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Application of covalent organic nanosheet material

A covalent organic and nanosheet technology, applied in the field of radionuclide excretion agents, can solve the problems of short biological half-life, high biological toxicity, poor membrane permeability and selectivity, etc.

Active Publication Date: 2020-12-22
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the short biological half-life and high biotoxicity, poor membrane permeability and selectivity of small-molecule stimulants limit the application of small-molecule stimulants in radiation and protection.

Method used

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  • Application of covalent organic nanosheet material
  • Application of covalent organic nanosheet material
  • Application of covalent organic nanosheet material

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] see figure 1 , this example prepared amidoxime-modified nanosheets CON-AO through a step-by-step post-modification synthesis method. The synthesis steps of CON-AO are as follows:

[0035] (1) Synthesis of COF-Imine: Weigh terephthalaldehyde (32mg, 0.24mmol) and 1,3,5-tris(4-aminophenyl)benzene (56mg, 0.16mmol) into a heat-resistant Schlenk glass tube (10mL) mmol), slowly added solvent o-dichlorobenzene (0.5 mL), solvent n-butanol (0.5 mL) and catalyst acetic acid (0.1 mL, 6M). After ultrasonication for two minutes, the reaction test tube was frozen in liquid nitrogen-vacuumized-filled with nitrogen, and cycled three times, filled with nitrogen protection and then sealed. Placed in an oven at 120°C for 72 hours, a yellow solid was generated. The solid was separated by centrifugation, washed with tetrahydrofuran and ethanol, activated by Soxhlet extraction with tetrahydrofuran for 24 hours, and dried in a vacuum oven at 50°C for 6 hours. The reaction scheme is as follo...

Embodiment 2

[0049] In order to study the influence of physiological pH and solution pH on adsorption, the present invention also studied the adsorption capacity of CON-AO prepared in Example 1 at pH 3-9 to uranyl.

[0050] The uranium solution (10mL, 8.0ppm) of CON-AO (5.0mg) was shaken and dispersed, and the shaking time was 1h, 12h and 24h respectively. When the pH value of the uranium solution was between 3 and 9, the effect of CON-AO on UO 2 2+ (8ppm) removal rate. Such as image 3 As shown in a, as the pH value increases from 3.0 to 6.0, the removal rate of uranium increases significantly, and the maximum removal rate reaches 98% at pH 6.0, and then decreases slightly. This phenomenon is due to the enhanced binding of uranyl due to the deprotonation reaction of the active binding sites (hydroxyl groups) on the nanoflakes. At physiological pH 7.4, the uranyl removal efficiency was about 90%, indicating that CON-AO is suitable for the removal of uranyl ions in vivo.

Embodiment 3

[0052] The selectivity between uranyl ions and other divalent metal elements in vivo is a key factor to evaluate the quality of uranium chelating agents in vivo. To this end, the adsorption selectivity of CON-AO for uranyl in vitro was verified.

[0053] The first set of selectivity experiments used the UO 2 2+ (10ppm) and respectively and different divalent metal ions (50ppm, Mg 2+ , Ca 2+ 、Co 2+ , Mn 2+ 、Ni 2+ and Zn 2+ ) composed of bimetallic component HEPES buffer solution; the second set of selectivity experiments is UO 2 2+ (4ppm) and mixed divalent metal ions (10ppm, Mg 2+ , Ca 2+ 、Co 2+ , Mn 2+ 、Ni 2+ and Zn 2+ ) multi-component HEPES buffer solution.

[0054] From image 3 It can be seen in b that although the concentration of other ions is UO 2 2+ 5 times, but in each group UO 2 2+ The removal rate of CON-AO is 85.39%-94.5%, while the removal rate of other divalent metal ions by CON-AO is only 3.78%. The second group of selective adsorption expe...

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Abstract

The invention relates to application of a covalent organic nanosheet material to preparation of a medicine for preventing and / or treating radiation damage caused by radionuclide. The covalent organicnanosheet material comprises a plurality of amidoxime groups. The invention discloses the novel application of the covalent organic nanosheet material. The radionuclide is chelated and coordinated byutilizing the synergistic effect of multiple pieces of amidoxime, the covalent organic nanosheet material has very high selectivity on radionuclide, and the bottlenecks of fast metabolism, strong toxicity and poor excretion promoting effect of a conventional small molecular ligand are broken through.

Description

technical field [0001] The invention relates to the field of nuclide expulsion enhancers, in particular to the application of a covalent organic nano sheet material. Background technique [0002] In recent years, nuclear accidents and nuclear terrorist attacks have occurred frequently, and nuclear safety protection has been highly valued. Actinides are highly chemically toxic and radioactive. Once they enter the blood, they will quickly deposit in the organs and cause internal exposure. The chemical toxicity of heavy metals can cause kidney failure, bone cancer, etc., which can be fatal. At present, using chelating agents to complex nuclide ions and promote their excretion is the most effective way to reduce internal pollution. However, the research progress of actinide excretion enhancers has been extremely slow in the past 30 years, and the only approved DTPA expulsion enhancer has limited efficiency. Therefore, it is urgent to explore new low-toxicity and high-efficiency...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/787A61P39/02B82Y5/00
CPCA61K31/787A61P39/02B82Y5/00
Inventor 王殳凹第五娟白茹陈龙王晓梅
Owner SUZHOU UNIV
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