Anti-cancer drug-combination composition comprising compound F-A

An anti-cancer drug and a combined drug technology, applied in the field of medical use of flavonoids, can solve the problems of myocardial necrosis, no solution, congestive heart failure and the like

Pending Publication Date: 2021-01-19
HUZHOU TEACHERS COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chemotherapy drugs usually have toxic side effects such as bone marrow suppression, nausea, vomiting, stomatitis, hair loss, high fever, bleeding symptoms, phlebitis, and skin pigmentation. In addition to these side effects, anthracycline chemotherapy drugs also have dose-dependent cardiotoxicity. It is manifested as various arrhythmias, and myocardial necrosis or even congestive heart failure will occur when the cumulative dose is large, seriously affecting the physical condition of the patient
For this reason, people have been trying to find an effective way to reduce this type of toxicity, but there is still no ideal solution so far.

Method used

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  • Anti-cancer drug-combination composition comprising compound F-A
  • Anti-cancer drug-combination composition comprising compound F-A
  • Anti-cancer drug-combination composition comprising compound F-A

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The therapeutic effect of embodiment 1 compound F-A on doxorubicin-induced cardiotoxicity

[0037] Rabbit test method for doxorubicin-induced cardiomyopathy (this experiment complies with relevant ethical regulations):

[0038] (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.

[0039] (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.

[0040] (3) After 4 weeks, separate the heart and weigh it, and detect the co...

Embodiment 2

[0047] Therapeutic Effect of Example 2 Compound F-A on Doxorubicin-induced Cardiotoxicity

[0048] Inhibition of cardiomyocyte apoptosis in the H9c2 cardiotoxicity model:

[0049](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.

[0050] (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

[0057] Embodiment 3 contains the tablet of flavonoid compound

[0058] The following ingredients are produced for each tablet:

[0059]

[0060] 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 provides an anti-cancer drug-combination composition comprising a compound F-A. The composition comprises an anti-cancer drug with cardiotoxicity, and the compound F-A. An experiment proves that the compound F-A in the composition can inhibit a myocardial fibrosis process caused by the function of the anti-cancer drug, and myocardial extracellular matrix hyperplasia is inhibited; andmeanwhile, the compound F-A also has a good function of resisting the cardiotoxicity and can be used for preparing a product used for preventing and / or treating heart injuries caused by cardiotoxicity substances. The flavonoid compound F-A and the anthracene nucleus anti-cancer drug with the cardiotoxicity are jointly prepared, and the cardiotoxicity of the anthracene nucleus anti-cancer drug can be lightened in a treatment process of the drug which has a toxic side effect for the heart.

Description

technical field [0001] The present invention relates to the field of medical application of flavonoids, in particular to an anticancer combined drug composition comprising compound F-A. Background technique [0002] With the improvement of cancer diagnosis and treatment technology, chemotherapy has become the main adjuvant therapy for cancer. Anthracycline chemotherapy drugs such as doxorubicin are an important class of broad-spectrum anti-tumor drugs, which can treat more types of tumor diseases. Chemotherapy using anthracycline chemotherapy drugs is currently the most effective and widely used anti-cancer therapy. First, cancers that can be used for treatment include leukemia, lymphoma, breast cancer, uterine cancer, ovarian cancer and lung cancer. Its mechanism of action is mainly that the anthracycline planar structure of its molecule is inserted into the double-stranded structure of DNA molecule, which affects the function of DNA, inhibits DNA replication and RNA trans...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P35/00A61P35/02A61K31/136A61K31/704
CPCA61K31/7048A61K31/704A61P35/00A61P35/02A61K31/136A61K2300/00
Inventor 周文娜王洪伦胡娜欧阳健
Owner HUZHOU TEACHERS COLLEGE
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