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Naphthalimide modified dendrimer transgenic carrier and preparation method and application thereof

A technology of dendrimer and transgene carrier, which is applied in the field of polymer chemistry and biological materials, can solve the problems of unsatisfactory transfection efficiency, complicated modification process, high cytotoxicity, etc., achieve excellent in vivo and in vitro imaging performance, and simple preparation method , high cytotoxic effect

Active Publication Date: 2018-11-06
西安九清医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the modification process of most current dendrimers is relatively complicated, the cytotoxicity after modification is high, and the transfection efficiency is not ideal. These factors greatly limit their application in gene therapy.

Method used

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  • Naphthalimide modified dendrimer transgenic carrier and preparation method and application thereof
  • Naphthalimide modified dendrimer transgenic carrier and preparation method and application thereof
  • Naphthalimide modified dendrimer transgenic carrier and preparation method and application thereof

Examples

Experimental program
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Effect test

example 1

[0052] Preparation of the fifth-generation polyamide-amine dendrimer transgenic carrier based on naphthalimide compound modification at a molar ratio of 1:10 to link 4-amino-1,8-naphthalimide based on covalent bonds Example of the modified fifth-generation polyamide-amine dendrimer transgene carrier:

[0053] A dendrimer transgene carrier modified by naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0054]

[0055] In formula (I), G5 is the fifth-generation polyamide-amine dendrimer, a is the number of naphthalimide compound groups covalently linked to the dendrimer surface, and the theoretically expected value of a is 10.

[0056] G5 is the fifth generation polyamide-amine dendrimer, and its structural formula (II) is as follows:

[0057]

[0058] In formula (II), M is ethylenediamine; the terminal primary amino group is 128, n=6; m=2.

[0059] Preparation of the above-mentioned naphthalimide-modified dendrimer transgene car...

example 2

[0063] Preparation of the fifth-generation polyamide-amine dendrimer transgenic carrier based on naphthalimide compound modification with a molar ratio of 1:40 to link 4-amino-1,8-naphthalimide based on covalent bonds Example of the modified fifth-generation polyamide-amine dendrimer transgene carrier:

[0064] A dendrimer transgene carrier modified by naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0065]

[0066] In formula (I), G5 is the fifth-generation polyamide-amine dendrimer, a is the number of naphthalimide compound groups covalently linked to the dendrimer surface, and the theoretically expected value of a is 40.

[0067] G5 is the fifth generation polyamide-amine dendrimer, and its structural formula (II) is as follows:

[0068]

[0069] In formula (II), M is ethylenediamine; the terminal primary amino group is 128, n=6; m=2.

[0070] Preparation of the above-mentioned naphthalimide-modified dendrimer transgene c...

example 3

[0074] Preparation of the fifth-generation polyamide-amine dendrimer transgenic carrier based on naphthalimide compound modification at a molar ratio of 1:80 to link 4-amino-1,8-naphthalimide based on covalent bonds Example of the modified fifth-generation polyamide-amine dendrimer transgene carrier:

[0075] A dendrimer transgene carrier modified by naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0076]

[0077] In formula (I), G5 is the fifth-generation polyamide-amine dendrimer, a is the number of naphthalimide compound groups covalently linked to the dendrimer surface, and the theoretically expected value of a is 80.

[0078] G5 is the fifth generation polyamide-amine dendrimer, and its structural formula (II) is as follows:

[0079]

[0080] In formula (II), M is ethylenediamine; the terminal primary amino group is 128, n=6; m=2.

[0081]Preparation of the above-mentioned naphthalimide-modified dendrimer transgene carr...

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Abstract

The invention provides a naphthalimide modified dendrimer transgenic carrier which comprises a dendritic polymer skeleton and a naphthalimide containing functional group, wherein the naphthalimide containing functional group is covalently attached to surfaces of dendritic polymers. The invention further provides a preparation method of the dendrimer transgenic carrier and an application of the dendrimer transgenic carrier serving as a nucleic acid molecular transport carrier. A brand new modification method and the functional group are adopted to modify the dendritic polymers, and simple and efficient reaction and high yield are achieved; efficient transfection effect is achieve din the process of cell transfection, simple material production and low cost are achieved, the transfection process has low cytotoxicity, and genetic molecules can be effectively and safety transported into cells; the dendrimer transgenic carrier has the advantages of high efficiency, low toxicity, low price and easiness in synthesis.

Description

technical field [0001] The invention belongs to the technical field of polymer chemistry and biological materials, and in particular relates to a dendrimer transgene carrier modified by naphthalimide, a preparation method and application thereof. Background technique [0002] Gene therapy is to introduce exogenous normal genes into target cells to correct or compensate diseases caused by gene defects or abnormalities, so as to achieve the purpose of treatment. Gene therapy has shown great potential in the treatment of many major diseases, such as: cancer, AIDS, diabetes, cystic fibrosis, cardiovascular disease, etc. [0003] The key to gene therapy is to efficiently introduce genes with therapeutic functions into cells. However, naked DNA generally exists in the form of a stretched linear helix, which is relatively large in size, and the DNA molecule itself is a negatively charged anion. Electrostatic repulsion occurs between anions in the outer layer of the cell membrane. ...

Claims

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Application Information

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IPC IPC(8): C12N15/87C08G73/02
CPCC08G73/028C12N15/87
Inventor 高永光骞爱荣田野李郁党凯姜山峰罗晓庆赵欣杨超飞
Owner 西安九清医疗科技有限公司
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