Pharmaceutical composition containing apigenin, apigenin derivative, rubescensin and rubescensin derivative, and application thereof

A technology of oridonin A and its derivatives, which can be applied in drug combinations, medical preparations containing active ingredients, antineoplastic drugs, etc., and can solve problems such as high toxicity and patient intolerance

Inactive Publication Date: 2012-09-26
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 apigenin, apigenin derivative, rubescensin and rubescensin derivative, and application thereof
  • Pharmaceutical composition containing apigenin, apigenin derivative, rubescensin and rubescensin derivative, and application thereof
  • Pharmaceutical composition containing apigenin, apigenin derivative, rubescensin and rubescensin derivative, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 The combination of different ratios of apigenin and Rubescensin A synergistically promotes the death of HCT-116 cells, see Table 2.

[0047] Table 2

[0048]

[0049] In the experiment of investigating the cell death of colon cancer cell line HCT-116 caused by related compounds, it was found that when 20.0 μM apigenin was used alone, about 23% of the cells died, and when 15.0 μM oridonin was used alone, about 14% of the cells died; And when the two were used in combination at a lower concentration (15.0 μM apigenin+10.0 μM oridonin), a significant synergistic effect was produced, resulting in the death of 57% of cancer cells; When the ratio of μM Rubescensine A is combined, a more significant synergistic effect is produced, resulting in the death of 99% of cancer cells.

Embodiment 2

[0050] Example 2 The combination of different ratios of apigenin and Rubescensin A synergistically promotes the death of HUH-7 cells, see Table 3.

[0051] table 3

[0052]

[0053] In the experiment of investigating the cell death of liver cancer cell line HUH-7 caused by related compounds, it was found that when 25.0 μM apigenin was used alone, there was almost no cell death, and when 15.0 μM oridonin was used alone, less than 10% of the cells died and when the two were used in combination at lower concentrations (15.0 μM apigenin+10.0 μM oridonin) then produced a significant synergistic effect, resulting in the death of 61% of cancer cells; When the ratio of 15.0 μM oridonin was used together, a more significant synergistic effect was produced, resulting in the death of 99% of cancer cells.

Embodiment 3

[0054] Example 3 The combination of different ratios of apigenin and Rubescensin A synergistically promotes the death of SK-Hep-1 cells, see Table 4.

[0055] Table 4

[0056]

[0057]

[0058]In the experiment of investigating the cell death of liver cancer cell line SK-Hep-1 caused by related compounds, it was found that when 25.0 μM apigenin was used alone or 15.0 μM oridonin was used alone, about 10-15% of the cells died; When the two were used in combination at lower concentrations (20.0 μM apigenin+10.0 μM oridonin), a more obvious synergistic effect was produced, resulting in the death of 43% of cancer cells; When the ratio of oridonin A is used in combination, a more significant synergistic effect is produced, resulting in the death of 81% of cancer cells.

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Abstract

The present invention relates to a pharmaceutical composition containing apigenin, an apigenin derivative, rubescensin, and a rubescensin derivative, and applications of the pharmaceutical composition for preparing pharmaceuticals to cure lung cancer, pancreas cancer, colorectal carcinoma, liver cancer, prostate cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, mesothelioma, head and neck squamous cancer, ovary cancer or breast cancer. The pharmaceutical composition has an obvious synergistic effect, increases the pharmic curative effect, reduces the administration dosage and reduces the adverse reactions.

Description

technical field [0001] The present invention relates to a pharmaceutical composition and its application in the preparation of medicines for treating cancer, in particular to a pharmaceutical composition containing apigenin and apigenin derivatives, oridonin and oridonin derivatives Its application in the preparation of medicines for treating lung cancer, pancreatic cancer, colon cancer, liver cancer, prostate cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, mesothelioma, head and neck squamous carcinoma, ovarian cancer or breast 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. Among them, primary liver cancer is a cancer that occurs in liver cells and intrahepa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61P35/00
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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