Application of dihydromyricetin in preparing medicament for preventing and treating adverse reaction of tumor chemoradiotherapy

A technology of dihydromyricetin and adverse reactions, applied in the field of medicine, can solve problems such as difficult to control and eliminate adverse reactions, macromolecular function damage, inactivation and the like

Inactive Publication Date: 2009-07-22
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy drugs and radiotherapy can fight tumors, but they all produce some adverse reactions more or less, and it is difficult to control and eliminate adverse reactions, especially body mutations and secondary tumors, etc.
During radiotherapy and chemotherapy, chemotherapy drugs induce free radicals in the body, or themselves can be transformed into chemical structures in the form of free radicals, attacking cell membrane lipids, proteins and nucleic acid molecules, destroying the conformation and structural stability of these macromolecules, resulting in macromolecules The function is damaged or gradually inactivated; due to the functional inactivation of macromolecular proteins and the breakage of the linear structure of nucleic acids (DNA and RNA), gene mutations occur, cell repair functions are severely reduced, and the accumulation of gene mutations will trigger new seco

Method used

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  • Application of dihydromyricetin in preparing medicament for preventing and treating adverse reaction of tumor chemoradiotherapy
  • Application of dihydromyricetin in preparing medicament for preventing and treating adverse reaction of tumor chemoradiotherapy
  • Application of dihydromyricetin in preparing medicament for preventing and treating adverse reaction of tumor chemoradiotherapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1: Extraction and Purification of Dihydromyricetin from Grape Dendrobii Plant

[0022] Add 1 kg of young leaves, or shoots, or a mixture of young leaves and shoots of the Snake-toothed grape plant into water at a weight ratio of 1:8 to 1:12 (raw material: water), and soak for 30 minutes-4 After 1 hour, heat to boiling, heat-preserve and extract for 30-60 minutes, filter or centrifuge while it is hot, and collect the extract; add water again according to the weight ratio of 1:5-1:8 (raw material: water), heat to boil, and keep warm Extract for 20 to 40 minutes, filter or centrifuge while it is hot, and collect the extract; concentrate the extract to 20% to 50% of the original volume, add edible alcohol until the ethanol concentration is 40% to 75%, heat it to boiling and keep it warm for 10 ~ 60 minutes, after cooling slightly, filter or centrifuge to remove the precipitate, reclaim ethanol or directly cool the filtrate and let it stand for 1 to 2 days, collect t...

Embodiment 2

[0023] Example 2: Confirmation of the structure of dihydromyricetin

[0024] The dihydromyricetin prepared in Example 1.

[0025] (1) NMR analysis

[0026] The nuclear magnetic resonance detection instrument is an INOVA500 superconducting pulse Fourier transform nuclear magnetic resonance spectrometer.

[0027] After proton nuclear magnetic resonance spectrum, carbon spectrum, DEPT spectrum, gCOSY spectrum, gHMQC spectrum, gHMBC spectrum detection and analysis, it is determined that it is related to 3,5,7,3,,4,,5,-hexahydroxy 2,3 dihydroflavonol structure matches.

[0028] ① Hydrogen spectrum, gCOSY spectrum

[0029] Spectrum width: 6711.4Hz (~13ppm)

[0030] gCOSY spectrum: spectral width 4598.2×4598.2Hz; data points 2048×256.

[0031] Table 1, 1H NMR spectrum data and analysis

[0032] Chemical shift COZY correlation

[0033] Peak number Number of split peaks Coupling constant Number of protons Remarks

[0034] δ(ppm) bee

[0035] ...

Embodiment 3

[0075] Embodiment 3: The inhibitory effect of dihydromyricetin on the formation of methemoglobin caused by tertiary peroxide (TBHP)

[0076] 1. Experimental method

[0077] Add packed erythrocytes to double distilled water to make 1% erythrocytes completely hemolyzed, add each sample component and incubate at 37°C for 30min, add TBHP to make the final concentration reach 250uM, continue to incubate for 30min, measure OD 630 Relative changes in methemoglobin content were detected. Calculation of high ferritin production inhibition rate:

[0078] Generation inhibition rate=(OD of oxidative damage group 630 - Sample group OD 630 ) / (Oxidative damage group OD 630 - control group OD 630 ).

[0079] 2. Experimental results

[0080] TBHP releases H gradually in the aqueous phase 2 o 2 , H 2 o 2 Catalyzed by free or bound iron in heme to produce superoxide anion and hydroxyl radicals through the Fenton reaction. The maximum light absorption values ​​of the α and β peptide c...

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Abstract

The invention discloses application of dihydromyricetin in preparing a medicine for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor. In particular, the application is to prepare medicines for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor, preventing and treating arrest of bone marrow and baldness, resisting mutation, preventing and treating the generation of secondary tumors, preventing and treating tumor transfer, and preventing and treating breast cancer, cervical carcinoma, intestinal cancer and the like. The invention creatively finds that the dihydromyricetin has the effects of removing free radicals, inhibiting reaction chains of the free radicals, resisting the mutation, inhibiting the expression of the tumor gene, causing the death of tumor cells, preventing and treating the tumor generation, preventing and treating the secondary tumors and the transfer of the secondary tumors and preventing and treating infection. Therefore, as the medicine for preventing and treating untoward reactions in radiotherapy and chemotherapy of tumor, the dihydromyricetin can inhibit and alleviate chemical damage, prevent and treat damage of a mutagen and further prevent gene mutation or the secondary tumors; and by combination with the radiotherapy and chemotherapy, the effects of preventing untoward reactions in radiotherapy and chemotherapy of tumor and preventing generation of tumors are achieved.

Description

technical field [0001] The present invention relates to a new medical application of dihydromyricetin, in particular to a medicine for preventing and treating adverse reactions and toxic side effects of tumor radiotherapy and chemotherapy, preventing tumor occurrence and tumor metastasis, and preventing and treating concurrent infection diseases in tumor treatment. Background technique [0002] Dihydromyricetin (dihydromyricetin), also known as staphylophyllin, the scientific name is 3, 5, 7, 3`, 4`, 5`-hexahydroxyflavone. Dihydromyricetin is a known compound, and the document Walter Karrarr, Birkhauser Verlag undStuttgart (1958), P.652, NO: 1640 announced that its structural formula is: [0003] [0004] Application No. 03123879 discloses the use of a composition containing dihydromyricetin and myricetin in the preparation of broad-spectrum antiviral drugs and the preparation of immunity-enhancing drugs; Application No. 200410062289 discloses the use of staphylosin in t...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P39/02A61P35/00
Inventor 张晓元郭勇
Owner SOUTH CHINA UNIV OF TECH
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