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Application of compound s4 in the preparation of anti-cancer medicine

An anti-cancer drug and compound technology, applied in the field of cell biology, can solve the problems of increasing carcinogenesis, increasing loss of heterozygosity, cell life metabolism and signal transduction disorders, etc.

Inactive Publication Date: 2008-01-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chromosome segregation, centriole duplication and segregation are abnormal, which will lead to abnormal number of chromosomes in each cell, neither aneuploidy, increase the chance of heterozygosity loss, loss of tumor suppressor gene or increase in the number of proto-oncogene Disturb cell life metabolism and signal transduction, increase the chance of cancer

Method used

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  • Application of compound s4 in the preparation of anti-cancer medicine
  • Application of compound s4 in the preparation of anti-cancer medicine
  • Application of compound s4 in the preparation of anti-cancer medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 In vitro enzyme activity inhibition experiment

[0024] The E. coli expression system was used to clone, express and purify the human Aurora-B protein kinase (NCBI accession number is NP 004208), which was used for high-throughput screening experiments. Using radioisotope technology, AURORAB phosphorylates the substrate MBP (UPSTATE company, CAT#13-110, lot#27845), and [γ- 33 γ- on P]-ATP 33 P transfer covalently binds to the substrate, phosphorylates its Ser, and produces an isotope-labeled substrate 33 P-MBP. Finally, scintillation fluid is added to detect the activity of the enzyme by counting with a liquid scintillation counter, and the inhibition of the activity by different compounds can be observed to preliminarily evaluate the activity of the compound.

[0025] The results of parallel experiments showed that the compound s4 of the present invention inhibited the Aurora-B protein kinase activity with an IC50 of 632nM.

Embodiment 2

[0026] Embodiment 2 cancer cell inhibition experiment

[0027] According to the standard MTS experiment, the specific parameters are as follows:

[0028] Seed plate: 1000 cells / well

[0029] Compound: s4

[0030] Culture time: 96h

[0031] Processing time after adding medicine: 3h

[0032] Compound concentration gradient: unit: uM

[0033] Repeat experiment: 6 groups

[0034] Data presentation form: mean ± standard deviation

[0035] Cell line: human colon cancer cell line (sw620)

[0036] The results showed that the compound s4 of the present invention inhibited sw620 with an IC50 of about 1 μM. See the table below for details:

[0037] drug

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Abstract

The present invention relates to the field of cell biology, and provides a compound s4 and the application in the preparation of anti-cancer drugs. Cancer becomes a first cause of death, and the substances which can kill the tumor and the growth of the cancer cells also become the hot spot in research in the current biomedical field. The s4 of the present invention can kill or inhibit a variety of tumor cells and cancer cells; at the same time, the compound s4 of the present invention also has the inhibition effect of phosphate kinase Aurora-B. All these probe that the compound s4 of the present invention has the inhibition effect of malignant tumors. The compound s4 of the present invention can be linked with the suitable pharmaceutical acceptable carriers to prepare the anti-cancer drugs, so as to inhibit the continuous growth of the tumors.

Description

technical field [0001] The invention relates to the field of cell biology and provides the application of compound s4 in the preparation of anticancer drugs. Background technique [0002] Tumor is a disease that seriously endangers human health. In recent years, the incidence of tumors has been increasing day by day. At present, more than 6 million people die of cancer every year in the world, and 8 million new cases are diagnosed, and this number is still increasing year by year. Among the 1.3 billion people in my country, there are millions of new cancer patients every year, about 2 million patients waiting for treatment, and about 1.3 million deaths. It is estimated that by the end of 2006, 1.7 million people will die of cancer in my country, and cancer has become the first cause of death. [0003] Malignant tumor, commonly known as cancer, is a mass that grows and spreads without restriction caused by the mutation of organs and tissue cells in the human body. It can d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K9/20A61K9/19A61K9/08A61P35/00
CPCA61K31/122A61P35/00A61P35/04
Inventor 余龙张昊星郎庆宇李佳唐丽莎
Owner FUDAN UNIV
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