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Applications of staurosporine compounds

A staurosporine and compound technology, applied in the application field of staurosporine compounds, can solve the problems of poor selectivity and achieve high inhibitory effect and high activity effect

Inactive Publication Date: 2018-01-12
FUYANG KEXING BIOCHEM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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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  • Applications of staurosporine compounds
  • Applications of staurosporine compounds
  • Applications of staurosporine compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] 1. Seed solution

[0038] The above Streptomyces was inoculated into 500mL Erlenmeyer flasks containing 250mL of liquid medium, each bottle containing 250mL of Gaoshi No. 1 liquid medium, and cultured in a shaker at 28°C at 180rpm for 4 days to obtain seed liquid.

[0039] 2. Fermentation

[0040] 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.

[0041] 3. Rough extraction

[0042] Soak each bottle of solid fermented product with about 300 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).

[0043] 4. Separation and purification

[0044] The crude extract was dissolved in 90% methanol water, extracted three tim...

Embodiment 2

[0048](1) Structural identification of compound 1

[0049] White powder (CH 3 OH), with blue-violet fluorescence under ultraviolet light. according to 1 H and 13 C NMR data speculates that its molecular formula is C 29 h 26 N 4 o 4 , 1 H NMR (CD 3 OD, 400MHz): δ H 7.26(1H, d, J=7.8Hz, H-1), 7.49(1H, br t, H-2), 7.39(1H, br t, H-3), 9.43(1H, d, J=7.9Hz , H-4), 5.03 (1H, d, J=14.7Hz, H-7a), 5.04 (1H, d, J=14.7Hz, H-7b), 7.93 (1H, d, J=7.8Hz, H -8), 7.36 (1H, br t, H-9), 7.50 (1H, br t, H-10), 7.76 (1H, d, J=7.9Hz, H-11), 4.02 (1H, d, J=2.0Hz, H-3'), 5.02(1H, m, H-4'), 2.52(1H, d, J=4.4Hz, H-5'a), 2.68(1H, m, H-5 'b), 6.75 (1H, dd, J=6.2&7.1Hz, H-6'), 2.52 (3H, s, H-2'-CH 3 ), 3.42 (3H, s, H-3'-OCH 3 ), 2.86 (3H, s, H-N-CH 3 ), 8.14(1H, s, H-1"), 13 C NMR (CD 3 OD, 100MHz): δ C 107.8(C-1), 125.6(C-2), 120.4(C-3), 126.8(C-4), 123.6(C-4a), 116.5(C-4b), 119.0(C-4c), 173.3 (C-5), 46.2(C-7), 132.6(C-7a), 114.7(C-7b), 124.7(C-7c), 121.7(C-8), 120.8(C-9), 125.2( C-1...

Embodiment 3

[0059] Proliferation inhibition experiment of human prostate cancer cell line PC3.

[0060] Cells in the logarithmic growth phase were taken and configured as 5×10 4 cells / mL, spread in 96-well culture plate at 100 μL / well, CO 2 Cultivate in the incubator for 24 hours, take out the culture plate, add different concentrations of samples to be tested in each well, set 3 duplicate holes for each concentration, and place in CO 2After continuing to cultivate in the incubator for 72 hours, take out the culture plate, discard the culture medium, add 100 μL of 10% trichloroacetic acid (TCA) pre-cooled in a refrigerator at 4°C to each well to fix it, let it stand for 5 minutes, and then move the culture plate to 4 °C refrigerator overnight. Pour off the fixative, wash each well 5 times with deionized water, spin dry, and air dry. Add 70 μL of SRB solution to each well, place at room temperature for 20 minutes, remove the supernatant, wash 5 times with 1% acetic acid, and air dry. T...

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Abstract

The invention discloses applications of staurosporine compounds in preparing medicines for treating cancer, inflammation or AIDS. The compounds are obtained through separation and purification from actinomycetes, and are identified to be staurosporine compounds. The functional research shows that the compounds have relatively high activity for prostate cancer cells, and also have a relatively highinhibiting effect for Brd4 protein, and therefore, the compounds have good application prospects in preparing the medicines for treating tumor, HIV, leukemia and other diseases.

Description

technical field [0001] The invention relates to the field of biotechnology, in particular to the application of a staurosporine compound. Background technique [0002] Cancer is one of the major diseases that endanger human life and health, and has the characteristics of long disease course and high mortality. Prostate cancer is a malignant tumor commonly found in the male genitourinary system. Its incidence rate is the first among all male tumors in Western Europe and the United States, and its mortality rate is second only to lung cancer. Compared with western countries, the incidence of prostate cancer in my country is significantly lower, but in recent years due to the influence of various factors, it has shown a significant increase. The World Health Organization reported that in 2012, the number of cancer patients and deaths in the world continued to increase. Nearly half of the new cancer cases occurred in Asia, most of which were in China, and China ranked first in ...

Claims

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Application Information

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IPC IPC(8): A61K31/553A61P35/00A61P29/00A61P31/18A61P19/02A61P17/00C07D498/22
Inventor 马忠俊周彪丁婉婧刘美星
Owner FUYANG KEXING BIOCHEM
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