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Application of jervine to preparation of multidrug resistance reversal agent for tumor

A technology of multi-drug resistance and euphenamine, which is applied in the field of natural medicinal chemistry, can solve the problem of weak direct anti-tumor effect of euphenamine, and achieve the effect of abundant drug sources, easy access and low price

Inactive Publication Date: 2017-12-22
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At present, the most researched is the study of euphenamine and its analog cyclopamine (cyclopamine) as a specific inhibitor of the Hh signaling pathway, among which cyclopamine has a good inhibitory effect on pancreatic cancer, small cell lung cancer and other tumors, but The direct anti-tumor effect of euphenamine is relatively weak, and the application of euphenamine in the reversal of tumor multidrug resistance has not been involved

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  • Application of jervine to preparation of multidrug resistance reversal agent for tumor
  • Application of jervine to preparation of multidrug resistance reversal agent for tumor
  • Application of jervine to preparation of multidrug resistance reversal agent for tumor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: The effect of musterphenamine alone on the proliferation of different cells

[0026] Experimental method: MTT method was used to detect the effect of different concentrations of mustardine on the proliferation activity of drug-resistant cell lines (MCF-7 / ADR) and corresponding maternal cell lines (MCF-7), as well as other tumor cells (K562, HL) -60, A549, HCT116, HeLa) and normal tissue cells (HUVEC). The experimental procedure is as follows: Take the logarithmic growth phase cell line, use 10% FBS 1640 medium to make a cell suspension, adjust the cell number to 4.0×10 4 Pieces / mL, 100 μL / well were inoculated in 96-well plates, incubated in an incubator at 37°C and 5% CO2 saturated temperature for 24 hours, and then treated with drugs. After 72 hours of drug action, MTT solution was added, and the supernatant medium was removed after 4 hours of incubation. 150 μL / well of dimethyl sulfoxide (DMSO) was added, the optical density value OD was measured, and the inhi...

Embodiment 2

[0030] Example 2: The effect of mustardine combined with ADR on the proliferation of MCF-7 / MDR cells

[0031] Experimental method: The MTT method was used to detect the effect of different concentrations of mustardine combined with ADR on the proliferation activity of drug-resistant cell lines (MCF-7 / ADR). The experimental procedure is as follows: Take the logarithmic growth phase cell line, use the medium containing 10% FBS 1640 to make a cell suspension, and adjust the cell number to 4.0×10 4 Pcs / mL, inoculate 100 μL / well in 96-well plate, at 37℃, 5% CO 2 After 24 hours of incubation in a saturated temperature incubator, dosing is carried out. The combined action of mustardamine and ADR for 72 hours, then add MTT solution, continue to incubate for 4 hours, remove the supernatant medium, add 150 μL / well dimethyl sulfoxide (DMSO), detect the optical density value OD, calculate the inhibition rate and IC50 And reversal multiple (Reversal Fold, RF).

[0032] Experimental results: fi...

Embodiment 3

[0033] Example 3: Effect of mustardine combined with ADR on apoptosis of drug-resistant cell lines

[0034] Experimental method: Take the drug-resistant tumor cell line MCF-7 / ADR in the logarithmic growth phase, culture it overnight for 24 hours and then add drugs to the cells. After 24 hours of incubation in the incubator, the cells were lysed to obtain total protein. Western blotting was used to detect the changes of cell-related proteins to reflect the apoptosis.

[0035] Experimental results: In order to explore whether mustardine can enhance the anti-tumor effect of these drugs, this experiment uses western bloting to detect the changes of apoptosis-related molecules in drug-resistant cells after treatment with mustardine combined with ADR. Experimental results ( figure 2 ) Showed that single use of 12.5 μM ADR and mustardine (12.5 μM and 25 μM) did not significantly induce apoptosis of drug-resistant tumor cells, and when 12.5 μM or 25 μM doses of mustardine were used in com...

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Abstract

The invention provides an application of jervine to preparation of a multidrug resistance reversal agent for a tumor. When jervine is jointly used with other tumor chemotherapeutic drugs, the killing effect of the chemotherapeutic drugs on drug-resistant tumor cells can be improved obviously, dosage of the tumor chemotherapeutic drugs can be reduced, and the toxic effect of the chemotherapeutic drugs is reduced. The unique action mechanism of jervine is as follows: jervine can inhibit transport of ABCs (ATP-bindingcassette transporters) such as P-gp, ABCG2 and the like, reduce efflux of the chemotherapeutic drugs by the tumor cells, increase concentration of the chemotherapeutic drugs in the cells and induce apoptosis of the drug-resistant tumor cells, so that the multidrug resistance of the tumor cells is overcome. Jervine can be combined with other chemotherapeutic drugs for preparation of a compound drug for overcoming multidrug resistance of the tumor and has broad application prospect.

Description

Technical field [0001] The invention belongs to the field of natural medicinal chemistry, and specifically relates to the application of mustardine in the preparation of a tumor multidrug resistance reversal agent. Background technique [0002] Tumor multi-drug resistance refers to the phenomenon of cross-resistance to many other anti-tumor drugs with different structures and different mechanisms of action while being resistant to one anti-tumor drug. The mechanism of action of tumor multidrug resistance is very complicated, mainly including the following aspects: (1) Decreasing the intracellular drug concentration by reducing drug intake and increasing drug outflow. (2) Activate or inactivate drugs through intracellular drug metabolism. (3) By changing the level of the drug-resistant target enzyme in the cell or the affinity between the enzyme and the drug in the cell, the drug becomes invalid. (4) Strengthen DNA damage repair function. (5) Enhance the ability of cell anti-ap...

Claims

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Application Information

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IPC IPC(8): A61K31/58A61K31/165A61K31/513A61K45/06A61P35/00
CPCA61K31/165A61K31/513A61K31/58A61K45/06A61K2300/00
Inventor 刘明林秀坤赵兴增李静戚欣
Owner OCEAN UNIV OF CHINA
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