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New application of total glucosides of paeony as EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor

A technology of tyrosine kinase and total glucosides of paeony, which is applied in the field of total glucosides of paeony as an EGFR tyrosine kinase inhibitor, can solve the problem of blood toxicity, gastrointestinal tract reactions, and patient treatment costs and loss of treatment opportunity due to tumor cell killing , Drugs lose their therapeutic effect and other problems, to achieve significant curative effect, low price, reduced expression and activation

Active Publication Date: 2014-02-05
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the application of a new generation of chemotherapeutic drugs has improved their curative effect to a certain extent in recent years, most data show that the side effects such as blood toxicity and gastrointestinal reactions caused by chemotherapeutic drugs on tumor cells are still the biggest reason for their in-depth and wide application. obstacle
The therapeutic effect of EGFR tyrosine kinase inhibitors on cancer has aroused people's attention. The tyrosine kinases currently on the market are very expensive, and ordinary patients cannot afford the huge cost of treatment and lose the opportunity for treatment. Moreover, studies have shown that such drugs Due to the single component, it will induce secondary mutations (acquired mutations) of EGFR tyrosine kinase molecules produced by tumor cells after administration, and drug resistance will cause this type of drug to lose its therapeutic effect
Total glucosides of paeony are non-toxic, cheap, and rich in resources. At present, there are no literature reports on the use of total glucosides of paeony as EGFR tyrosine kinase inhibitors.

Method used

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  • New application of total glucosides of paeony as EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor
  • New application of total glucosides of paeony as EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor
  • New application of total glucosides of paeony as EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 Western blot experiment

[0019] Take lung cancer cells A549, H1299, and H1650 logarithmic growth phase cells, and prepare 9×10 cells with RPMI1640-5% FBS medium 4 cells / mL single cell suspension, inoculated in 10cm culture dish, 10mL per well, and set the cell suspension without sample as negative control.

[0020] The total glucosides of paeony and gefitinib were prepared to the required concentration with the culture solution, the original culture solution was sucked away with a vacuum pump, and the culture solution containing different concentrations of drugs was added to the culture dish, 10mL per dish; the control group was added with RPMI1640 -5% FCS medium, cultivated for 72 hours.

[0021] After 72 hours, draw the culture supernatant into the test tube, centrifuge at 4500 for 1 min at 4°C, discard the supernatant, quickly resuspend the cells with pre-cooled PBS and transfer to a 1.5mL centrifuge tube for centrifugation, and absorb the supernatant PBS...

Embodiment 2

[0025] Example 2 Cell Viability Experiment

[0026] Take lung cancer cells A549, H1299, and H1650 logarithmic growth phase cells, and prepare each cell line to 1×10 with RPMI1640-5% FBS culture medium 4 cells / mL single cell suspension, seeded in 96-well plate, 200uL per well, and the cell suspension without sample was set as negative control.

[0027] The total glucosides of paeony and gefitinib were prepared to the required concentration with the culture solution, the original culture solution was sucked away with a vacuum pump, and the culture solution containing different concentrations of the total glucosides of paeony was added to the wells, and each concentration was set at three times. 2 parallel wells, 200uL per well; add RPMI1640-5% FCS culture solution to the control group, and culture for 72h.

[0028] After 72 hours, add 2mg / mL Resazurin solution 20uL / well, mix well and store at 37°C, 5% CO2 and incubated for 16 h under saturated humidity conditions. After the in...

Embodiment 3

[0030] Example 3 Cell Morphology Observation

[0031] Take lung cancer cells A549, H1299, and H1650 logarithmic growth phase cells, and prepare 9×10 cells with RPMI1640-5% FBS medium 4 cells / mL single cell suspension, inoculated in 10cm culture dish, 10mL per dish, and set the cell suspension without sample as negative control.

[0032] Prepare the total glucosides of paeony with the culture solution to the required concentration, absorb the original culture solution with a vacuum pump, add the culture solution containing different concentrations of drugs into the culture dish, 10mL per dish; add RPMI1640-5%FCS culture to the control group solution, cultivated for 72h.

[0033] Take different groups of cell culture dishes and place them under a microscope for observation, adjust the microscope to a 10x eyepiece and a 10x objective lens, and use camera software to take pictures of the cell morphology in the field of view. see results Figure 4 .

[0034] Figure 4 It showe...

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PUM

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Abstract

The invention belongs to the field of medicines and relates to a new application of total glucosides of paeony as an EGFR (epidermal growth factor receptor) tyrosine kinase inhibitor. The content of paeoniflorin (C23H28O11) in the total glucosides of paeony is not less than 34.6%. Compared with the traditional EGFR tyrosine kinase inhibitor gefitinib, the total glucosides of paeony have the advantages that the total glucosides of paeony have high safety, can obviously reduce the expression quantity and activation quantity of EGFR tyrosine kinase, are low in price and have abundant resources, thereby providing a new choice for medicine development.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the new use of total glycosides of paeony as an EGFR tyrosine kinase inhibitor. Background technique [0002] Total Glucosides of Paeony (Total Glucosides of Paeony) is the total glycosides extracted from the traditional Chinese herbal medicine Paeoniae Alba. It is a mixture of a series of glycoside compounds such as paeoniflorin, hydroxy-paeoniflorin, paeonin, albiflorin and benzoylpaeoniflorin. Total glucosides of paeony have a variety of biological functions and pharmacological values. They have the effects of calming the liver and relieving pain, nourishing blood and regulating menstruation, astringing yin and antiperspirant, etc. Its resources are very rich in China. As a traditional Chinese medicine, it has been used in a variety of Chinese medicine compounds More than 1500 years. Total glucosides of paeony was approved by the State Food and Drug Administration (SFDA) in 1998 as a cl...

Claims

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Application Information

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IPC IPC(8): A61K36/71A61P35/00
Inventor 张丽娟唐洋崔怡迪邱培菊兰莹
Owner OCEAN UNIV OF CHINA
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