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Pharmaceutical composition containing artemisinin, artemisinin derivatives and histon deacetylase (HDAC) inhibitor and application thereof

A technology of sirtuin and artemisinin, which is applied in drug combinations, active ingredients of heterocyclic compounds, medical preparations containing active ingredients, etc., can solve problems such as high toxicity and patient intolerance

Inactive Publication Date: 2010-06-30
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 histon deacetylase (HDAC) inhibitor and application thereof
  • Pharmaceutical composition containing artemisinin, artemisinin derivatives and histon deacetylase (HDAC) inhibitor and application thereof
  • Pharmaceutical composition containing artemisinin, artemisinin derivatives and histon deacetylase (HDAC) inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Example 1 The combination of different ratios of artesunate (ART) and SAHA synergistically promotes the death of HepG2 cells, see Table 2.

[0065] Table 2

[0066]

[0067] In the experiment investigating the cell death of liver cancer cell line HepG2 caused by related compounds, it was found that when 5.0 μM artesunate or lower concentration and 2.0 μM SAHA or lower concentration were used alone, there was only a small amount of cell death; When the concentration of artesunate reached 10.0μM, only about 20% of the cells died; and when the two were used together at a lower concentration (5.0μM artesunate + 1.0μM SAHA), there was an obvious synergistic effect, resulting in About 50% of the cancer cells died; when the two were combined at the ratio of 10.0 μM artesunate + 2.0 μM SAHA, a more significant synergistic effect was produced, resulting in the death of 99% of the cancer cells.

Embodiment 2

[0068] Example 2 The combination of different ratios of dihydroartemisinin (DHA) and SAHA synergistically promotes the death of HepG2 cells, see Table 3.

[0069] table 3

[0070]

[0071] In the experiment investigating the cell death of liver cancer cell line HepG2 caused by related compounds, it was found that when 2.5 μM dihydroartemisinin, 2.0 μM SAHA or lower concentrations were used alone, only a small amount of cell death occurred; even if the concentration of the single drug was increased to At 10.0 μM dihydroartemisinin, only about 20% of the cells died; and when the two were used together at a lower concentration (5.0 μM dihydroartemisinin + 1.0 μMSAHA), there was an obvious synergistic effect, resulting in about 45 % of cancer cells died; when the two were combined at the ratio of 10.0 μM dihydroartemisinin + 2.0 μM SAHA, a more significant synergistic effect was produced, resulting in the death of 99% of cancer cells.

Embodiment 3

[0072] Example 3 The combination of different ratios of artesunate (ART) and SAHA synergistically promotes the death of 22RV1 cells, see Table 4.

[0073] Table 4

[0074]

[0075] In the experiment of examining the cell death of the prostate cancer cell line 22RV1 caused by related compounds, it was found that only about 15% of the cells died when 10.0 μM artesunate or lower concentration and 1.0 μM SAHA or lower concentration were used alone; When the drug concentration reaches 1.5μM SAHA, only about 20% of the cells die; and when the two are used together at a lower concentration (5.0μM artesunate + 1.0μM SAHA), there is an obvious synergistic effect, resulting in about 40 % of cancer cells died; when the two were combined at the ratio of 10.0 μM artesunate + 1.5 μM SAHA, a more obvious synergistic effect was produced, resulting in the death of about 90% of cancer cells.

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Abstract

The invention relates to a pharmaceutical composition containing artemisinin, artemisinin derivatives and a histon deacetylase (HDAC) inhibitor and an application thereof to prepare medicines for treating intestinal cancer, liver cancer, lung cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer, prostate cancer or leukaemia. The pharmaceutical composition of the invention has obvious synergistic effect, thus improving curative effect of medicines, lowering administration dosage and reducing occurrence of side effect.

Description

technical field [0001] The invention relates to a pharmaceutical composition and its application in the preparation of medicines for treating cancer, in particular to a pharmaceutical composition containing artemisinin, artemisinin derivatives and histone deacetylase inhibitors and its preparation Application in drugs for the treatment of colon cancer, liver cancer, lung cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer, prostate cancer or leukemia. 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. Among them, lung cancer is one of the common malignant tumors. It originates from bronchial epithelium at all levels and is div...

Claims

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Application Information

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IPC IPC(8): A61K31/357A61K45/00A61P35/00A61K31/16A61K31/404A61K31/44
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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