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Antitumor use of antisense thionucleotide

An antisense thionucleotide and tumor technology, applied in the anti-tumor application field of antisense thionucleotide, can solve the problem of not obtaining the dosage of drugs, etc., and achieve high toxic and side effects, small toxic and negative effects, and large impact Effect

Inactive Publication Date: 2007-11-07
SHANGHAI KAIMU BIOMEDICINE SCI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, it has not been compared with the existing antisense drugs, showing that this kind of antisense nucleotides can inhibit the expression of the oncogene bcl-2 in the human lung cancer cell line cultured in vitro, and the occurrence of cell apoptosis and the antisense effect in the nude mouse animal model. Tumor activity, and no specific drug dosage, etc., as key technical characteristics of anti-tumor drugs

Method used

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  • Antitumor use of antisense thionucleotide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] KS0604 inhibits the expression of Bcl-2 gene in the human lung cancer cell line NCI-H446 cultured in vitro.

[0057] The same type of drug G3139 from Genta Company was used as a positive control, and the mismatched sequence (TM) was used as a negative control, and the effect of KS0604 was detected by reverse transcription PCR. The level of bcl-2 mRNA in the human tumor cell line NCI-H446 after 48 hours of transfection is shown in FIG. 2 .

[0058] Also using G3139 and TM as controls, Western blot method was used to detect drug-induced down-regulation of NCI-H446Bcl-2 protein. See Figure 3.

[0059] It can be seen from the above results that:

[0060] ①In the RT-PCR experiment, there was no significant difference in the mRNA level of Actin among the groups, while the G3139 and KS0604 treatment groups both showed a significant down-regulation of the bcl-2 mRNA level, and the mismatched sequence had no such effect. Although a linear comparison could not be made as a res...

Embodiment 2

[0067] KS0604 induces apoptosis of human lung cancer cell NCI-H446 cultured in vitro.

[0068] 400nM KS0604 acted on NCI-H446 cells for 48h, G3139 was used as a positive control, and TM sequence was used as a negative control. The ratio of apoptotic cells was detected by the Annexin V / PI double-staining flow cytometry method, and the results are shown in Table 4.

[0069] 48h early apoptosis (%)

48h late apoptosis (%)

Total apoptosis rate (%)

blank control

4.67

0.21

4.87

tm

5.04

0.42

5.46

G3139

6.02

0.66

6.68

KS0604

10.38

1.20

11.58

[0070] The results showed that 400nM KS0604 induced apoptosis in some NCI-H446 cells for 48 hours, 10.38% of the cells in the early stage of apoptosis, and 1.20% of the cells in the late stage of apoptosis. Considering that the ability of cells to adhere to the wall decreases in the late stage of apoptosis, and it is ea...

Embodiment 3

[0074] KS0604 effectively inhibits tumor growth in animal models of lung cancer.

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Abstract

The present invention relates to one kind of medicine composition including antisense thionucleotide 5'-CTC CCA GCG TGC GCC ATC-3' in the clinical dosage of 5-20 mg / kg and pharmaceutically acceptable carrier. In extracorporeal cultured human lung cancer cell line, the antisense thionucleotide with Bcl-2 protein mRNA as target point can inhibit the expression of the cancer causing gene bcl-2 effectively and specifically and make the cancer cell die in obvious early apoptosis effect. The animal model test shows that the antisense thionucleotide can inhibit the growth of tumor in human lung cancer induced nude mice obviously, with the inhibition rate in 20 mg / kg dosage reaching 90 %. The antisense thionucleotide and its medicine composition are suitable for use in preparing antitumor medicine.

Description

technical field [0001] The invention belongs to the field of biotechnology, in particular to an anti-tumor application of an antisense thionucleotide. Background technique [0002] Cancer is the number one disease that threatens human life, and about 7 million people die of cancer worldwide every year. With the aging of the world population and the deterioration of the human living environment, the incidence of cancer is increasing year by year, which brings great suffering to patients and a heavy burden on the whole society. [0003] It is generally believed that tumorigenesis is a process promoted by multiple factors, including genetic factors, infection factors, physical and chemical factors, and gene mutations. The means used for cancer treatment are still surgery, radiotherapy and chemotherapy. At present, there are more than 80 commonly used anti-tumor drugs in clinical practice, which can be roughly divided into the following categories according to the molecular ta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K48/00A61K31/7052A61P35/00A61P11/00
Inventor 崔雅迪翟培彬陈仁海陈希中林英略王巍黄旭华
Owner SHANGHAI KAIMU BIOMEDICINE SCI TECH
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