Application of rutin medicines to preparing medicines for preventing or treating medicine-induced cardiac toxicity

A cardiotoxicity and cardiotoxicity technology, applied in the directions of drug combinations, pharmaceutical formulations, organic active ingredients, etc., can solve the problem of prevention or treatment. There are no reports or inspirations, no research reports on the cardiotoxicity of rutin drugs, and different pathogenic factors, etc. question

Inactive Publication Date: 2017-09-26
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Sun Bo et al. ("Experimental Animal Science", Volume 31, Issue 1, February 2014) published "Effect of Rutin on ROCK I Protein in Rat Diabetic Cardiomyopathy", and diabetic cardiomyopathy and drugs especially Cardiotoxicity caused by antineoplastic drugs belongs to different clinical diseases, with different pathogenesis, course of disease, pathological changes, characteristics of cardiac function changes, and treatment principles. There is no report or inspiration on whether it has a preventive or therapeutic effect on drug-induced cardiotoxicity
[0013] Mandziuk S et al. ("Drug Chem Toxicol" 38 (1): 1-8. January 2015) disclosed "The protective effect of Mutellina purpurea polyphenolic compounds on doxorubicin-induced H9c2 cardiomyocyte toxicity", which disclosed that Mutellina purpurea polyphenols The protective effects of phenolic compounds on delayed cardiomyopathy were compared in this paper by comparing doxorubicin combined with LH8, quercetin, rutin and chlorogenic acid to treat H9c2 cardiomyocytes to observe the morphological changes and the results of MTT experiments. The results suggest that: The antioxidative effect of Ding is clear, but it has no effect on the reduction of cardiomyocyte activity induced by doxorubicin (that is, it has no protective effect on the damage of cardiomyocytes induced by doxorubicin). The author finally proposes that more extensive experimental research is needed to carry out Therefore, the literature did not draw a clear conclusion on whether rutin has a protective effect on doxorubicin-induced delayed cardiotoxicity
[0014] The inventor tracked the progress of related research and found that no rutin-like drugs have been found for drug-induced cardiotoxicity, especially pirarubicin or epirubicin-induced cardiotoxicity.

Method used

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  • Application of rutin medicines to preparing medicines for preventing or treating medicine-induced cardiac toxicity
  • Application of rutin medicines to preparing medicines for preventing or treating medicine-induced cardiac toxicity
  • Application of rutin medicines to preparing medicines for preventing or treating medicine-induced cardiac toxicity

Examples

Experimental program
Comparison scheme
Effect test

experiment example

[0054] The combination of rutin and anthracycline in different doses was prepared according to the ratio in Table 1 below.

[0055] For the liquid combination of rutins in Examples 1 to 32, rutins and anthracyclines of corresponding concentrations can be prepared into the same solution, and then used directly when administered; they can also be made into corresponding Concentration solutions are then mixed and used directly during administration; they can also be administered after mixing during use, or administered to subjects separately, and the sequence of their administration is not limited.

[0056] For the combination of rutin drugs administered through the gastrointestinal tract in Examples 1-32, the corresponding quality of rutin drugs and anthracycline drugs can be directly mixed and taken at the same time; they can also be made into unit preparations respectively , administered to the subject at the same time, or sequentially, but the order of use between them is not...

experiment example 1

[0068] Experimental example 1 in vitro test

[0069] 1.1.1 The effect of different proportions of rutin on the inhibitory rate of H9c2 cells (MTT method)

[0070] experiment method:

[0071]H9c2 cardiomyocytes were seeded in 96-well culture plates. When the cells grew to about 80% of the culture well area, different treatments were carried out according to the needs of the experiment: (1) 10, 30, 50, 70 and 100 μmol / L different concentrations of Rutin (Rutin) was pretreated for 1 hour, discarded, washed twice with PBS, and cultured with 5 μmol / L pirarubicin for 24 hours; L-pirarubicin was cultured for 24 hours; 8 replicate wells were set up for each treatment factor. After terminating the culture, add 10 μL MTT to each well, shake gently, and incubate at 37°C. Then measure cell inhibition rate=(1-OD value of experimental group / OD value of control group)×100%. The measurement results are shown in Table 2 and figure 1 .

[0072] Data statistics The SPSS 17.0 software was u...

experiment example 2

[0087] Experimental example 2 in vivo test

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Abstract

The invention relates to the field of pharmacy, and particularly provides application of rutin medicines to preparing medicines for preventing or treating medicine-induced cardiac toxicity. The rutin medicines comprise rutin or troxerutin, and the medicine-induced cardiac toxicity refers to cardiac toxicity due to application of antitumor anthracycline medicines and preferably refers to cardiac toxicity due to application of pirarubicin or epirubicin. The application has the advantages that the cardiac toxicity of subjects due to the anthracycline medicines can be effectively prevented or treated by the medicines, and toxic and side effects of the medicines can be lowered.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to the application of a rutin drug in the preparation of a drug for preventing or treating drug-induced cardiotoxicity. Background technique [0002] Tumor disease is currently one of the frequently-occurring diseases of human beings, which has brought great pain to patients. At present, chemotherapy is the main treatment for tumors. Pain other than the disease itself, mild such as headache, nausea, fatigue, severe such as hair loss, liver and kidney and heart toxicity and so on. [0003] Anthracyclines, such as epirubicin and pirarubicin, have been widely used in the treatment of hematological malignancies and solid tumors, such as breast cancer, lymphoma, and acute leukemia. It has good effect on anti-tumor. The 2014 "NCCN Guidelines for Breast Cancer" recommended that the preferred adjuvant chemotherapy regimen for breast cancer is AC×4→T(P)×4 (erubicin, pirarubicin / cyclophosphamide-pac...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P9/00A61P9/04
CPCA61K31/7048
Inventor 任立群王亚帝胡彦武李相军孙波苗春生张洋
Owner 任立群
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