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Staurosporine compound as well as preparation method and application thereof

A technology of staurosporine and compounds, applied in the field of staurosporine compounds and their preparation, to achieve good anti-tumor activity and good BRD4 inhibitory activity

Inactive Publication Date: 2017-11-07
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, few reports of such compounds have BRD4 inhibitory activity

Method used

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  • Staurosporine compound as well as preparation method and application thereof
  • Staurosporine compound as well as preparation method and application thereof
  • Staurosporine compound as well as preparation method and application thereof

Examples

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Embodiment 1

[0025] 1. Fermentation of compounds

[0026] The marine actinomycete adopts the streptomyces Streptomycessp.CICC 11021 sold by China Industrial Microorganism Culture Collection Management Center;

[0027] 1) Inoculate marine actinomyces Streptomyces sp.CICC 11021 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 fermentable cultivated seed solution;

[0028] 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.

[0029] 2. Compound preparation and identification

[0030] The solid fermentation product containing the compound with antitumor activ...

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Abstract

The invention discloses a staurosporine compound as well as a preparation method and application thereof. The structure of the compound is of formula I shown in the specification. The compound has antitumor activity and BRD4 inhibition activity, can be used for treating cancer diseases such as leukemia, breast cancer and colon cancer related to over cell proliferation or abnormal cell proliferation, and can be also applied to research and development of medicines related to anti-HIV incubation and anti-human papillomatosis viruses (HPV). According to the preparation method, the staurosporine compound is prepared from marine actinomycete via solid fermentation culture, and a fermentation product is extracted with ethyl acetate and is further separated and purified by using gel chromatography and inversed phase chromatography. The preparation method is easy to operate and implement.

Description

technical field [0001] The invention relates to the field of compounds prepared by culture of actinomycetes, in particular to a staurosporine compound and its preparation method and application. Background technique [0002] Staurosporine alkaloid staurosporine (STA) has good antitumor activity, and studies have found that it has inhibitory effects on protein kinase C (PKC), tyrosine kinase, topoisomerase, extracellular regulatory protein kinase, etc. Strong inhibitory effect, especially the inhibitory activity on protein kinase C (PKC) (IC 50 =2.7nM), and its derivatives also exhibit certain antitumor and protein kinase inhibitory activities. However, few reports of such compounds have BRD4 inhibitory activity. [0003] Bromodomain (BRD) is a highly conserved evolutionary functional domain of about 110 amino acids. It can specifically bind to acetylated lysine residues in histones, and can also be widely involved in cell cycle regulation, cell differentiation, signal tra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/23C07H1/00A61P35/00A61P29/00A61P31/18A61P31/20C12P17/18C12R1/465
CPCC07H1/00C07H19/23C12P17/182
Inventor 马忠俊王佳楠丁婉婧
Owner ZHEJIANG UNIV
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