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Medicament composition containing tetrandrine, tetrandrine derivatives and histone deacetylase inhibitor and application thereof

A technology of sirtuin and tetrandrine, which is applied in the direction of drug combinations, medical preparations containing active ingredients, antineoplastic drugs, etc., can solve the problems of patient intolerance and high toxicity, reduce the dosage of drugs, reduce the Side Effects, Effects to Improve Curative Effects

Inactive Publication Date: 2010-09-22
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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  • Medicament composition containing tetrandrine, tetrandrine derivatives and histone deacetylase inhibitor and application thereof
  • Medicament composition containing tetrandrine, tetrandrine derivatives and histone deacetylase inhibitor and application thereof
  • Medicament composition containing tetrandrine, tetrandrine derivatives and histone deacetylase inhibitor and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1 The combination of different proportions of Tetrandrine and SAHA synergistically promotes the death of HepG2 cells, see Table 2.

[0052] Table 2

[0053]

[0054]

[0055] In the experiment investigating the cell death of liver cancer cell line HepG2 caused by related compounds, it was found that only a small amount of cell death was observed when 5.0 μM tetrandrine or lower concentration and 1.5 μM SAHA or lower concentration were used alone; When the concentration reaches 10.0 μM tetrandrine and 2.0 μM SAHA, only about 10-20% of the cells die; and when the two are used together at a lower concentration (5.0 μM tetrandrine + 1.5 μM SAHA), there is an obvious synergistic effect , resulting in the death of about 32% of cancer cells; when the two were used in combination at the ratio of 10.0 μM tetrandrine + 2.0 μM SAHA, a more significant synergistic effect was produced, resulting in the death of about 85% of cancer cells.

Embodiment 2

[0056] Example 2 The combination of different proportions of tetrandrine and LBH589 synergistically promotes the death of HepG2 cells, see Table 3.

[0057] table 3

[0058]

[0059]

[0060] In the experiment of investigating the cell death of the liver cancer cell line HepG2 caused by related compounds, it was found that when 5.0 μM tetrandrine, 0.015 μM LBH589 or lower concentrations were used alone, there was only a small amount of cell death; even if the concentration of the single drug was increased to 10.0 μM When tetrandrine and 0.025 μ M LBH589, only about 20% of the cells died; and when the two were used together at a lower concentration (5.0 μ M tetrandrine + 0.015 μ M LBH589), there was a more obvious synergistic effect, resulting in about 20% cell death Cancer cells die; when the two are combined at a ratio of 10.0 μM tetrandrine + 0.025 μM LBH589, a more significant synergistic effect is produced, resulting in the death of 91% of cancer cells.

Embodiment 3

[0061] Example 3 The combination of different proportions of tetrandrine and LBH589 synergistically promotes the death of PLC / PRF / 5 cells, see Table 4.

[0062] Table 4

[0063]

[0064] In an experiment investigating the death of liver cancer cell lines PLC / PRF / 5 caused by related compounds, it was found that only about 15% of the cells died when 5.0 μM tetrandrine, 0.015 μM LBH589 or lower concentrations were used alone; When the concentration reaches 7.5μM tetrandine and 0.025μMLBH589, only about 20-25% of the cells die; and when the two are used together at lower concentrations (5.0μM tetrandine + 0.015μMLBH589), a more obvious synergistic effect is produced. , resulting in the death of about 34% of cancer cells; when the two were combined in a ratio of 7.5μM tetrandine + 0.025μM LBH589, a more significant synergistic effect was produced, resulting in the death of 95% of cancer cells.

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Abstract

The invention relates to a medicament composition containing tetrandrine, tetrandrine derivatives and a histone deacetylase (HDAC) inhibitor and application thereof in preparing medicaments for treating colon cancer, liver cancer, lung cancer, stomach cancer, encephaloma, sarcoma, pancreatic cancer, ovarian cancer, breast cancer, prostatic cancer or glioma. The medicament composition has remarkable synergistic effect, improves the curative effect of the medicament, decreases the administration dosage and reduces the occurrence of 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 tetrandrine, tetrandrine derivatives and histone deacetylase inhibitors and its preparation Use in a drug 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 glioma. 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 divided into...

Claims

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Application Information

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IPC IPC(8): A61K31/4748A61K31/167A61K31/165A61K31/4045A61K31/4406A61P35/00
Inventor 赵镭
Owner DINKUM INT INVESTMENT HONG KONG
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