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Angiostatin activator polypeptide

An angiostatin and activator technology, applied in the field of polypeptides for the treatment of malignant tumors, to achieve the effect of inhibiting proliferation and improving survival rate

Inactive Publication Date: 2015-11-11
倪勤华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no well-developed angiostatin activator polypeptide available for the treatment of malignant tumors

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0011] Activity of angiostatin activator polypeptides on the hydrolysis of plasminogen in vitro.

[0012] ELISA method was used to detect plasminogen hydrolyzate—angiostatin. With 1ml of 1mg / ml plasmin as substrate, add 2, 4, 8ng of angiostatin activator polypeptide (Shanghai Sangong Synthetic) and positive control drug metalloprotease 10ng respectively in the substrate solution, at 37 ℃, after reacting for 5 minutes, centrifuge, take the supernatant, and use the ELISA method to react the content of angiostatin in the solution. The results show that the angiostatin produced by 2, 4, and 8 ng of angiostatin activator polypeptide and metalloprotease are respectively 24.87, 31.98, 53.98 μM.

Embodiment 2

[0014] IC50 of angiostatin activator polypeptide on the growth and survival of human vascular endothelial cells cultured in vitro.

[0015] The MTT colorimetric method was used. The logarithmic growth of human vascular endothelial cells HUVEC, 1.0 × 10 5 Added to 96-well culture plate, cultured for 24h, experimental wells, positive drug control wells were added different concentrations of experimental drug angiostatin activator polypeptide (Shanghai Sangong Synthetic) and positive control drug paclitaxel; blank group was added the same volume of solvent. Set up five duplicate wells per well, culture for 48h, add MTT to each well at 0h, 2h, 8h, 14h, 20h, 24h, 36h, and 48h respectively, add DMSO after 4h of action, incubate for 30min, and incubate at 620nm in a microplate reader Measure the absorbance A value, according to the formula HUVEC growth inhibition rate=(1-absorbance value of the experimental group / absorbance value of the control group)×100%. The calculated IC50 of t...

Embodiment 3

[0017] The in vivo activity of angiostatin activator polypeptide was detected by tumor model.

[0018] The prostate cancer tumor model was established, and the positive control drug paclitaxel was added; the same volume of solvent was added to the blank group, and three doses of polypeptide (Shanghai Sangong Synthetic) were set in the experimental group: 2, 4, and 8 mg / Kg. After 21 days, the number of surviving mice was observed, and the survival rate was calculated. The results showed that the angiostatin activator polypeptide can effectively protect mice and improve the survival rate of tumor-bearing mice, with the survival rate reaching 81.54%.

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Abstract

The invention relates to the field of medicines and in particular relates to a polypeptide capable of activating angiostain and treating malignant tumour. A sequence of the polypeptide is EALALMYYHSQSLRKTYP is brand-new, and the polypeptide can activate angiostain in vitro and inhibit proliferation of vascular endothelial cells and also can improve survival rate of tumour-bearing mice during in-vivo test, so that the polypeptide has potential value in development of new drugs.

Description

technical field [0001] The invention relates to angiostatin activator polypeptide, in particular to a polypeptide capable of activating angiostatin and treating malignant tumors. Background technique [0002] In 1971, Folkman proposed that tumor growth and metastasis depend on angiogenesis. It is also believed that after the formation of a solid tumor, its development can be divided into two stages: the avascular phase and the vascular phase. In the avascular stage, the existence of tiny tumors depends on the diffuse blood supply of the surrounding interstitium, the growth rate is linear, the tumor is limited within 1mm to 2mm, and the number of tumor cells is less than 10 5 ~10 6 One, forcing the tumor to be in a "dormant state"; after entering the vascular phase, the tumor tissue is perfused with blood supply, and the tumor grows exponentially, and can increase by 16,000 times after 2 weeks. New blood vessels not only provide the nutrients and oxygen needed by the tumor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N9/68A61P35/00
CPCC12N9/50C12Y304/21007
Inventor 倪勤华
Owner 倪勤华
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