Difunctional heteropolyacid discharge promoting agent

A technology of heteropolyacids and excretion-promoting agents, applied in the directions of antitoxins, drug combinations, active ingredients of phosphorus compounds, etc., can solve the problems of poor selectivity, high toxicity of excretion-promoting agents, kidney damage, etc., and reduce the increase of oxidative stress. High, excellent biocompatibility, ROS reduction effect

Active Publication Date: 2022-07-22
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Siderophore ligands: catechol (CAM) and hydroquinone amide (TAM) have limited oral and delayed administration ability under low molar ratio conditions, and have obvious nephrotoxicity, which can cause long-term kidney damage in severe cases; hydroxyl Pyridone ligands can efficiently remove uranium in the kidney, but the bone uranium excretion rate is not good, the metabolism in the body is fast, and the bioavailability is low
[0007] To sum up, the existing excretors have high toxicity, poor selectivity, limited excretion capacity of the kidneys and bones, and small molecule drugs also have limitations such as poor cell membrane permeability, fast metabolism, and repeated drug intake.
In addition, the above-mentioned excretion-promoting agents focus on the improvement of excretion rate, ignoring the oxidative stress caused by internal radionuclide irradiation, which leads to the increase of intracellular ROS levels, which in turn leads to cell apoptosis and tissue damage.
At present, the research on bifunctional nuclide excretion enhancers is very limited and the effect needs to be improved

Method used

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  • Difunctional heteropolyacid discharge promoting agent
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  • Difunctional heteropolyacid discharge promoting agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation and characterization of polyoxometalates (POMs)

[0040] Under magnetic stirring, 120 g (0.36 mol) of sodium tungstate dihydrate Na 2 WO 4 ·2H 2 O was stirred with 150 mL of water in a 300 mL beaker until the solids were completely dissolved. Phosphoric acid (85%) was added dropwise (4.0 mL, 0.06 mol) with constant stirring. After the addition of the acid, the pH of the solution was 8.9-9.0. Glacial acetic acid (22.5 mL, 0.40 mol) was added dropwise with vigorous stirring and a large white precipitate formed during the addition. The final pH of the solution was 7.5 ± 0.3. Continue to stir for 1 h, collect the precipitate and dry it by suction filtration to obtain POMs (α-PW 9 Heteropolyacid salt), the yield of the product is 90 g (85-90%), the structure is as follows figure 1 shown, infrared spectroscopy and thermogravimetric analysis as figure 2 shown.

[0041] Biocompatibility experiments such as image 3 From left to right, deionized...

Embodiment 2

[0045] Example 2: Preparation of polyoxometalates (POMs)

[0046]Stir 0.36 mol potassium tungstate with 150 mL water in a 300 mL beaker with magnetic stirring until the solid is completely dissolved, phosphoric acid (85%) is added dropwise (8.0 mL, 0.12 mol) with constant stirring; dropwise with vigorous stirring Glacial acetic acid (15.75 mL, 0.28 mol) was added, a large amount of white precipitate was formed during the addition, and stirring was continued for 0.5 h, the precipitate was collected and dried by suction filtration to obtain POMs.

Embodiment 3

[0047] Example 3: Preparation of polyoxometalates (POMs)

[0048] 0.36 mol of sodium tungstate dihydrate and 150 mL of water were stirred in a 300 mL beaker with magnetic stirring until the solid was completely dissolved, phosphoric acid (85%) was added dropwise (2.4 mL, 0.036 mol) with constant stirring; Glacial acetic acid (27 mL, 0.48 mol) was added dropwise with stirring, a large amount of white precipitate was formed during the addition, and stirring was continued for 3 h, the precipitate was collected and dried by suction filtration to obtain POMs.

[0049] The POMs obtained in Example 1 were subjected to the following detection tests

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Abstract

The invention belongs to the technical field of biological excretion promotion, and particularly relates to a difunctional heteropolyacid excretion promoting agent which is used for nuclide excretion promotion and ROS removal, and the difunctional heteropolyacid excretion promoting agent comprises phosphotungstic heteropolyacid salt. The novel phosphotungstic heteropolyacid salt molecular cleanup promoting agent is adopted, has excellent biocompatibility, mild biotoxicity and good cleanup promoting effect and ion selectivity on uranyl, and compared with ZnNa3-DTPA, the novel phosphotungstic heteropolyacid salt molecular cleanup promoting agent can remarkably improve the cleanup promoting rate of uranium in kidneys and bones; while uranium is removed, the ROS level rise, caused by radionuclide, in an organism can be effectively reduced, a brand-new and efficient radionuclide cleanup promoting agent is successfully developed, and important practical significance is achieved for safe and efficient development of nuclear energy and nuclear safety emergency.

Description

technical field [0001] The invention belongs to the technical field of biological excretion, in particular to a bifunctional heteropolyacid excretion promoter. Background technique [0002] Nuclear accidents and nuclear leaks may cause environmental pollution of the key actinide elements such as uranium in nuclear (spent) fuel, and may lead to further internal contamination of personnel. 24 hours after entering the human body, about one-third of uranium is released in the form of hexavalent uranyl ions (UO 2 2 + ) accumulates in the kidneys and bones, and forms stable complexes with protein or calcium hydroxyapatite (HAP) in bones that are difficult to excrete from the body. In addition, internal exposure of uranium stimulated cells to produce high levels of superoxide radicals ( O 2 - ), H 2 O 2 and hydroxyl radicals ( OH), thereby inducing cellular oxidative stress as well as enzyme inactivation and membrane dysfunction. Therefore, in vivo contamination of uranium ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/42A61P39/02A61P39/06
CPCA61K33/42A61P39/02A61P39/06Y02E30/30
Inventor 王殳凹第五娟石培珩王晓梅
Owner SUZHOU UNIV
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