KCl 1 %, MgSO 4 1%, 1% monosodium glutamate, 0.1% corn steep liquor, 2% mannitol, 2% maltose, 1% glucose, 0.3% yeast extract, pH=7.0] in a 500...

Embodiment 2

[0029] Example 2 Test of antitumor activity

[0030] 1 Experimental samples and experimental methods

[0031] Preparation of the tested sample solution: the test sample is the pure product compound notatone (Notatone A) isolated and refined in the above-mentioned embodiment 1, an appropriate amount of sample is accurately weighed, and a solution of the required concentration is prepared with methanol for activity testing.

[0032] Subculture of cell lines and cells: P388, HL60, BEL-7402 and A549 cell lines were used for activity testing, and all kinds of cells were cultured in RPMI-1640 medium containing 10% FBS at 37°C with 5% carbon dioxide Subculture in box.

[0033] Cell Proliferation Inhibitory Activity Test Method (MTT Method)

[0034] 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 3-(4,...

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Abstract

The invention relates to a group of Notatone A compounds, method for preparation and use thereof, which is prepared from Penicillium notatum B-62 fungus isolated from Qinghai lake mud samples and has novel structure, experiment has proved that the compounds can be used as cell propagation depressant and antineoplastic agent.

Description

Technical field: [0001] The invention relates to a method for preparing specific penicillone compounds by using Penicillium notatum B-62 (Penicillium notatum B-62) (preservation number: CCTCCM205047); use in pharmaceuticals. Background technique: [0002] The specific penicillinone (notatone A), a compound of formula I discovered by the present inventors, is a brand-new skeleton, and there is no report on the structure or activity of this type of compound. Invention content: [0003] The present invention aims to provide a new skeleton compound with unique structure and anti-tumor activities such as inhibiting cell proliferation and directly killing cancer cells. [0004] The purpose of the present invention is also to provide a preparation method of a new compound and its use in the preparation of tumor cell proliferation inhibitors or anti-tumor agents. [0005] The present invention discovers the specific penicillin (Notatone A) compound with a new skeleton from the f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/06C12P17/18C12N1/14A61K31/352A61P35/00
Inventor 朱伟明辛志宏顾谦群方玉春朱天骄刘红兵王文良
Owner OCEAN UNIV OF CHINA
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