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Application of compound F-C in preparation of product for preventing and/ or treating heart injury

A heart injury, F-C technology, applied in the field of medical use of flavonoids, can solve problems such as side effects, patient prognosis and adverse effects on rehabilitation, cardiotoxicity, etc.

Active Publication Date: 2021-02-19
CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, many drugs will cause side effects of cardiotoxicity during treatment, especially in the chemotherapy of malignant tumors, the cytostatics used will cause severe cardiotoxicity, which has a negative impact on the prognosis and rehabilitation of patients

Method used

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  • Application of compound F-C in preparation of product for preventing and/ or treating heart injury
  • Application of compound F-C in preparation of product for preventing and/ or treating heart injury
  • Application of compound F-C in preparation of product for preventing and/ or treating heart injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Therapeutic Effect of Example 1 Compound F-C on Doxorubicin-Induced Cardiotoxicity

[0041] Rabbit test method for doxorubicin-induced cardiomyopathy (this experiment complies with relevant ethical regulations):

[0042] (1) Test with two sexes of rabbits whose initial body weight is 2.3 ± 0.2kg, group a is untreated animals (for control animals, n=8), group b is animals treated with doxorubicin (+ replace test substance with placebo, n=8), group c is doxorubicin and test substance treated animals (n=8), test substance is flavonoids F-A, F-B, F-C, respectively c1, c2 , Group c3.

[0043] (2) Groups b and c administered intravenously twice a week with doxorubicin, 1 mg / kg each time, for a total of 4 weeks, and group c took orally administered the test substance 20 mg / kg body weight per day, starting from the first day of doxorubicin treatment To start, feed the feed at the same time.

[0044] (3) After 4 weeks, separate the heart and weigh it, and detect the content o...

Embodiment 2

[0051] Example 2 Therapeutic effect of compound F-C on doxorubicin-induced cardiotoxicity

[0052] Inhibition of cardiomyocyte apoptosis in the H9c2 cardiotoxicity model:

[0053] (1) After incubating H9c2 cells with different concentrations of flavonoids F-A, F-B, and F-C for 24 hours, the toxic effects of flavonoids on cardiomyocytes were evaluated by MTT colorimetry. H9c2 cells were incubated with flavonoids for 1 hour before adding 2.5 After cultured with μM DOX for 24 hours, MTT colorimetric method was used to screen the activity of flavonoids on doxorubicin (DOX)-induced cardiomyocyte apoptosis, and determine the optimal concentration range.

[0054] (2) After treating H9c2 cardiomyocytes with different seabuckthorn flavonoids for 1 hour, treat them with 2.5 μM DOX for 24 hours, then extract the protein, lyse, scrape, collect the cell lysate, centrifuge at 12000 g for 15 minutes, collect the supernatant and discard the precipitate, - Store at 80°C, and use BCA method to...

Embodiment 3

[0061] Embodiment 3 contains the tablet of flavonoid compound

[0062] The following ingredients are produced for each tablet:

[0063]

[0064] The above-mentioned components were mixed according to the stated dosage, granulated, blended and compressed into tablets to prepare 250 mg tablets.

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PUM

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Abstract

The invention discloses application of a compound F-C in preparation of a product for preventing and / or treating heart injury. Activity research is performed on the compound F-C, and the compound F-Cis verified to be capable of reducing the ratio of heart to body weight, inhibiting myocardial cell fibrosis by reducing the content of hydroxyproline, thereby inhibiting proliferation of a myocardial extracellular matrix, and obviously inhibiting cell apoptosis induced by myocardial toxicity; and the myocardial cytotoxicity of H9C2 is relieved by down-regulating the expression level of p-JNK and / or Cleaved-Caspase-3, so that the effect of preventing and / or treating the myocardial cytotoxicity is achieved, and the compound F-C can be used for preparing a drug for preventing or treating diseases related to the heart injury.

Description

technical field [0001] The invention relates to the field of medical application of flavonoids, in particular to the application of flavonoids F-C. Background technique [0002] At present, many drugs will cause side effects of cardiotoxicity during treatment, especially in the chemotherapy of malignant tumors, the cytostatics used will cause severe cardiotoxicity, which has a negative impact on the prognosis and rehabilitation of patients. [0003] According to reports, anthracyclines are generally cardiotoxic, and these drugs are widely used in clinic because of their good antitumor activity. Taking doxorubicin (DOX), the most widely used and most successful anthracycline antineoplastic drug, as an example, its accumulation and dose-dependent cardiomyocyte toxicity are the main problems that have plagued the practice of cancer treatment from drug development to clinical use. , manifested in its therapeutic dose greater than 550mg / m 2 The incidence of congestive heart fai...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P39/02A61P9/00
CPCA61K31/7048A61P39/02A61P9/00
Inventor 王洪伦周文娜胡娜
Owner CHINA ACAD OF SCI NORTHWEST HIGHLAND BIOLOGY INST
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