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Tubulin depolymerizing agent polypeptides and application thereof

A tubulin and depolymerizing agent technology is applied to the tubulin depolymerizing agent polypeptide and its application field, which can solve the problems of lack of specificity of small molecule depolymerizing agents, and achieve the effect of increasing the survival rate and improving the survival rate.

Active Publication Date: 2013-08-21
NANTONG GUANGTAI BIOCHEM PROD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Many successful small-molecule depolymerization agents can inhibit the activity of tubulin at the nanomolar level, but small-molecule depolymerization agents lack specificity. If long-term use of tubulin depolymerization agents lacking specificity in chronic diseases may cause produce major side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Effect of the tubulin depolymerizer polypeptide 4 on tubulin polymerization and depolymerization in vitro.

[0018] Take fresh bovine brain tissue, peel off the meninges and large blood vessels, cut into pieces, wash 1-2 times with cold MES buffer, add MES buffer at a ratio of 0.5-1ml per gram of brain tissue, at 4°C, use electric Homogenize with a homogenizer; centrifuge at 105,000 g for 1 hour at 4°C, take the supernatant, add an equal volume of microtube polymerization buffer, and incubate in a water bath at 37°C for 30 minutes. Centrifuge at 105,000g at 26°C for 1 hour, take the precipitate, add about 1 / 10 of the homogenate volume of cold MES buffer, stir gently or crush the precipitate with a homogenizer; place the suspension in an ice bath for 30 minutes to dissolve the precipitate completely. Protein content was determined by Lowry's method (SDS polyamide gel electrophoresis). Tubulin was diluted to 4-5mg / ml with MES buffer and stored in liquid nitrogen. Take t...

Embodiment 2

[0022] IC50 of tubulin depolymerizer polypeptide 4 on the growth and survival of tumor cells cultured in vitro.

[0023] The MTT colorimetric method was used. The logarithmic growth of U937 cells was added to a 96-well culture plate at 1.0×105, and cultured for 24 hours. Different concentrations of the experimental drug tubulin depolymerizer polypeptide 4 and the positive control drug Changchunxin were added to the experimental wells and positive drug control wells, respectively. base; add the same volume of solvent to the blank group. 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 place at 620nm in a microplate reader Measure the absorbance A value, according to the formula tumor cell growth inhibition rate=(1-absorbance value of the experimental group / absorbance value of the control group)×100%. The calculated IC50 of the test drug was ...

Embodiment 3

[0025] In vivo activity of tubulin depolymerizer polypeptide 4 was tested in a tumor model.

[0026] The U937 tumor model was established, and the positive control drug vincristine was added; the same volume of solvent was added to the blank group, and three doses were set in the experimental group: 0.75, 1.5 μM, and 3 μM mg / Kg. After 21 days, the number of surviving mice was observed, and the survival rate was calculated. The results showed that the tubulin depolymerizing agent polypeptide 4 could effectively protect mice and improve the survival rate of tumor-bearing mice, with the survival rate reaching 65.1%.

[0027]

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Abstract

The invention relates to tubulin depolymerizing agent polypeptides and application thereof, particularly polypeptides capable of inhibiting polymerization of tubulin and treating acute lymphatic leukemia, belonging to the field of medicine. The sequence is VELSQHYLTHR which is a brand-new sequence. The polypeptides can inhibit polymerization of tubulin in vitro on the 1 micromole level and enhance the survival rate of tumor bearing mice in an in-vivo test, thereby having potential new drug development value.

Description

technical field [0001] The present invention relates to tubulin depolymerizing agent polypeptide 4 and its application, in particular to a polypeptide capable of inhibiting tubulin polymerization and treating acute lymphocytic leukemia. Background technique [0002] Acute lymphoblastic leukemia (ALL) is a progressive malignant disease characterized by large numbers of immature white blood cells that resemble lymphoblasts. These cells can be found in the blood, bone marrow, lymph nodes, spleen and other organs. Acute lymphoblastic leukemia accounts for 80% of acute leukemia in children, and the peak incidence is between 3 and 7 years old. ALL can also occur in adults and accounts for 20% of all adult leukemias. In recent years, with the deepening of medical research, great progress has been made in the understanding and treatment of acute lymphoblastic leukemia. Among them, tubulin plays an important role in acute lymphoblastic leukemia. [0003] Microtubules are the main...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/06A61K38/08A61P35/02
Inventor 罗瑞雪
Owner NANTONG GUANGTAI BIOCHEM PROD
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