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Curvularin derivatives and preparation method and application thereof

A technology of Curvularia and its derivatives, which is applied in the field of Curvularycin derivatives and their preparation, can solve the problems of anti-tumor drugs such as high toxicity and side effects, treatment failure, and drug resistance, and achieve significant inhibitory activity and low product cost. The effect of low cost and short production cycle

Active Publication Date: 2013-12-11
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

On the other hand, due to the toxicity and side effects of existing anticancer drugs and long-term or repeated use, drug resistance is easy to cause treatment failure

Method used

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  • Curvularin derivatives and preparation method and application thereof
  • Curvularin derivatives and preparation method and application thereof
  • Curvularin derivatives and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Fermentative production and separation and purification of compounds 1 and 2:

[0047] 1) Fermentation culture

[0048] Strain culture: According to the conventional culture method of microorganisms, take Penicillium sumatrense preserved in agar-malt extract medium (the bacteria is preserved in the General Microbiology Center of the China Committee for the Collection of Microbial Cultures, and the address of the preservation unit is Beijing No. 3, No. 1 Yard, Beichen West Road, Chaoyang District, preservation date: July 3, 2013, preservation number is CGMCC No.7869) appropriate amount of strains were inoculated on PDA plate medium, and cultured in a 28°C incubator for 4 days. As the bacterial species for the next step of fermentation and cultivation, it is ready for use.

[0049] The Penicillium sumatrense is isolated from the rhizosphere soil of the mangrove plant Prunus in Wenchang, Hainan.

[0050]Cut off the appropriate amount of bacteria on the surface...

Embodiment 2

[0063] Embodiment 2: antitumor activity test

[0064] Select the following 8 test cell lines: mouse melanoma cell line (B16), human liver cancer cell line (Hu-7), human pancreatic cancer cell line (SW1990), human cervical cancer cell line (HeLa), human prostate cancer cell line Anti-tumor activity tests were performed on human non-small cell lung cancer cell line (NCI-H460), human breast cancer cell line (MCF-7) and human gastric cancer cell line (SGC-7901).

[0065] 1) Preparation of experimental samples:

[0066] Preparation of the test sample solution: the test samples were the pure compounds 1 and 2 isolated and obtained in the above examples. Accurately weigh an appropriate amount of sample, and use dimethyl sulfoxide (DMSO) to prepare a solution of the desired concentration for activity testing.

[0067] 2) Tumor cell growth inhibitory activity test (MTT method):

[0068] The present invention uses a tetrazolium salt staining method (MTT method) to test and evaluate t...

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Abstract

The invention relates to microbe medicament technology, and specifically relates to curvularin derivatives and a preparation method and an application thereof. The curvularin derivatives have a chemical structural formula shown as formula I, wherein R1 and R2 are H or R5CO; R3 is H or R6CO; R4 is H, alkyl containing 1-20 carbon atoms or alkoxy; when R1 or R2 is R5CO, R5 is H, linear or branched alkyl containing 1-20 carbon atoms, alkenyl, phenyl, substituted phenyl, or aryl containing hetero atoms; when R3 is R6CO, R6 is H, linear or branched alkyl containing 1-20 carbon atoms, alkenyl, phenyl, substituted phenyl, or aryl containing hetero atoms. The prepared curvularin derivatives are subjected to fermentation production by using microbes, and the preparation method has the characteristics of simple operation technology, short production period and low product cost.

Description

technical field [0001] The invention relates to microbial drug technology, in particular to a curvyin derivative and its preparation method and application. Background technique [0002] Cancer is a chronic disease that seriously endangers human health. According to the statistical report of the "2012 China Cancer Registration Annual Report" released by the National Cancer Registry Center in early 2013, there are about 3.12 million new cancer cases in China every year, and more than 2 million cancer deaths. The incidence and mortality of cancer have continued to rise in recent years. . On the other hand, the existing anti-tumor drugs have severe side effects and long-term or repeated use are prone to drug resistance, resulting in treatment failure. Therefore, the development of new anticancer drugs is urgent. Contents of the invention [0003] The object of the present invention is to provide a curviramycin derivative and its preparation method and application. [0004...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D313/00C12P17/02A61P35/00C12R1/80
Inventor 王斌贵孟令红黄才国吕翠婷李晓明李春顺徐刚明
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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