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Zwitterionic polypeptide, derivatives thereof and nano-drug based on zwitterionic polypeptide and derivatives thereof

A technology of zwitterions and nano-drugs, which is applied in drug combinations, peptide preparation methods, peptides, etc., can solve the problems of unclear biological functions of the hydrophobic core of albumin molecules, interference with small-molecule drug loading capacity, etc., and achieve excellent intracellular The effects of chemicalization and entry into the nucleus, excellent blood compatibility, and accelerated release

Active Publication Date: 2020-08-21
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the albumin retained in the tumor can still have a high distribution in organs such as liver and kidney due to its small molecular weight, and the biological function of the hydrophobic core of the albumin molecule is unknown, and it will interfere with the loading capacity of small molecule drugs

Method used

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  • Zwitterionic polypeptide, derivatives thereof and nano-drug based on zwitterionic polypeptide and derivatives thereof
  • Zwitterionic polypeptide, derivatives thereof and nano-drug based on zwitterionic polypeptide and derivatives thereof
  • Zwitterionic polypeptide, derivatives thereof and nano-drug based on zwitterionic polypeptide and derivatives thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0090] Example 1: Preparation of doxorubicin-loaded nanomedicine based on glutamic acid lysine dimer (EK) and cysteine ​​(C) (EK-C)

[0091] (1) Synthesis of thiol-activated EK-C polypeptide backbone

[0092] Referring to the synthetic route (1), weigh the EK dimer (2mmol) protected by 1g side chain benzyloxycarbonyl (Z) and the cysteine ​​(H-Cys(Trt) protected by 0.2422g mercaptotrityl group respectively). -OH) (0.667 mmol) was added to a 50 mL round bottom flask, followed by 4 mL of anhydrous DMF solution. Then weigh 0.69g 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC·HCl) (3.6mmol), 0.4865g anhydrous N-hydroxybenzotriazole (HOBt ) (3.6mmol) and 0.9306g N,N-diisopropylethylamine (DIEA) solution (7.2mmol) were added to the above-mentioned round bottom flask, sonicated until completely dissolved, then sealed with a parafilm and stirred for 48h. By changing the amount of H-Cys(Trt)-OH, the mixed polypeptide products with EK and C molar ratios of 2:1, 3:1 and...

Embodiment 2

[0106] Example 2: Preparation of doxorubicin-loaded nanomedicine based on glutamic acid lysine dimer (EK), cysteine ​​(C) and aspartic acid (EK-C-D)

[0107] (1) Synthesis of thiol-activated EK-C-D polypeptide backbone

[0108] Refer to the synthetic route (4), weigh 1g side chain Z-protected EK dimer (2mmol), 0.3mmol side chain Z-protected aspartic acid and 0.1817g H-Cys(Trt)-OH (0.5mmol) and add into a 50 mL round bottom flask, then add 4 mL of anhydrous DMF solution. Then weigh 0.69g EDC·HCl (3.6mmol), 0.4865g HOBt (3.6mmol) and 0.9306g DIEA solution (7.2mmol) into the above-mentioned round-bottomed flask, sonicate until completely dissolved, then seal and stir the reaction with a parafilm 48h. By changing the amount of H-Cys(Trt)-OH, the hybrid polypeptide products with EK and C molar ratios of 2:1, 3:1 and 4:1 were synthesized.

[0109] After the reaction, add 10 times the amount of DMF in anhydrous ether to the flask to precipitate the reaction product, and stir for a...

Embodiment 3

[0118] Embodiment 3: Carrying doxorubicin nanoparticles based on glutamic acid lysine dimer (EK), cysteine ​​(C), aspartic acid and phenylalanine (EK-C-D-F) drug preparation

[0119] (1) Synthesis of EK-C-D-F polypeptide backbone

[0120] Referring to the synthetic route (6), weigh 1g side chain Z-protected EK dimer (2mmol), 0.3mmol side chain Z-protected aspartic acid, 0.1817g H-Cys(Trt)-OH (0.5mmol) and 0.3mmol of phenylalanine (F) was added to a 50mL round bottom flask, and then 4mL of anhydrous DMF solution was added. Then weigh 0.9g EDC·HCl (4.7mmol), 0.64g HOBt (4.7mmol) and 1.21g DIEA solution (9.4mmol) into the above-mentioned round-bottomed flask, sonicate until completely dissolved, then seal with a parafilm and stir for 48h . By changing the addition amount of H-Cys(Trt)-OH, the molar ratio of synthetic EK and cysteine ​​(C) is 2:1, 4:1 and 6:1 mixed polypeptide products respectively; The molar ratios of EK and phenylalanine were 2:1, 3:1 and 4:1 to synthesize t...

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Abstract

The invention discloses a zwitterionic polypeptide, a derivative of the zwitterionic polypeptide and a nano-drug based on the zwitterionic polypeptide. Nano-drugs can be prepared on the basis of the zwitterionic polypeptide or derivatives thereof, the secondary structure of the zwitterionic polypeptide has excellent conversion capability before and after drug release, and release of the drugs in cells can be accelerated. The obtained nano-drug can be used for tumor targeted therapy; unexpected tumor targeting performance is obtained; and the nano-drug has excellent blood compatibility, has thecapability of avoiding immune recognition, tumor targeting, intracellular transformation and entering into cell nuclei, can reduce the distribution in liver, kidney, spleen, lung, heart and other organs rich in reticuloendothelial tissues, and finally realize the capability of efficiently inhibiting tumor growth and the in-vivo low-toxicity targeting tumor treatment effect.

Description

technical field [0001] The invention relates to a zwitterionic polypeptide, its derivatives and nano-medicine, and belongs to the field of functional polypeptide and nano-medicine manufacture. Background technique [0002] Malignant tumors, a chronic health disease worldwide, are characterized primarily by abnormal proliferation of cells. After half a century of huge investment by human beings, although some progress has been made in the treatment of cancer in the medical field, cancer is still a huge threat to human beings. According to the assessment of the International Agency for Research on Cancer, it is still a huge threat to human beings. According to the International Agency for Research on Cancer, by 2030, there will be 22.2 million new cancer cases and 13.2 million deaths. Chemotherapy is one of the main methods of existing tumor treatment, but it has three major defects, including: toxic and side effects on normal cells in healthy organs and tissues, multidrug r...

Claims

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Application Information

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IPC IPC(8): C07K7/02C07K1/06A61K47/64A61K31/704A61P35/00
CPCC07K5/0202A61K47/64A61K31/704A61P35/00Y02P20/55A61K47/645C07K5/1021C08G69/10A61K9/1075
Inventor 陈圣福薛伟利阿斯·屈塔
Owner ZHEJIANG UNIV
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