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Pharmaceutical composition containing artemisinin, artemisinin derivatives and Bcl-2 inhibitor and application thereof

A technology of bcl-2 and artemisinin, which is applied in the direction of drug combination, medical preparations containing active ingredients, antineoplastic drugs, etc.

Inactive Publication Date: 2014-05-07
DINKUM INT INVESTMENT HONG KONG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are many anti-tumor drugs on the market, such as alkylating agent drugs, antimetabolite drugs, anti-tumor antibiotics, immunomodulators, etc., but most of the drugs are more toxic due to large, patient intolerance

Method used

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  • Pharmaceutical composition containing artemisinin, artemisinin derivatives and Bcl-2 inhibitor and application thereof
  • Pharmaceutical composition containing artemisinin, artemisinin derivatives and Bcl-2 inhibitor and application thereof
  • Pharmaceutical composition containing artemisinin, artemisinin derivatives and Bcl-2 inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 The combination of different ratios of artesunate and ABT-263 synergistically promotes the death of Hep3B cells, see Table 2.

[0050] Table 2

[0051]

[0052] In the experiment of examining the cell death of liver cancer cell line Hep3B caused by related compounds, it was found that only about 10% of the cells died when 10.0 μM artesunate or lower concentration and 2.0 μM ABT-263 or lower concentration were used alone; When the two were used together at a lower concentration (7.5 μM artesunate + 1.5 μM ABT-263), they produced an obvious synergistic effect, resulting in the death of 39% of cancer cells; when the two were combined with 10.0 μM artesunate + 2.0 When the ratio of μM ABT-263 was combined, a more significant synergistic effect was produced, resulting in the death of 59% of cancer cells.

Embodiment 2

[0053] Example 2 The combination of different ratios of dihydroartemisinin and ABT-263 synergistically promotes the death of Hep3B cells, see Table 3.

[0054] table 3

[0055]

[0056]

[0057] In the experiment of examining the cell death of the liver cancer cell line Hep3B caused by related compounds, it was found that only about 13% of the cells died when 10.0 μM dihydroartemisinin or a lower concentration, 2.0 μM ABT-263 or a lower concentration was used alone; When the two were used together at a lower concentration (7.5 μM dihydroartemisinin + 1.5 μM ABT-263), there was an obvious synergistic effect, resulting in the death of 42% of cancer cells; when the two were combined with 10.0 μM dihydroartemisinin When the ratio of ABT-263 + 2.0μM ABT-263 was combined, a more significant synergistic effect was produced, resulting in the death of 63% of cancer cells.

Embodiment 3

[0058] Example 3 The combination of different ratios of artesunate and ABT-263 synergistically promotes the death of U2-OS cells, see Table 4.

[0059] Table 4

[0060]

[0061] In the experiment of investigating the death of the sarcoma cell line U2-OS cells caused by related compounds, it was found that only about 20% of the cells died when 10.0 μM artesunate was used alone, and only a small amount was only a small amount when 2.0 μM ABT-263 or lower concentrations were used alone. cell death; and when the two were combined at a lower concentration (7.5 μM artesunate + 1.5 μM ABT-263), there was an obvious synergistic effect, resulting in the death of 44% of cancer cells; when the two were combined at 10.0 μM When the ratio of artesunate + 2.0μM ABT-263 was combined, a more significant synergistic effect was produced, resulting in the death of 76% of cancer cells.

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Abstract

The invention relates to a pharmaceutical composition containing artemisinin, artemisinin derivatives and a Bcl-2 inhibitor and application of the pharmaceutical composition in preparing medicines used for treating colorectal carcinoma, liver cancer, lung cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, pancreas cancer, ovarian cancer, breast cancer or prostate cancer. The pharmaceutical composition provided in the invention has a remarkable synergistic effect, improves curative effects of drugs and reduces administration dosage and possibility of occurrence of side effects.

Description

technical field [0001] The invention relates to a pharmaceutical composition and its application in the preparation of drugs for treating cancer, in particular to a pharmaceutical composition containing artemisinin, artemisinin derivatives and Bcl-2 inhibitors and its application in the preparation of drugs for treating colon cancer , liver cancer, lung cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer or prostate cancer. Background technique [0002] The survey report of the World Health Organization shows that the global cancer situation is getting worse. In the next 20 years, the number of new patients will increase from the current 10 million to 15 million per year, and the number of deaths from cancer will also increase from 6 million to 10 million per year. Primary liver cancer is a cancer that occurs in liver cells and intrahepatic bile duct epithelial cells, and is one of the most common malignant tumors in...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/366A61K31/357A61K31/5377A61K31/495A61P35/00
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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