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A kind of antitumor pharmaceutical composition and application thereof

A composition and anti-tumor technology, applied in the direction of anti-tumor drugs, drug combinations, medical preparations containing active ingredients, etc., can solve the problems that have not yet been reported on harpagoside anti-tumor drug combinations, and achieve cardiotoxicity relief Effect

Active Publication Date: 2022-04-15
BEIJING UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] At present, there is no report on the combination of harpagoside and other antineoplastic drugs

Method used

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  • A kind of antitumor pharmaceutical composition and application thereof
  • A kind of antitumor pharmaceutical composition and application thereof
  • A kind of antitumor pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0052] Experimental Example 1: Detection of resistance to doxorubicin-induced cardiotoxicity

[0053] 1. Animals and groups

[0054] Mice were purchased from SPEF (Beijing) Biotechnology Co., Ltd.

[0055] After 3 days of adaptive feeding, the mice were randomly divided into normal saline group (Control), doxorubicin group (DOX), doxorubicin+harpagoside group (DOX+HAR), doxorubicin+enalapril group Positive drug group (DOX+ENA) and other 4 groups.

[0056]Both basic and clinical studies have shown that enalapril can reduce doxorubicin-induced cardiotoxicity and improve cardiac function, so it is used as a positive control drug in mouse experiments.

[0057] 2. Preparation of doxorubicin-induced cardiotoxicity model

[0058] After the mice (18-20g) were fixed, they were injected with doxorubicin into the tail vein, the injection concentration was 10 mg / mL, and the injection dose was 5 mg / kg, once every 7 days for 4 consecutive weeks. The normal saline group was injected with...

experiment example 2

[0111] Experimental example 2: Detection of anti-tumor activity

[0112] 1. Test method: Different tumor cells, including liver cancer cells (HepG2 cells) and breast cancer cells (MCF-7 cells), were tested with 8*10 4 The cells were inoculated into 96-well plates (100 μl / well) at a density of / mL, cultured for 24 hours, and then stimulated according to the following groupings. After 24 hours, the cell viability was detected by a microplate reader using the CCK8 method.

[0113] 2. Test groups:

[0114] Group 1: normal group (Control), HAR 50μmol / L, HAR 80μmol / L, HAR 100μmol / L, HAR150μmol / L, HAR 200μmol / L;

[0115] Group 2: Normal group (Control), DOX 1 μmol / L, DOX 1 μmol / L+HAR 50 μmol / L, DOX 1 μmol / L+HAR 80 μmol / L, DOX 1 μmol / L+HAR 100 μmol / L, DOX 1 μmol / L+HAR 150μmol / L, DOX 1μmol / L+HAR 200μmol / L.

[0116] 3. Detection index: The OD value detected by the microplate reader represents the cell viability.

[0117] 4. Statistical method: Graphpad Prism 6.0 was used for data proc...

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PUM

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Abstract

The present invention relates to the field of pharmaceutical compositions, in particular to an anti-tumor pharmaceutical composition and its application. The pharmaceutical composition comprises the following ingredients in parts by weight: 1-10 parts of doxorubicin and 10-200 parts of harpagoside. The invention also provides the application of the pharmaceutical composition in the preparation of anti-tumor drugs. The applicant unexpectedly found that harpagoside itself has no anti-tumor effect, but when harpagoside is combined with doxorubicin, it can be used to treat breast cancer and liver cancer, and the combined effect of the two is better than that of doxorubicin alone. It is confirmed that the two have a synergistic anticancer effect, and at the same time, harpagoside can also alleviate the cardiotoxicity caused by the anticancer drug doxorubicin.

Description

technical field [0001] The invention relates to the field of pharmaceutical compositions, in particular to an anti-tumor pharmaceutical composition and its application. Background technique [0002] The anthracycline antibiotic doxorubicin (doxorubicin, DOX, molecular weight: 543.519) is widely used as an effective chemotherapy drug in various cancers, such as leukemia, solid tumors, soft tissue sarcoma and breast cancer. However, the dose-dependent cardiotoxicity of DOX severely limits its clinical application. Doxorubicin-induced cardiotoxicity ranges from asymptomatic decreased left ventricular ejection fraction (LVEF), tachycardia and arrhythmias, and cardiomyopathy to myocardial infarction and severe congestive heart failure (grades III to IV). [0003] Dexrazoxane (DRX) is currently the only cardioprotective agent approved by the US Food and Drug Administration (FDA) in combination with DOX for the treatment of cancer. However, it was reported that dexrazoxane could ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61P35/00A61P9/00A61K31/704
CPCA61K31/704A61K31/7048A61P35/00A61P9/00A61K2300/00
Inventor 王勇李伟利王晓平张亚雯江艳艳孙乾斌曹静姚骏凯王伟李春
Owner BEIJING UNIV OF CHINESE MEDICINE