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Medical composition of didemethyl tetrandrine dual ethyl formate and tyrosine kinase inhibitor

A technology of ethyl bisformate and tyrosine kinase, which is applied in the field of medicine and can solve problems such as treatment failure

Active Publication Date: 2019-07-19
CHONGQING MEDICAL & PHARMA COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sorafenib is clinically used to treat kidney cancer, thyroid cancer and liver cancer. In the 10 years since it was approved for the treatment of advanced liver cancer in 2007, it has been the only gold standard drug for the treatment of advanced liver cancer. However, a large number of patients have developed drug resistance during treatment. or serious adverse reactions that require withdrawal or reduction of treatment, leading to treatment failure (CHENGAL et al., Lancet Oncol, 2009, 10(1):25-34; WOO HY et al., Expert Opin Pharmacother, 2017, 18(1):35 -44)

Method used

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  • Medical composition of didemethyl tetrandrine dual ethyl formate and tyrosine kinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Synergistic sensitization effect of W18 combined with sorafenib on cytotoxicity of intrinsically drug-resistant hepatocellular carcinoma Bel7402

[0027] Bel7402 cells in the logarithmic growth phase were digested with trypsin, mixed evenly, and seeded in a 96-well culture plate at a seeding concentration of 1200 cells / well. After culturing for 24 hours, add Sorafenib (1.0 μM, 10 μM, 25 μM), or W18 (0.25 μM, 0.5 μM, 1.0 μM, 3.0 μM), or a combination of the two drugs, and set 3 parallel wells for each drug concentration . After continuing to cultivate for 72 hours, discard the culture medium, add 0.5 mg / ml MTT 100 μl (dissolved in serum-free RPMI1640 culture solution) to each well, continue to cultivate for 4 hours, discard MTT, add 150 μl of DMSO to each well, shake with a mixing shaker, and use a microplate reader Measure the absorbance value at the wavelength of 570nm, and calculate the cytotoxicity (inhibition rate) with the following formula: inhibition rate (%)=(1...

Embodiment 2

[0032] Synergistic sensitization effect of W18 combined with regorafenib on cytotoxicity of acquired drug-resistant hepatocellular carcinoma HepG2 / sor

[0033] HepG2 / sor cells in the logarithmic growth phase were digested with trypsin, mixed evenly, and inoculated in a 96-well culture plate at a seeding concentration of 2000 cells / well. After culturing for 24 hours, add regorafenib (1.0 μM, 10 μM, 25 μM), or W18 (0.25 μM, 0.5 μM, 1.0 μM, 3.0 μM), or a combination of the two drugs, and set 3 parallel wells for each drug concentration . After continuing to cultivate for 72 hours, discard the culture medium, add 0.5 mg / ml MTT 100 μl (dissolved in serum-free RPMI1640 culture solution) to each well, continue to cultivate for 4 hours, discard MTT, add 150 μl of DMSO to each well, shake with a mixing shaker, and use a microplate reader Measure the absorbance value at the wavelength of 570nm, and calculate the cytotoxicity (inhibition rate) with the following formula: inhibition rate...

Embodiment 3

[0039] Synergistic inhibitory effect of W18 combined with sorafenib on the proliferation of Bel7402 single cells

[0040] For Bel7402 cells in exponential growth phase, make cell suspension. Cells were counted, and the cell concentration was adjusted with medium, ready for use. Dilute the cell suspension several times, and inoculate 5ml of the cell suspension into culture dishes (diameter 60mm) according to the concentration of 200 cells per dish, and gently shake the culture dish in a cross direction to make the cells evenly dispersed. Place the Petri dish at 37°C, 5% CO 2 After culturing for 24 hours, the cells adhered to the wall, added Sorafenib (1.0 μM, 10 μM, 25 μM), or W18 (0.25 μM, 0.5 μM, 1.0 μM, 3.0 μM), or a combination of the two drugs, and cultured for another 2 to 3 weeks. When clones were visible to the naked eye in the culture dish, the culture was terminated, the culture medium was discarded, carefully soaked twice in PBS solution, and air-dried. Fix with m...

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Abstract

The invention relates to the technical field of medicines, specifically discloses a medical composition of didemethyl tetrandrine dual ethyl formate (W18) and a tyrosine kinase inhibitor and the use of the medical composition for treating medicine-resisting liver cancer. Particularly, a medical composition of didemethyl tetrandrine dual ethyl formate (W18) and sorafenib or regorafenib has the effects of synergistically increasing sensitivity and reversing medicine resistance in the respect of treating drug tolerance liver cancer, and can significantly increase the treatment effects of treatingthe drug tolerance liver cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a pharmaceutical composition of bis-demethyl tetrandrine dicarboxylate and a tyrosine kinase inhibitor and its application in treating drug-resistant liver cancer, especially bis-demethyl A pharmaceutical composition of tetrandrine ethyl dicarboxylate and sorafenib or regorafenib and its use for treating drug-resistant liver cancer. Background technique [0002] Malignant tumor is one of the major diseases that seriously threaten human life and health, and has become the second leading cause of death for human beings. Some tumors represented by lung cancer, pancreatic cancer, liver cancer and cholangiocarcinoma have primary drug resistance at the beginning of treatment and the emergence of acquired drug resistance during the treatment of most tumors, leading to tumor progression, recurrence and metastasis, and eventually Leading to treatment failure is the main reason for the f...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61K31/4748A61P35/00
CPCA61K31/44A61K31/4748A61P35/00A61K2300/00
Inventor 刘小东张稳稳
Owner CHONGQING MEDICAL & PHARMA COLLEGE
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