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Application of compound in RADNOVA anti-radiation treatment

A compound and anti-radiation technology, applied in the field of biomedicine, to achieve outstanding effects on bone marrow hematopoietic system damage

Pending Publication Date: 2020-06-12
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Increased HIF-2 activity leads to some cancers, while decreased activity leads to anemia in chronic kidney disease

Method used

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  • Application of compound in RADNOVA anti-radiation treatment
  • Application of compound in RADNOVA anti-radiation treatment
  • Application of compound in RADNOVA anti-radiation treatment

Examples

Experimental program
Comparison scheme
Effect test

preparation example

[0031] Add o-benzoylsulfonimide (5g, 27.3mmol) into a 100mL round-bottomed flask, add thionyl chloride (10mL) at room temperature, and then add anhydrous DMF (0.1mL) dropwise under stirring . The system was heated to 80°C and reacted for 2 hours. After the reaction was completed, the reaction system was directly evaporated to dryness to obtain 6 g of a colorless and transparent paste crude product (Compound 1), which could be directly used in the next reaction without further purification.

[0032] The crude product of compound 1 (6g) was added in a 100mL round bottom flask, followed by sequential addition of 1,4-dioxane (15mL), triethylamine (8g, 82mmol), 3,5-bis(trifluoromethane base) aniline (6.3 g, 27.3 mmol). The reaction system was heated to 30° C. for 1 hour. After the reaction was completed, the reaction system was directly evaporated to dryness. The solid product was washed with water (30mL*3) and methanol (10mL*3) respectively, finally filtered and dried to obtai...

experiment example 1

[0035] Mice: Male wild-type C57 mice (6-8 weeks) were purchased from Chinese Academy of Sciences (Shanghai). All mice were bred in the Special Pathogen Free (SPF) laboratory of Animal Experiment Center of Second Military Medical University (Shanghai). The mice were randomly divided into 2 groups (irradiation + normal saline group and irradiation + RADNOVA group), with 10 mice in each group, and the mice in the RADNOVA group were injected intraperitoneally 24 hours before irradiation and 2 hours before irradiation. 2.0mg / piece / time. The normal saline group was given the same dose of normal saline as a control.

[0036] Whole-body irradiation with 12Gy γ-rays was given to the mice, all the mice in the saline group died within 7 days, and the average survival time of the mice in the RADNOVA administration group was significantly prolonged. Experimental results such as figure 1 shown.

[0037] RADNOVA can improve the damage of intestinal tissue in mice after 12Gy γ-ray whole b...

experiment example 2

[0039] Mice: Male wild-type C57 mice (6-8 weeks) were purchased from Chinese Academy of Sciences (Shanghai). All mice were bred in the Special Pathogen Free (SPF) laboratory of Animal Experiment Center of Second Military Medical University (Shanghai). The mice were randomly divided into 2 groups (irradiation + normal saline group and irradiation + RADNOVA group), with 10 mice in each group, and the mice in the RADNOVA group were injected intraperitoneally 24 hours before irradiation and 2 hours before irradiation. 2.0mg / piece / time. The normal saline group was given the same dose of normal saline as a control.

[0040] Whole-body irradiation with 8.5Gy gamma rays was given to the mice, all the mice in the saline group died within 10 days, and the 30-day survival rate of the mice in the RADNOVA administration group was 100%. Experimental results such as Figure 4 shown. It can be seen that RADNOVA has an unusually obvious protective effect on lower doses of radiation (8.5Gy ...

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Abstract

The invention relates to the field of biological medicines, in particular to application of a compound RADNOVA in preparation of anti-radiation medicines. The application has the beneficial effects that the new application of the compound RADNOVA in radiation resistance is discovered and proved for the first time, and the compound RADNOVA has an outstanding effect in the aspects of intestinal tract tissue damage and bone marrow hematopoietic system damage caused by radiation resistance.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the use of compound RADNOVA in anti-radiation therapy. Background technique [0002] With the extensive development and utilization of nuclear energy in my country and the rapid development of nuclear medicine, people are more and more exposed to ionizing radiation. The Fukushima nuclear power plant accident in 2011 and the recent North Korean nuclear crisis once again remind us that nuclear threats still exist. The damage of radiation to intestinal tissue, lung tissue and bone marrow tissue is particularly obvious. [0003] Hypoxia-inducible factor 2 (HIF-2) is a heterodimeric transcription factor formed by the hypoxia-sensitive HIF-2α subunit and its specific partner subunit ARNT dimer. Increased HIF-2 activity leads to some cancers, while decreased activity leads to anemia in chronic kidney disease. Cummins EP et al. demonstrated that upregulation of HIF using PHD inhibitors can ...

Claims

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Application Information

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IPC IPC(8): A61K31/428A61P39/00A61P1/00A61P7/06C07D275/06
CPCA61K31/428A61P39/00A61P1/00A61P7/06C07D275/06
Inventor 刘聪杜继聪东肃河高福程赢蔡建明崔建国刘虎刘入菱杨彦勇
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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