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Drug compound of apigenin, apigenin-like derivants, artemisinin and artemisinin-like derivants and application thereof

The technology of a derivative, apigenin, is applied to the pharmaceutical composition containing apigenin and apigenin derivatives, artemisinin and artemisinin derivatives and its application field, which can solve the problem of patient intolerance and high toxicity And other issues

Inactive Publication Date: 2012-05-09
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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  • Drug compound of apigenin, apigenin-like derivants, artemisinin and artemisinin-like derivants and application thereof
  • Drug compound of apigenin, apigenin-like derivants, artemisinin and artemisinin-like derivants and application thereof
  • Drug compound of apigenin, apigenin-like derivants, artemisinin and artemisinin-like derivants and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 The combination of different ratios of artesunate and apigenin synergistically promotes the death of H460 cells, see Table 2.

[0044] Table 2

[0045]

[0046]

[0047] In the experiment of investigating the death of lung cancer cell line H460 cells caused by related compounds, it was found that about 25% of the cells died when 10.0 μM artesunate or 30.0 μM apigenin were used alone; and when the two were used in combination at lower concentrations (7.5 μM artesunate + 25.0 μM apigenin) produced a more obvious synergistic effect, resulting in the death of about 40% of cancer cells; when the two were combined in the ratio of 10.0 μM artesunate + 30.0 μM apigenin A more significant synergistic effect was produced, leading to the death of 73% of cancer cells.

Embodiment 2

[0048] Example 2 The combination of different ratios of dihydroartemisinin and apigenin synergistically promotes the death of H460 cells, see Table 3.

[0049] table 3

[0050]

[0051] In the experiment of investigating the death of lung cancer cell line H460 caused by related compounds, it was found that about 25% of the cells died when 10.0 μM dihydroartemisinin or 30.0 μM apigenin were used alone; When used (7.5μM dihydroartemisinin+25.0μM apigenin), then produce obvious synergistic effect, cause 42% cancer cells to die; When used, a more significant synergistic effect was produced, leading to the death of 77% of cancer cells.

Embodiment 3

[0052] Example 3 The combination of different ratios of artesunate and apigenin synergistically promotes the death of Panc-1 cells, see Table 4.

[0053] Table 4

[0054]

[0055] In the experiment of investigating the death of pancreatic cancer cell line Panc-1 cells caused by related compounds, it was found that only about 20% of the cells died when 7.5 μM artesunate and 25.0 μM apigenin were used alone; (5.0 μ M artesunate + 20.0 μ M apigenin) then produced a significant synergistic effect, resulting in the death of 61% of cancer cells; Produced a more significant synergistic effect, resulting in the death of 92% of cancer cells.

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Abstract

The invention relates to a drug compound of apigenin, apigenin-like derivants, artemisinin and artemisinin-like derivants and application thereof in the preparation of drugs for curing lung cancer, pancreas cancer, colon cancer, liver cancer, prostate gland cancer, kidney cancer, stomach cancer, encephaloma, sarcoma, ovarian cancer or breast cancer. The drug compound has a remarkable coordination effect, improves the curative effect of the drugs, reduces the drug dosage, and reduces the side effects.

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 apigenin and apigenin derivatives, artemisinin and artemisinin derivatives and its preparation Use in a drug for the treatment of lung cancer, pancreatic cancer, colon cancer, liver cancer, prostate cancer, kidney cancer, stomach cancer, brain tumor, sarcoma, 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, lung cancer is one of the common malignant tumors. It originates from the bronchial epithelium at all levels and is divided into ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/366A61K31/352A61K31/357A61P35/00
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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