Anti-tumor application of a covalent organic framework material

A covalent organic framework and tumor technology, applied in the field of tumor treatment, can solve the problems of inability to inject intravenously, decrease ROS production ability, and easy aggregation, etc., to enhance the ability to kill cells, enhance the ability of ROS, and promote apoptosis or necrosis Effect

Active Publication Date: 2021-09-21
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most photosensitizer molecules are insoluble in water, easy to aggregate and lead to a decrease in the ability to generate ROS, and cannot be directly injected intravenously
Therefore, it is very necessary to construct photosensitizers in the form of nanometers to solve the problems that photosensitizers are difficult to dissolve in water and cannot be directly injected intravenously, and the problem of reduced ROS production ability due to aggregation

Method used

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  • Anti-tumor application of a covalent organic framework material
  • Anti-tumor application of a covalent organic framework material
  • Anti-tumor application of a covalent organic framework material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Preparation of Covalent Organic Framework Materials with Heterostructures

[0107] (1) Under anhydrous and oxygen-free conditions, the donor (2,3,6,7,10,11-hexahydroxytriphenyl, 2 equivalents) and the acceptor (5,15-Bis(4-boronophenyl)porphyrin, 3 equivalents) in acetonitrile / mesitylene (7:3), the reaction temperature is 80-150°C, the reaction time is 2-5 days, and the solid product obtained is washed with toluene until the liquid is colorless. The solvent is removed by heating under vacuum, the temperature is selected as 80-120°C, and the time is selected as 12-48h.

[0108] (2) Add the obtained solid powder (3-6 mg) into water, PBS, serum (6 mL) and ultrasonically disperse to obtain a nano-sized covalent organic nanosheet dispersion (0.5-1 mg / mL).

Embodiment 2

[0110] The covalent nanosheets of covalent organic framework materials prepared in the examples of the present invention were characterized.

[0111] Material particle size and potential determination

[0112] A PBS-dispersed covalent organic nanosheet dispersion (0.1 mg / mL) was prepared, followed by measurement of particle size and potential.

[0113] see figure 1 , figure 1 The particle size distribution and potential diagram of the heterostructure covalent nanosheets prepared in Example 1 of the present invention.

[0114] Such as figure 1 As shown, the particle size of the heterostructure covalent nanosheet is about 350nm, and the potential is -37mV, which is beneficial to realize the intravenous injection of the nanosheet.

[0115] see figure 2 , figure 2 Electron micrographs of heterostructure covalent nanosheets prepared in Example 1 of the present invention.

Embodiment 3

[0117] The photodynamic properties of the covalent organic framework material covalent nanosheet material prepared in the embodiment of the present invention were evaluated.

[0118] 1,3-Diphenylisobenzofuran (DPBF) was used to detect the production of ROS, DPBF (50 μL, 1 mM)

[0119] Added to the covalent organic nanosheet dispersion (3mL, 0.1mg / mL), using a laser (1W cm-2 , 635nm) radiate the mixed solution, and monitor the change of DPBF absorption by ultraviolet absorption.

[0120] see image 3 , image 3 Material-level photodynamic evaluation of covalent organic nanosheets prepared for the examples of the present invention. That is, under the light condition, the curve graph of the DPBF absorption intensity changing with the irradiation time.

[0121] Depend on image 3 It can be seen that this proves the generation of ROS.

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Abstract

The present invention provides the application of one or more of covalent organic framework materials in the preparation of drugs for treating tumors, photodynamic therapy and photothermal therapy; the covalent organic framework materials have the formula (I ) structure shown. In the present invention, the covalent organic framework material having the structure of formula (I) is used in drugs for treating tumors, drugs for photodynamic therapy and drugs for photothermal therapy, which can release heat after light excitation, thereby realizing photothermal therapy of tumors , and the synergistic therapy of photodynamic and photothermal can be realized under a single wavelength, thus achieving powerful killing of cells. In addition, the present invention also found that the covalent organic framework material has an EPR effect, which improves the enrichment of nanosheets in vivo experiments. At the same time, it has the ability of photoacoustic imaging, and can determine the optimal enrichment time of the covalent organic framework material, thereby realizing Imaging-guided tumor therapy.

Description

technical field [0001] The present invention relates to the technical field of tumor treatment, in particular to the anti-tumor application of a covalent organic framework material, in particular to the application of a covalent organic framework material in the preparation of tumor-treating drugs, photodynamic therapy agents and photothermal therapy agents One or more applications, drugs or medicaments, covalent organic framework material dispersions. Background technique [0002] Tumor refers to the neogrowth formed by the proliferation of local tissue cells in the body under the action of various tumorigenic factors, because this neogrowth is mostly in the form of space-occupying blocky protrusions, also known as neoplasm (neoplasm) . According to the cell characteristics of new organisms and the degree of harm to the body, tumors are divided into two categories: benign tumors and malignant tumors, and cancer is the general term for malignant tumors. There are many type...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/66A61K31/80A61K41/00A61P35/00
CPCA61K31/66A61K31/80A61K41/0052A61K41/0071A61P35/00
Inventor 田华雨王奎陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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