Polypeptide for inhibiting in vivo pulmonary metastasis in tumor cells and preparation method and application thereof

A tumor cell and lung technology, applied in the field of biopharmaceuticals, can solve problems such as unmet expectations, achieve structural stability, no toxic side effects, and inhibit the formation of lung metastases.

Active Publication Date: 2019-10-08
DALIAN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In any case, these peptide clinical trials have not yet achieved the intended purpose

Method used

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  • Polypeptide for inhibiting in vivo pulmonary metastasis in tumor cells and preparation method and application thereof
  • Polypeptide for inhibiting in vivo pulmonary metastasis in tumor cells and preparation method and application thereof
  • Polypeptide for inhibiting in vivo pulmonary metastasis in tumor cells and preparation method and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 prepares polypeptide of the present invention

[0029] The following 2-CL resins for preparing polypeptides, Fmoc protected amino acids, condensation reagents, and cleavage reagents were all purchased from domestic biochemical reagent companies.

[0030] 1.1 The synthesis of polypeptide resin of the present invention

[0031] Polypeptide resin of the present invention is:

[0032] Lys(Boc)-Lys(Boc)-Lys(Boc)-Lys(Boc)-Asp(otbu)-Lys(Boc)-Ser(tbu)-Ser(tbu)-Phe-Ile-Ala-Val-Leu- Gln(trt)-Thr(tbu)-Ala-Ala-Ala-Ala-Leu-Arg(Pbf)-Met-Gly-Ala-Tyr(tbu)-2-CL resin.

[0033] Using 2-CL resin as the initial carrier, the polypeptide resin of the present invention was prepared by de-Fmoc protection and coupling reaction, followed by coupling with the protected amino acids shown in Table 1. The protected amino acids used in this embodiment correspond to the 1st to 25th amino acids from the resin as shown in the following table:

[0034] Table 1. Protected Amino Acids

[...

Embodiment 2

[0051] Example.2 The effect of the polypeptide of the present invention on lung metastasis of mouse lung cancer LLC tumor cells in vivo

[0052] 20-25 g of syngeneic NCR (purchased from Dalian Medical University Animal Center) mice were divided into control group and treatment group, with 7 mice in each group. The control group was injected with mouse lung cancer LLC tumor cells (ATCC number, CRL1642 via tail vein) TM )0.1mL, about 1.5×10 6 cells (diluted in 0.9% saline); the treatment group was injected with 0.1 mL of mouse lung cancer LLC tumor cells via tail vein, about 1.5×*10 6 (Add the polypeptide of the present invention to a final concentration of 50 μg / mL, the amino acid sequence is: KKKKDKSSFIAVLQTAAAALRMGAY). A mouse model of lung metastasis of lung cancer LLC tumor cells was established. The mice were sacrificed by decapitation 5 weeks after the injection, and the lungs were isolated to observe the formation of lung tumor metastases (the arrows indicate tumor no...

Embodiment 3

[0053] Example.3 Effect of the polypeptide of the present invention on the formation of lung metastases in nude mouse model of human breast cancer MDA-MB-231 cells

[0054] 20-25 grams of BALB / cA-nu / nu mice (purchased from Beijing Zhongke Zesheng Technology Co., Ltd.) were divided into control group and treatment group, 8 mice in each group. The control group was injected with 0.1ml MDA-MB- 231 (ATCC number, HTB-26 TM ) cell suspension (1×10 6 cells, diluted with 0.9% normal saline); the treatment group was simultaneously added with the polypeptide of the present invention to a final concentration of 50 μg / ml. 35 days after the inoculation, the mice were sacrificed by decapitation, the lungs were isolated, and the formation of lung tumor nodules (the arrows indicated tumor nodules) were observed by naked eyes. Macroscopic tumor nodules on the lung surface were considered tumorigenesis positive, and no macroscopic tumor nodules were tumorigenesis negative. The result is as ...

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Abstract

The invention discloses a polypeptide for inhibiting in vivo pulmonary metastasis of tumor cells and a preparation method and application thereof, and belongs to the field of biological pharmacy. Thepolypeptide is composed of 25 amino acids, and an amino acid sequence is SEQ ID No.1. The polypeptide for inhibiting the in vivo pulmonary metastasis in the tumor cells is synthesized by a solid phasechemical synthesis, the yield of high, a technology is stable, and the molecular weight is 2698.08Da. The polypeptide for inhibiting the in vivo pulmonary metastasis in the tumor cells has activity for inhibiting tumor pulmonary metastasis, and is safe and effective for treating tumor. Therefore, the polypeptide for inhibiting the in vivo pulmonary metastasis in the tumor cells has important application value on clinical anti-tumor treatment.

Description

technical field [0001] The invention relates to a polypeptide and its application, in particular to a polypeptide for inhibiting lung metastasis of tumor cells in vivo, its preparation method and application, and belongs to the field of biopharmaceuticals. Background technique [0002] Cancer is one of the diseases that seriously threaten human life and health, and tumor metastasis is the main cause of death in cancer patients. According to clinical data and epidemiological investigation and analysis, when malignant tumors are clinically diagnosed, more than 60% of patients have tumor cells that have spread throughout the body. To some extent, the control of tumor metastasis can control the death caused by tumor. At present, although huge manpower and material resources have been invested in the research on the mechanism of tumor metastasis and anti-metastasis drugs at home and abroad, there is no real anti-metastasis drug in clinical application. The reason is that tumor ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K14/00C07K1/30C07K1/16C07K1/14C07K1/36C07K1/04C07K1/06A61K38/16A61P35/04
CPCA61K38/00A61P35/04C07K14/00Y02P20/55
Inventor 马克里何欣马晓光黄晓华王聪聪李颖
Owner DALIAN MEDICAL UNIVERSITY
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