A 7-carbonyl staurosporine compound, its preparation method and its application in the preparation of anticancer drugs

A compound and carbonyl star technology, applied in the field of preparation of active compounds from secondary metabolites of actinomycetes, can solve problems such as poor selectivity, and achieve the effects of simple operation, easy cultivation, and easy production expansion

Active Publication Date: 2019-12-03
浙江美新控股有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

STA is a strong PKC inhibitor (IC 50 =2.7nM), mainly acting on various kinases, topoisomerases and cell cycle regulatory factors in the cell signal transduction pathway, but later proved to be a broad-spectrum kinase inhibitor with poor selectivity, so it could not be drugged

Method used

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  • A 7-carbonyl staurosporine compound, its preparation method and its application in the preparation of anticancer drugs
  • A 7-carbonyl staurosporine compound, its preparation method and its application in the preparation of anticancer drugs
  • A 7-carbonyl staurosporine compound, its preparation method and its application in the preparation of anticancer drugs

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Experimental program
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Embodiment

[0050] 1. Seed solution

[0051]The above Streptomyces were inoculated into 500mL Erlenmeyer flasks containing 250mL of liquid medium, each bottle containing 250mL of Gao's No. 1 liquid medium, and cultured in a shaker at 28°C at 180rpm for 3 days to obtain seed liquid.

[0052] 2. Fermentation

[0053] Inoculate the above-mentioned seed liquid into the rice fermentation medium (made by the following weight components: rice 40g, 25% sea salt water 60mL) with the amount of inoculating 8mL per bottle, and stop the fermentation after 60 days of static culture at 28°C.

[0054] 3. Rough extraction

[0055] Soak each bottle of solid fermented product with about 200 mL of EA (ethyl acetate) overnight, filter through three layers of gauze to remove mycelia, collect the filtrate, and concentrate under reduced pressure to obtain a crude extract (oily extract).

[0056] 4. Separation and purification

[0057] The above crude extract was extracted three times with an equal volume of e...

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Abstract

The invention discloses a 7-carbonyl staurosporine compound, and a preparation method and an application thereof. The staurosporine compound provided by the invention has a structural formula as shownin a formula (I) which is described in the specification. The staurosporin compound provided by the invention is prepared through the following steps: subjecting actinomycete to fermentation in a rice solid medium, then carrying out extraction and filtration so as to obtain a crude extract, and carrying out separation and purification. The staurosporin compound provided by the invention has significant antitumor activity, specifically has high activity to prostate cancer, colon cancer, pancreatic cancer and gastric cancer, and can be used for preparation of anticancer drugs.

Description

technical field [0001] The invention relates to the field of active compounds prepared from secondary metabolites of actinomycetes, in particular to a 7-carbonyl staurosporine compound, a preparation method thereof and an application in the preparation of anticancer drugs. Background technique [0002] Staurosporine compounds are a class of natural products with good pharmaceutical and biological activities, among which staurosporine (STA, structural formula as follows (1)) was discovered the earliest. The compound was first obtained by Omura in 1997 as an indolecarbazole alkaloid isolated from soil actinomycetes. X-ray single-crystal diffraction analysis shows that the center is an indolecarbazole ring, the N below the ring is connected with a small molecular sugar, and the upper part is connected with a lactam ring. STA is a strong PKC inhibitor (IC 50 =2.7nM), mainly acting on various kinases, topoisomerases and cell cycle regulatory factors in the cell signal transduct...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D498/22A61P35/00A61P35/02C12P17/18C12R1/465
CPCA61P35/00A61P35/02C07D498/22C12P17/188
Inventor 陈喆马忠俊周晓欣李嘉琦高思之刘美星
Owner 浙江美新控股有限公司
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