3-O-demethylation-4-N-demethylation-4-N-ethanoyl-staurosporine and preparation method and application thereof

A staurosporine and demethylation technology, applied in the field of actinomycete culture and preparation of compounds, can solve the problems of limited research, poor protein kinase selectivity, etc., and achieve strong cytotoxicity, strong anti-tumor activity, and good protein kinase inhibitory activity Effect

Active Publication Date: 2018-05-25
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to its poor selectivity for p...

Method used

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  • 3-O-demethylation-4-N-demethylation-4-N-ethanoyl-staurosporine and preparation method and application thereof

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Embodiment 1

[0023] 1. Fermentation of compounds

[0024] The actinomycete adopts the streptomyces Streptomycessp.CICC 11026 sold by China Industrial Microorganism Culture Collection Management Center;

[0025] 1) Inoculate Actinomyces Streptomyces sp.CICC 11026 into 500mL Erlenmeyer flasks, each bottle contains 250mL Gaoshi No. 1 liquid medium, and cultivate them in a shaker at 28°C and 180rpm for 3 days to obtain a fermentable culture the seed liquid;

[0026] 2) Inoculate the seed solution obtained in step 1) into rice medium (rice medium, made of the following components: 40g rice, 60mL water, 1.5g sea salt), the inoculation volume is 12mL, and the culture condition is constant temperature at 28°C Static culture for 70 days to obtain a solid fermentation product containing the compound with anti-tumor activity of the present invention.

[0027] 2. Compound preparation and identification

[0028] The solid fermentation product containing the compound with antitumor activity of the pr...

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Abstract

The invention discloses 3-O-demethylation-4-N-demethylation-4-N-ethanoyl-staurosporine and a preparation method and an application thereof. The compound has the antineoplastic activity and the proteinkinase inhibiting effect, and can be used for preparing pharmaceuticals of protein kinase inhibitors and antineoplastic pharmaceuticals. The compound is prepared and obtained from a fermentation product of actinomycetes (Streptomyces sp. CICC 11026) by using a rice fermentation method. The preparation method comprises the following steps: after executing the ethyl acetate extraction to the fermentation product, separating and purifying by using a gel chromatography and a high performance liquid chromatography, to obtain the compound. The preparation method is easy to operate and carry out.

Description

technical field [0001] The present invention relates to the technical field of actinomycetes culture and preparation of compounds, in particular to an anti-tumor active 3-O-desmethyl-4-N-desmethyl-4-N-acetyl staurosporine and its preparation method and application. Background technique [0002] Staurosporine (STA) was an indolecarbazole alkaloid isolated from the culture medium of actinomycetes in soil as early as 1977. Since then, a large number of studies have shown that it has various pharmacological activities such as anti-tumor activity , antibacterial effect, inhibition of platelet aggregation, etc. The most important thing is that it has broad-spectrum protein kinase inhibitory activity, such as protein kinase C (PKC), tyrosine kinase (TPK), cell cycle-dependent kinase proteins, etc. However, due to its poor selectivity for protein kinases, further research on it is limited. The subsequently discovered derivatives exhibit certain anti-tumor and protein kinase inhib...

Claims

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Application Information

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IPC IPC(8): C07D498/22A61P35/00A61P35/02A61P25/28A61P25/14A61P27/02A61P27/06C12P17/18C12R1/04
CPCC07D498/22C12P17/188
Inventor 马忠俊王佳楠丁婉婧陈喆刘美星
Owner 浙江美新控股有限公司
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