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Polypeptide, anti-tumor drug made from polypeptide and preparation method of anti-tumor drug

A technology for tumor drugs and fat-soluble drugs, which is applied in the preparation of tumor drugs and in the field of tumor drugs. It can solve the problems of difficult assembly and preparation, easy to cause inflammation, poor biocompatibility, etc., and achieve low synthesis cost, convenient purification and stability. good sex effect

Inactive Publication Date: 2019-09-24
WEIFANG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although nanoparticles have achieved great success in tumor therapy, some polymer nanomaterials have problems such as poor biocompatibility, refractory degradation, easy to cause inflammation, and difficult to self-assemble and prepare.

Method used

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  • Polypeptide, anti-tumor drug made from polypeptide and preparation method of anti-tumor drug
  • Polypeptide, anti-tumor drug made from polypeptide and preparation method of anti-tumor drug
  • Polypeptide, anti-tumor drug made from polypeptide and preparation method of anti-tumor drug

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Embodiment 1: Preparation of Ac-IIIIIIKKKKK-NH2 polypeptide

[0055] Step 1. Distill N,N-dimethylformamide (DMF) and piperidine (Piperidine) solvents

[0056] Distill the purchased DMF solution under reduced pressure at 60°C to obtain pure DMF solvent; add a small amount of CaH2 to the purchased piperidine and heat to reflux for 1-2 hours, and receive the fraction with boiling point temperature (106°C) to obtain pure piperidine pyridine solvent.

[0057] Step 2, preparation of amino acid, resin, activator, capping agent, deprotecting agent

[0058] Calculate the amount of amino acids and other reagents required for the preparation of 0.25mM NH2-IIIIIIKKKKK-NH2 on the polypeptide solid-phase synthesizer:

[0059] Lys (lysine): 2.54g dissolved in 27mL DMF;

[0060] Ile (isoleucine): 2.27g dissolved in 32mL DMF;

[0061] Resin (loaded at 0.6mmol / g): 0.417g;

[0062] Activator: Diisopropylcarbodiimide (DIC): 17mL;

[0063] Activated base: 17-(Acetyloxy)-3-Methoxy-20-oxo...

Embodiment 2

[0069] Embodiment 2: Preparation of Ac-IIIIIIKKKKK-NH2 drug-loaded carrier

[0070] Weigh 0.519mg (0.5mmol / L) of peptide Ac-IIIIIIKKKKK-NH2, add 1mL of PBS buffer solution (pH7.4), sonicate for 5min, and after standing at room temperature for 4h, TEM observation results show that nanoparticle self-assembly has been formed at this time body (such as figure 1 shown).

Embodiment 3

[0071] Example 3: Detection of the self-assembly morphology of Ac-IIIIIIKKKKK-NH2 drug-loaded carrier in PBS buffer

[0072] The specific detection method is as follows:

[0073] Examination of self-assembled morphologies in PBS buffer (TEM).

[0074] TEM: Adjust the pH of the peptide solution to 6.0, and after standing at room temperature for a certain period of time, pipette 50 μL of the peptide solution of the sample onto the parafilm, and then adsorb it on the pure carbon membrane for 3 minutes. Excess solution was removed with filter paper, and the surface was air dried. The sample was stained with a small amount of phosphotungstic acid dye (1.0%) for 3 minutes, and then the dye was removed with filter paper. The samples were air-dried and tested. HITACHIHT7700 instrument (Japan) was used for transmission electron microscopy (TEM) research. The results showed that the peptide sample Ac-IIIIIIKKKKK-NH2 observed by transmission electron microscopy self-assembled into a n...

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PUM

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Abstract

The invention discloses a polypeptide, an anti-tumor drug made from the polypeptide and a preparation method of the anti-tumor drug. The structural formula of the polypeptide is Ac-IIIIIIKKKKK-NH2. The anti-tumor drug includes a polypeptide nano drug carrier which is a nanosphere structure that can be broken in an acid environment, and a liposoluble drug is embedded into the polypeptide nano drug carrier. The preparation method of the anti-tumor drug includes the following steps that S1, the liposoluble drug and the polypeptide are dissolved in a DMSO; S2, a PBS buffer solution is added into the DMSO for ultrasonic mixing; S3, mixed liquid is added into dialysis bags for dialysis for 24 hours to remove the DMSO and unbound liposoluble drugs, and the prepared anti-tumor drug is obtained.

Description

technical field [0001] The invention relates to the field of bioengineering, in particular to a polypeptide, a tumor drug made of the polypeptide and a preparation method of the tumor drug. Background technique [0002] The size, shape, and biodistribution of nanomaterials have sparked widespread interest in the design of more efficient drug delivery. Spherical nanomaterials have great application value in the diagnosis and treatment of tumors, and the enhanced permeability and retention effect (EPR effect) of nanomaterials with a diameter of 20-200 nm in tumor tissue eventually led to the development of FDA-approved liposome therapy. develop. Nanoscale drug carriers allow the superior action of nanoparticles and macromolecules via EPR, mainly through tumor-associated leaky blood vessel diffusion, and are ideal materials for tumor diagnosis and therapy. It can improve the stability of various drugs, realize the controlled release of drugs, and improve the bioavailability. ...

Claims

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Application Information

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IPC IPC(8): C07K7/06A61K31/704A61K47/42A61P35/00
CPCA61K31/704A61K47/42A61P35/00C07K7/06
Inventor 白靖琨龚中英
Owner WEIFANG MEDICAL UNIV
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