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Polypeptide capable of inhibiting matrix metalloproteinase 10 and application of polypeptide

A matrix metal, peptide inhibition technology, applied in the direction of peptide/protein components, peptides, enzymes, etc.

Inactive Publication Date: 2016-04-20
SUZHOU PULUODA BIOLOGICAL SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite this, there are no well-developed matrix metalloproteinase 10 inhibitors available for the treatment of osteoporosis

Method used

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  • Polypeptide capable of inhibiting matrix metalloproteinase 10 and application of polypeptide
  • Polypeptide capable of inhibiting matrix metalloproteinase 10 and application of polypeptide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Chemical Synthesis of Peptides

[0013] The peptides were synthesized using Fmoc chemistry. The synthesis reaction is carried out from the C-terminus to the N-terminus. There are free amino groups on the Rink medium (available from AdvancedChemTech), and the amino acids are connected in the order from the C-terminus to the N-terminus. During each ligation step, the amino acid residues are activated, and the activation mixture contains 4 times as many HBTU, HOBt, DIEA and Fmoc-amino acids as there are free amino groups on the medium. After each amino acid attachment reaction, a pyridine / acetic acid / N-methylimidazole mixture was used to block the unattached free amino groups. After each amino acid linking reaction and before the next amino acid linking, the Fmoc-group on the medium should be removed, and the Fmoc-group should be removed using dimethylformamide containing 20% ​​piperidine. Finally, after all amino acid residues are linked sequentially, the peptide is cle...

Embodiment 2

[0016] The IC50 value of the inhibitory polypeptide against matrix metalloproteinase 10 in vitro.

[0017] The enzyme activity of recombinant human matrix metalloproteinase 10 is detected by cleaving the fluorescently produced polypeptide substrate Mca-Arg-Pro-Lys-Pro-Val-Glu-Nval-Trp-Arg-Lys(Dnp)-NH 2 And detect the generated fluorescence value (excitation wavelength=328nm, detection wavelength=392nm). All assays were performed in 100 μl reactions at 37°C. The concentration of matrix metalloproteinase 10 during activation was 100 ng / μl (1 μM). At the beginning of the reaction, 10 μl of matrix metalloproteinase-10 storage solution (1 ng / μl) was added to the reaction system, and the final concentration of the substrate was 10 μM. The IC50 value of the matrix metalloproteinase 10 inhibitory polypeptide of Example 1 was 11.81 μmol.

Embodiment 3

[0019] Inhibiting the EC50 of polypeptides on the growth of human osteoblasts in vitro.

[0020] The MTT colorimetric method was used. Human osteoblasts growing logarithmically, at 1.0×10 5 Add it into a 96-well culture plate and culture it for 24 hours. Add different concentrations of the experimental drug Example 1 polypeptide (Shanghai Jier Synthetic) to the experimental wells; add the same volume of solvent to the blank group. Set up five duplicate wells in each hole, after culturing for 48 hours, add MTT to each hole, after acting for 4 hours, add DMSO, incubate for 30 minutes, measure absorbance A value at 620nm place of microplate reader, according to the formula osteoblast proliferation rate=(1-experiment Absorbance value of group / absorbance value of control group)×100%. The calculated EC50 of the polypeptide of Example 1 was 4.31 μM.

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Abstract

The invention relates to the field of medicine, in particular to a polypeptide capable of inhibiting matrix metalloproteinase 10 and relieving osteoporosis. The sequence of the polypeptide is EEVTPLTFSRLYEGEADIMISFAVKE, and is a brand-new sequence. The polypeptide can inhibit the activity of matrix metalloproteinase 10 in vitro, can relieve bone mineral density decrease of a model animal of osteoporosis in an in-vivo test, and has a potential new drug development value.

Description

technical field [0001] The invention relates to matrix metalloproteinase 10 inhibitory polypeptide, in particular to a polypeptide capable of inhibiting matrix metalloproteinase 10 and reducing osteoporosis. Background technique [0002] Osteoporosis, or osteoporosis, is a group of bone diseases caused by a variety of reasons. Bone tissue has normal calcification, and the ratio of calcium salt to matrix is ​​normal. It is characterized by a decrease in the amount of bone tissue per unit volume. bone lesions. In most cases of osteoporosis, the loss of bone tissue is mainly due to increased bone resorption. Characterized by bone pain and susceptibility to fractures. [0003] At present, drugs used to treat and prevent the development of osteoporosis are divided into two categories. The first category is drugs that inhibit bone resorption, including calcium, vitamin D and active vitamin D, calcitonin, bisphosphonates, and estrogen. and isoflavones; the second category is bon...

Claims

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Application Information

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IPC IPC(8): C07K14/00A61K38/16A61P19/10
CPCA61K38/00C07K14/001C12N9/6491C12Y304/24022
Inventor 罗瑞雪
Owner SUZHOU PULUODA BIOLOGICAL SCI & TECH
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