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Staurosporine aldehyde substituted derivative as well as preparation method and application thereof

A technology of staurosporine aldehyde and derivatives, applied in the field of staurosporine aldehyde substituted derivatives and its preparation, can solve the problems of high toxicity, no specificity of Staurosporine, and influence on normal cell proliferation and division, and achieve experimental operation Simple, easy to expand production, and good application prospects

Active Publication Date: 2017-12-01
浙江美新控股有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have found that Staurosporine has no specificity, and while it acts on tumor cells, it also affects the proliferation and division of normal cells. It is too toxic for clinical development and application, so it cannot be made into a drug.

Method used

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  • Staurosporine aldehyde substituted derivative as well as preparation method and application thereof
  • Staurosporine aldehyde substituted derivative as well as preparation method and application thereof
  • Staurosporine aldehyde substituted derivative as well as preparation method and application thereof

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Embodiment 1

[0025] 1. Fermentation of compounds

[0026] Marine actinomycetes use Streptomycessp.CICC 11027 sold by China Common Microbial Species Collection and Management Center;

[0027] 1) Inoculate marine actinomycetes in a 500mL Erlenmeyer flask, each flask containing 250mL Gao's No. 1 liquid medium, culture condition is 28 ℃, 180rpm shaker for 3 days to obtain seed liquid that can be used for fermentation culture ;

[0028] 2) Inoculate the seed liquid obtained in step 1) into rice culture medium (rice culture medium, made of the following components: 40g of rice mass; 60mL of seawater, placed in a 500ml Erlenmeyer flask and sterilized by autoclaving), inoculate The volume is 12 mL, and the solid fermentation product containing the compound with anti-tumor activity of the present invention is obtained by static culture at 28° C. for 120 days.

[0029] 2. Preparation of the compound

[0030] The solid fermentation product containing the compound with anti-tumor activity of the present inven...

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Abstract

The invention discloses a Staurosporine aldehyde substituted derivative as well as a preparation method and application thereof. The compound, namely the Staurosporine aldehyde substituted derivative, has structures represented by a formula I and a formula II. The compound provided by the invention can be used for treating cancers such as acute and chronic leukemia, lymph cancer, breast cancer, lung cancer as well as diseases such as AIDS, coronary heart disease, diabetes mellitus and senile dementia which are relevant with protein kinase inhibition. The preparation method comprises the steps of carrying out fermentation by virtue of a marine actinomycete rice solid culture medium, carrying out extraction by virtue of ethyl acetate, carrying out gel column chromatography and high performance liquid chromatography and separation on the obtained ferment, so as to obtain the Staurosporine aldehyde substituted derivative. The preparation method is easy in operation and implementation.

Description

Technical field [0001] The invention relates to the field of preparing active compounds by culturing marine actinomycetes, in particular to a staurosporine aldehyde group substituted derivative, and a preparation method and application thereof. Background technique [0002] In recent years, the inhibitory activity of indolocarbazole compound Staurosporine and its derivatives on tumor-related enzymes has been extensively studied. Such compounds have good inhibitory effects on protein kinase C (PKC), cyclin-dependent kinases, topoisomerases, checkpoint kinases, etc., and can inhibit tumor cell proliferation, so they can be used for tumor treatment. The main mechanism of action is as follows: Staurosporine prevents the binding of ATP and protein kinase under physiological conditions by interacting and binding with protein kinase, so it has the ability to inhibit the activity of the enzyme and affect the normal process of the cell cycle. However, studies have found that Staurosporin...

Claims

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Application Information

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IPC IPC(8): C07H9/06C07H1/06C12P19/26A61P35/02A61P35/00A61P31/18A61P9/10A61P3/10A61P25/28
CPCC07H1/06C07H9/06C12P19/26
Inventor 马忠俊秦乐乐丁婉婧陈喆刘美星
Owner 浙江美新控股有限公司
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