Application of iodine-containing chrysin derivative in preparation of medicine with radiation-proof effect

A technique for chrysin and derivatives is applied in the application field of preparing anti-radiation damage medicines, which can solve the problems of poor effect, large toxic and side effects, and poor protection effect, and achieves small toxic and side effects, no weight loss, and no Effects that cause systemic toxicity

Inactive Publication Date: 2014-07-02
NANHUA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the past 50 years, scholars from various countries have screened anti-radiation damage drugs from existing compound structure modification, purposeful synthesis of new compounds, active ingr

Method used

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  • Application of iodine-containing chrysin derivative in preparation of medicine with radiation-proof effect
  • Application of iodine-containing chrysin derivative in preparation of medicine with radiation-proof effect
  • Application of iodine-containing chrysin derivative in preparation of medicine with radiation-proof effect

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Embodiment 1 4'-iodochrysin (compound 101 ) preparation

[0042] (1) React 0.1mol phloroglucinol with 0.2mol chloroacetonitrile in 50mL ether, use zinc chloride as a catalyst, pass dry HCl gas for 2 hours under the condition of ice-salt bath, put it in the refrigerator for one day, and pass HCl again Gas 2h, placed in the refrigerator for three days. Pour off ether, wash with anhydrous ether (20mL×3), transfer the crude extract to a round bottom flask with hot water, reflux for 1h, let stand overnight, and recrystallize with water to obtain 2,4,6-trihydroxy- α-Chloroacetophenone.

[0043] (2) Mix 1.0mmol 2,4,6-trihydroxy-α-chloroacetophenone, 1.4mmol 4-iodobenzaldehyde and 0.5mL 95% ethanol, shake well, slowly add 2mL 10% NaOH dropwise, then vigorously Shake for a while, place at room temperature for 3 days, acidify with dilute hydrochloric acid, then place at room temperature for 2-3 days, filter with suction, and recrystallize the crude product with acetone or 95% ...

Embodiment 2

[0045] Embodiment 2 3'-iodochrysin (compound 102) and 2′-iodochrysin (compound 103 ) preparation: carry out with reference to Example 1. The relevant data are as follows:

[0046] compound 102 : MS (EI, 70ev) m / z: 380; Anal. Calcd. For C 15 h 9 IO 4 : C, 47.59; H, 2.48; I, 33.45; O, 16.48; Found C, 47.49; H, 2.42; I, 33.38; O, 16.81.

[0047] compound 103 : MS (EI, 70ev) m / z: 380; Anal. Calcd. For C 15 h 9 IO 4 : C, 47.39; H, 2.46; I, 33.28; O, 16.97; Found C, 47.29; H, 2.39; I, 33.36; O, 17.04.

Embodiment 3

[0048] Example 3 5,7-dimethoxy-4'-iodochrysin (compound 104 ) and 7-methoxy-4′-iodochrysin (compound 108 ) preparation

[0049] 0.3mmol 4′-iodochrysin and 3.0mmol methyl bromide in 25mL acetone, using anhydrous potassium carbonate as a catalyst, heated to reflux for 12h, and used dichloromethane: acetone as 5:1 column chromatography to obtain 5,7-dimethyl Oxygen-4′-iodochrysine (compound 104 ) and 7-methoxy-4′-iodochrysin (compound 108 ), the relevant data are as follows:

[0050] compound 104 : MS (EI, 70ev) m / z: 408; Anal. Calcd. For C 17 h 13 IO 4 : C, 50.02; H, 3.21; I, 31.09; O, 15.68; Found C, 50.12; H, 3.27; I, 31.15; O, 15.46.

[0051] compound 108 : MS (EI, 70ev) m / z: 408; Anal. Calcd. For C 17 h 13 IO 4 : C, 50.23; H, 3.14; I, 31.25; O, 15.38; Found C, 50.33; H, 3.15;

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Abstract

The invention discloses an application of iodine-containing chrysin derivative in preparation of a medicine with radiation-proof effect. Results of experiments in vitro and vivo prove that the iodine-containing chrysin derivative has the advantages that toxic and side effects are small, weight can not be reduced and toxic reaction is not caused when effective dose of the iodine-containing chrysin derivative for resisting radiation damage is used, and the iodine-containing chrysin derivative can be prepared into a medicine for being taken by persons working in an environment with radiation and patients subjected to tumour radiation therapy. The application of the iodine-containing chrysin derivative relates to preparation of the medicine with radiation-proof effect, and the iodine-containing chrysin derivative is hopeful to become a medicine for preventing and treating radiation damage.

Description

technical field [0001] The invention relates to the application of iodine-containing chrysin derivatives in the field of medicine, in particular to the application in the preparation of anti-radiation damage drugs. Background technique [0002] With the development of science and technology, the progress of material civilization has also caused a certain degree of damage to the environment. Environmental radiation factors are increasing, and radiation is increasingly affecting human health, especially workers living in radiation environments and patients receiving radiation therapy. [0003] Radiation therapy refers to the use of rays to eliminate lesions. Radiation therapy is an important means of treating malignant tumors and can produce good results for many cancers. However, radiation therapy can produce toxic side effects such as radiation dermatitis, radiation esophagitis, loss of appetite, nausea, vomiting, abdominal pain, diarrhea or constipation. [0004] After t...

Claims

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Application Information

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IPC IPC(8): C07D311/30A61K31/352A61P39/00
CPCC07D311/30
Inventor 郑兴廖端芳薄少伟魏云何淑雅
Owner NANHUA UNIV
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