Antitumor application of covalent organic framework material

A covalent organic framework and tumor technology, which is applied in the field of tumor treatment, can solve the problems of decreased ROS production capacity, inability to direct intravenous injection, and decreased ROS capacity, and achieve the effects of enhancing ROS capacity, prolonging life, and increasing exposure

Active Publication Date: 2019-02-12
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 photosens

Method used

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  • Antitumor application of covalent organic framework material
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  • Antitumor application of covalent organic framework material

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0105] Example 1

[0106] Preparation of covalent organic framework materials with heterogeneous structure

[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, and the reaction time is 2-5 days. The obtained solid product is washed with toluene until the liquid is colorless. The solvent is removed by heating under vacuum, the temperature is 80~120℃, and the time is 12~48h.

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

Example Embodiment

[0109] Example 2

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

[0111] Material particle size and potential measurement

[0112] A PBS-dispersed covalent organic nanosheet dispersion (0.1 mg / mL) was prepared, and then the particle size and potential were measured.

[0113] See figure 1 , figure 1 This is a graph of the particle size distribution and potential of the covalent nanosheet with a heterogeneous structure prepared in Example 1 of the present invention.

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

[0115] See figure 2 , figure 2 This is an electron micrograph of the covalent nanosheet with heterogeneous structure prepared in Example 1 of the present invention.

Example Embodiment

[0116] Example 3

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

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

[0119] Add 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 UV absorption.

[0120] See image 3 , image 3 This is the photodynamic evaluation of the material level of the covalent organic nanosheets prepared in the examples of the present invention. That is, under light conditions, the DPBF absorption intensity varies with the irradiation time.

[0121] by image 3 It can be seen that it proves the generation of ROS.

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Abstract

The invention provides application of a covalent organic framework material to preparation of one or a plurality of tumor treatment medicine, photodynamic therapy medicaments and photothermal therapymedicaments. The covalent organic framework material is of a structure shown as a formula (I). The covalent organic framework material of the structure shown as the formula (I) is used for tumor treatment medicine, photodynamic therapy medicaments and photothermal therapy medicaments; after the optical excitation, the heat can be released, so that the photothermal therapy of the tumor is realized;the photodynamic and photothermal synergetic therapy can be realized under the single wavelength, so that the powerful cell killing is realized. In addition, the covalent organic framework material has an ERP effect; the enrichment of nanosheets in an in vivo experiment is improved; meanwhile, the photoacoustic imaging capability is realized; the optimal enrichment time of the covalent organic framework material can be determined, so that the tumor treatment under the imaging guidance is realized. The formula is shown in description.

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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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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