Novel staurosporine analogue and preparation method and applications thereof

A technology of staurosporine and analogues, which is applied in the field of a novel class of staurosporine analogues and their preparation and application, and can solve problems such as drugs that have not yet been seen

Inactive Publication Date: 2011-01-19
INST OF TROPICAL BIOSCI & BIOTECH CHINESE ACADEMY OF TROPICAL AGRI SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there has not been any report on the chemical structure and cell proliferation inhibitory activity of these two compounds, so there is no related drug on the market

Method used

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  • Novel staurosporine analogue and preparation method and applications thereof
  • Novel staurosporine analogue and preparation method and applications thereof
  • Novel staurosporine analogue and preparation method and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] [Example 1] Fermentative production and separation and purification of compounds 1 and 2

[0052] 1 Fermentation production

[0053] According to the conventional method for cultivating microorganisms, take an appropriate amount of Streptomyces sp.FMA (CCTCC M 2010021), and inoculate it into 20 mL of seed medium (the medium consists of 0.2% soluble starch, 1.5% soybean powder, 0.5% yeast extract powder, CaCO 3 0.4%, peptone 0.2%, NaCl 0.4%, pH 7.2-7.4, prepared by artificial seawater) in a 30mm×200mm test tube, carry out seed culture on a rotary shaker (28°C, 200rpm, tilt 45°); after one week, take The seed culture was inoculated into a plurality of 1000 mL Erlenmeyer flasks containing 200 mL of fermentation medium (composition of the medium as above) at a 5% inoculum size, and fermented under the same conditions as the seed culture. The shaker was cultivated for 7 days, and a total of about 100 L of fermentation liquid was obtained.

[0054] 2 Obtaining the extract ...

Embodiment 2

[0063] [Example 2] Test of cell growth inhibitory activity

[0064] 1 test method

[0065] Preparation of the test sample solution: the test samples are the monomer compounds 1 and 2 synthesized 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.

[0066] Cell lines and subculture of cells: HL-60 and A549 cell lines were used for activity testing. All kinds of cells were subcultured in RPMI-1640 medium containing 10% FBS in an incubator with 5% carbon dioxide at 37°C.

[0067] Cell Proliferation Inhibitory Activity Test Method

[0068] The invention uses the SRB method to test and evaluate the inhibitory activity of the tested samples on the proliferation of A549 and HL-60 cancer cells. SRB is a protein-binding dye that can bind to basic amino acids in biological macromolecules. The OD reading of the combined product at a wavelength of 515nm has a good line...

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PUM

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Abstract

The invention relates to a novel staurosporine analogue and a preparation method and applications thereof, wherein two staurosporine analogue molecules with a novel structure is prepared from the Streptomyces Sp.FMA which is separated from the soil sample of the Sanya Mangrove in Hainan Island of China and has the strain preservation number of CCTCC M 2010021. The in vitro cytotoxicity test proves that the compound has cytotoxicity to leukemia cell HL-60 and lung cancer cell A549 and can be used as the cell antiblastic.

Description

Technical field: [0001] The present invention relates to a class of novel staurosporine (Staurosporine) analogues, their preparation method and application. The present invention uses Streptomyces sp. FMA isolated from the soil samples of Sanya mangrove forest in Hainan, China, to produce the above-mentioned compounds with novel structures. The in vitro cytotoxicity test proves that these compounds have cytotoxicity to leukemia cells HL-60 and lung cancer cells A549, and can be used as cell proliferation inhibitors. Background technique: [0002] Cancer is one of the major diseases that endanger human health today and seriously threatens human life. The World Health Organization reports that the number of deaths due to cancer accounted for nearly 12% of the total death toll in 1996, and the proportion of malignant tumors in the cause of death has risen from 12.6% to 17.9% in the past 20 years (Janos B., Bioactive microbial metabolites, J.Antibiot . 2005, 58(1): 1-26). In ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D491/22C12P17/18A61K31/5517A61P35/00C12R1/465
Inventor 洪葵朱伟明杨春丽隋金蕾林海鹏徐小雄王乂
Owner INST OF TROPICAL BIOSCI & BIOTECH CHINESE ACADEMY OF TROPICAL AGRI SCI
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