Dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide, preparation method and application thereof

A dendrimer and transgenic vector technology, applied in the fields of polymer chemistry and biological materials, can solve the problems of low transfection efficiency, lack of targeting groups, poor cell selectivity, etc., and achieve high transfection efficiency, cheap and easy raw materials. high-efficiency, low cytotoxicity

Active Publication Date: 2021-06-29
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

In addition, due to the lack of targeting groups in most of the current vectors,

Method used

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  • Dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide, preparation method and application thereof
  • Dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide, preparation method and application thereof
  • Dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0055] Take the fifth-generation polyamide-amine dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide compound as an example: figure 1 Shown is the synthetic route of the dendrimer transgene carrier modified by bone-targeting peptide and naphthalimide of the present invention,

[0056] A dendrimer transgene carrier modified with a bone-targeting peptide and naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0057]

[0058] In formula (I), G5 represented by R is the fifth generation polyamide-amine dendrimer, the central core M is ethylenediamine, and the terminal primary amine group is 128, as shown in its structural formula (II):

[0059]

[0060] Among them, the theoretical expectation of a is 10, and the theoretical expectation of b is 20;

[0061] The fifth-generation polyamide-amine dendrimer transgene carrier material modified by bone-targeting peptide and naphthalimide compound, its synthesi...

example 2

[0080] A dendrimer transgene carrier modified with a bone-targeting peptide and naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0081]

[0082] In formula (I), G5 represented by R is the fifth generation polyamide-amine dendrimer, the central core M is ethylenediamine, and the terminal primary amine group is 128, as shown in its structural formula (II):

[0083]

[0084] Among them, the theoretical expectation of a is 10, and the theoretical expectation of b is 40;

[0085] The fifth-generation polyamide-amine dendrimer transgene carrier material modified by bone-targeting peptide and naphthalimide compound, its synthesis route is as follows:

[0086]

[0087] The specific steps of the method include:

[0088]Step 1: 50 mg of dendrimer R and 3.7 mg of compound 2 4-amino-1,8-naphthoic anhydride were weighed and dissolved in 5 ml of ethanol. The reaction solution was heated to 70°C, stirred for 8 hours, and then cooled to ...

example 3

[0104] A dendrimer transgene carrier modified with a bone-targeting peptide and naphthalimide, the structural formula (I) of the dendrimer transgene carrier is as follows:

[0105]

[0106] In formula (I), G5 represented by R is the fifth generation polyamide-amine dendrimer, the central core M is ethylenediamine, and the terminal primary amine group is 128, as shown in its structural formula (II):

[0107]

[0108] Among them, the theoretical expectation of a is 10, and the theoretical expectation of b is 80;

[0109] The fifth-generation polyamide-amine dendrimer transgene carrier material modified by bone-targeting peptide and naphthalimide compound, its synthesis route is as follows:

[0110]

[0111] The specific steps of the method include:

[0112] Step 1: 50 mg of dendrimer R and 3.7 mg of compound 2 4-amino-1,8-naphthoic anhydride were weighed and dissolved in 5 ml of ethanol. The reaction solution was heated to 70°C, stirred for 8 hours, and then cooled to...

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Abstract

The present invention provides a dendrimer transgene carrier modified with bone-targeting peptide and naphthalimide, which includes a dendrimer skeleton, a bone-targeting peptide group, and a functional group containing naphthalimide. The targeting peptide group and the naphthalimide functional group are covalently bonded on the surface of the dendrimer; the dendrimer is a polyamide-amine dendrimer. The invention also provides the preparation method of the gene transfection carrier and the application of the dendrimer transgene carrier as a nucleic acid molecule delivery carrier. The invention adopts a brand-new modification method and a functional group to modify the dendrimer, the reaction is simple and efficient, the yield is high, the efficient transfection effect is achieved in the cell transfection process, and the bone targeting performance is better. The production of materials is simple and low in cost, the cytotoxicity of the transfection process is low, and gene molecules can be effectively and safely transported into cells. The dendrimer transgene carrier of the present invention has the advantages of high efficiency, low toxicity, low price, and simple synthesis .

Description

technical field [0001] The invention belongs to the technical field of polymer chemistry and biomaterials, and in particular relates to a dendrimer transgene carrier modified with a bone-targeting peptide and naphthalimide, a preparation method and application thereof. Background technique [0002] As a new type of treatment, gene therapy has shown great application potential in the treatment of major diseases such as cancer, AIDS, and osteoporosis. However, due to the lack of safe and efficient targeted gene carriers, there has been no breakthrough in gene therapy for bone diseases such as osteoporosis. [0003] Gene therapy refers to the introduction of exogenous normal genes into target cells by means of gene carriers to correct or compensate diseases caused by gene defects or abnormalities, so as to achieve the purpose of treatment. However, naked DNA generally exists in the form of a stretched linear helix with a loose volume, and the DNA molecule itself is a negativel...

Claims

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Application Information

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IPC IPC(8): C12N15/87C08G73/02
CPCC08G73/028C12N15/87
Inventor 骞爱荣高永光蔺枭胡丽芳张文娟罗晓庆赵欣李迪杰
Owner 西安九清医疗科技有限公司
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