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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., can solve the problems of high toxicity and patient intolerance

Inactive Publication Date: 2012-07-11
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

[0048] Example 1 The combination of different ratios of artesunate and ABT-263 synergistically promotes Hep3B cell death test, see Table 2.

[0049] Table 2

[0050]

[0051] In an experiment investigating the cell death of the 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, 2.0 μM ABT-263 or lower concentration were used alone; When the two are used in combination at a lower concentration (7.5μM artesunate+1.5μM ABT-263), a significant synergistic effect is produced, resulting in 39% of cancer cell deaths; when the two are used at 10.0μM artesunate+2.0 When the proportion of μM ABT-263 is used together, it produces a more significant synergistic effect, resulting in 59% of cancer cells death.

Embodiment 2

[0052] Example 2 The combination of different ratios of dihydroartemisinin and ABT-263 synergistically promotes Hep3B cell death test, see Table 3.

[0053] table 3

[0054]

[0055]

[0056] In an experiment investigating 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 lower concentration, 2.0 μM ABT-263 or lower concentration were used alone; and When the two are used in combination at a lower concentration (7.5μM dihydroartemisinin + 1.5μM ABT-263), a significant synergistic effect is produced, causing 42% of cancer cells to die; when the two are used at 10.0μM dihydroartemisinin When combined with the ratio of ABT-263 and 2.0μM ABT-263, it produces a more significant synergistic effect, resulting in the death of 63% of cancer cells.

Embodiment 3

[0057] Example 3 The combination of different ratios of artesunate and ABT-263 synergistically promotes U2-OS cell death test, see Table 4.

[0058] Table 4

[0059]

[0060] In an experiment to investigate related compounds that cause cell death in the sarcoma cell line U2-OS, it was found that only about 20% of the cells died when 10.0μM artesunate was used alone, and only a small amount when 2.0μMABT-263 or lower was used alone. When the two are used in combination at a lower concentration (7.5μM artesunate + 1.5μM ABT-263), a significant synergistic effect results in the death of 44% of cancer cells; when the two are used at 10.0μM When the ratio of artesunate + 2.0 μM ABT-263 is used in combination, a more significant synergistic effect is 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 a medicine for treating cancer, in particular to a pharmaceutical composition containing artemisinin, artemisinin derivatives and a Bcl-2 inhibitor and its preparation for the treatment of colon cancer , Liver cancer, lung cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer or prostate cancer. Background technique [0002] The World Health Organization survey report 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 per year to 15 million, and the number of deaths due to cancer will increase from 6 million to 10 million per year. Primary liver cancer is a carcinogenesis that occurs in liver cells and intrahepatic bile duct epithelial cells. It is one of the most common malignant tumors in humans. The onset of c...

Claims

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Application Information

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