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Application of bifunctional chelating agent in uranium excretion promotion and radiation protection

A chemical compound, reaction temperature technology, applied in the field of medicine, can solve problems such as ecological environment and human health threats, radioactive and non-radioactive pollution pollutants, etc.

Active Publication Date: 2020-05-12
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002]With the rapid development of nuclear energy in my country, the demand for uranium is increasing day by day, but a large amount of radioactive and non-radioactive pollution will be produced during the mining and production process of uranium Pollutants that pose a serious threat to the entire ecological environment and human health

Method used

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  • Application of bifunctional chelating agent in uranium excretion promotion and radiation protection
  • Application of bifunctional chelating agent in uranium excretion promotion and radiation protection
  • Application of bifunctional chelating agent in uranium excretion promotion and radiation protection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the synthesis of chelating agent I-2 in structural general formula (I)

[0026]

[0027] 1,2 diphenylethylenediamine (2.12g, 10 mmol), NaOH (880mg, 22 mmol) were dissolved in 30 mL of dichloromethane solution, at 0 o Acetyl chloride cinnamate (984 mg, 60 mmol) was added at 0 C and the reaction was stirred overnight. TLC was used to detect the reaction process. After the reaction was completed, add 2 M HCl to adjust the pH to 1, extract with ethyl acetate (30 mL x 3), collect the organic phase, wash with saturated sodium chloride, dry with anhydrous sodium sulfate, spin dry, 200-300 By silica gel column chromatography, 3.97 g of the target compound 1 was obtained, with a yield of 82%.

[0028] To a 100 mL flask containing compound 1 (3.97g, 8.2 mmol) was added tetrahydrofuran: methanol: water = 4:1:1 (volume ratio) solvent 30 mL, then NaOH (1.28g, 32 mmol) was added at 70 o C under reflux for 3h. After the reaction was detected by TLC, the pH was adju...

Embodiment 2

[0033] Example 2 Chelation evaluation experiment of compounds represented by formula (I)

[0034] Accurately weigh an appropriate amount of uranyl acetate, and add deionized water to make a solution with a metal ion concentration of 0.2 mmol / L. Accurately weigh an appropriate amount of the bifunctional chelating agent (n=0, 1, 2, 3, 4, named I-0, I-1, I-2, I-3 and I-4) shown in (I), Add deionized water to make a solution with a concentration of 0.2 mmol / L. Different volumes of each metal ion solution and the compound solution represented by formula (I) are mixed separately to form a series of solutions to be tested. After forming a stable complex, use a UV-Vis spectrophotometer to scan a series of solutions in the range of 200-500 nm to find the maximum absorption peak of the complex, and record the absorbance value at this point. Take the mole fraction χ (the ratio of the mass concentration of metal ions to the total mass concentration) as the abscissa, and the absorbance a...

Embodiment 3

[0040] Example 3 Evaluation experiment of the uranium excretion promoting effect of the compound represented by formula (I)

[0041] SD rats, weighing 200±20 g, 12 in each group. Randomly divided into ① blank control group; ② exposure model group; ③ uranium exposure + 100 mg / kg DTPA-Ca positive drug group; ④ uranium exposure + 100 mg / kg bifunctional chelating agent shown in formula (I) ( n=0,1,2,3,4, named as I-0, I-1, I-2, I-3 and I-4) groups. Rats were intraperitoneally injected with 500 μg / kg uranyl acetate and immediately intramuscularly injected with DTPA-Ca and a bifunctional chelator group. Rats in the poisoning control group were intraperitoneally injected with uranyl acetate and immediately intramuscularly injected with equal volume of normal saline. Rats in the blank control group were intraperitoneally injected with normal saline and immediately intramuscularly injected with the same volume of normal saline, and the result was used as the background value.

[004...

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Abstract

The invention discloses a novel bifunctional chelating agent and application thereof in emission promotion and radiation protection of nuclide uranium. The novel difunctional chelating agent is obtained by coupling tomatidine and Tempol by utilizing the uranium chelating effect of tomatidine and the free radical scavenging and radiation damage protection effects of the Tempol nitroxide free radicals; meanwhile, the purposes of promoting discharge of uranium contamination and protecting internal radiation damage are achieved, so that a double-effect drug treatment effect is achieved. The invention has the advantages of simple synthesis process and low production cost, has strong uranium chelating excretion promotion and damage prevention and treatment effects, can be prepared into tablets,capsules, solutions, injections, dropping pills and other dosage forms, and is suitable for damage treatment of nuclear weapons, nuclear accidents and people infected with nuclide uranium in special environments.

Description

technical field [0001] The invention relates to a dual-functional chelating agent and its application in promoting the emission of nuclide uranium and radiation protection, which can be used for injury treatment of people exposed to nuclide uranium in nuclear weapons, nuclear accidents and special environments, and belongs to the technical field of medicine. Background technique [0002] With the rapid development of nuclear energy in my country, the demand for uranium is increasing day by day. However, a large number of radioactive and non-radioactive pollutants will be produced during the mining and production process of uranium, which poses a serious threat to the entire ecological environment and human health. Uranium is not only a heavy metal element but also a very harmful radioactive element. Once it is transferred into the human body through food, water or other means, it is extremely difficult to excrete it out of the body. These uranium elements will form a lifetime...

Claims

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Application Information

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IPC IPC(8): C07D401/14A61K31/4545A61P39/04
CPCC07D401/14A61P39/04Y02E30/30
Inventor 何炜刘慧霞张邦乐李明华谢学军
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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