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Application of Schizandrin A on curing drug resistance for multiple drugs of treating tumors

A schisandrin A, multi-drug resistance technology, applied in the direction of antitumor drugs, drug combinations, ether/aldol active ingredients, etc., can solve the toxic and side effects, cardiovascular toxicity, and unsatisfactory effect of solid tumor resistance reversal and other problems, to achieve a significant dose-dependent, strong reversal effect

Inactive Publication Date: 2009-01-07
CHANGCHUN JILIN UNIV HI TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, many compounds have been found to have strong tumor multidrug resistance reversal effects in vitro and in vivo animal experiments, such as calcium channel blockers including verapamil, calmodulin antagonists, cyclosporins, Quinolines and anti-estrogens, however, when used clinically, in addition to the relatively certain reversal effect on some blood system tumor drug resistance, the reversal effect on solid tumor drug resistance is not ideal
It is generally believed that these compounds cannot achieve an effective reversal concentration in the body at a dose that can be tolerated by the human body, and once the dose is increased to make the blood drug concentration reach the concentration with reversal activity in the in vitro test, serious toxic and side effects will occur. Or when reversal agents are used in combination with antineoplastic drugs, the pharmacokinetic parameters of antineoplastic drugs will be changed, resulting in unforeseen toxic and side effects
For example, verapamil as a positive control in the present invention has strong tumor resistance reversing activity in vitro, but it is found that cardiovascular toxicity is produced when it does not reach the concentration of reversing drug resistance when applied to the body, thus limiting its clinical use

Method used

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  • Application of Schizandrin A on curing drug resistance for multiple drugs of treating tumors
  • Application of Schizandrin A on curing drug resistance for multiple drugs of treating tumors
  • Application of Schizandrin A on curing drug resistance for multiple drugs of treating tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Take KB, KBv200, MCF-7, MCF-7 / Adr, Bel in the logarithmic growth phase 7402 The cells were seeded in a 96-well culture plate (Coster), and after 24 hours of culture, gradient concentrations of anticancer drugs, reversal agents and control solvents were added. Continue to cultivate for 72 hours, then discard the culture medium, add 0.5 mg / ml thiazolium (MTT) 100 μl (diluted with RPMI 1640 culture medium without serum) to each well, continue to cultivate for 4 hours, discard the thiazolium, add to each well 150 μl of dimethyl sulfoxide was shaken slightly to dissolve the precipitate, and the absorbance was measured at 570 nm in a microplate reader (Bio-Rad 450 type). Set up three to four replicate wells in each group and take the average value to calculate the IC 50 . 10 μmol / L verapamil was used as a positive control. See Table 1-10 for specific results.

[0043] Table 1. Effect of Schisandrin A on the sensitivity of KBv200 cells to vincristine

[0044]

[0045] ...

Embodiment 2

[0066] Take the logarithmic growth period Bel 7402 Cells, when the cells cover 70-80% of the bottom of the bottle, replace the RPMI 1640 culture medium containing 10 μmol / L doxorubicin, and add schisandrin at the final concentrations of 50 and 25 μmol / L respectively, and add 10 μmol / L vera Pamir was used as a positive control, and three parallel samples were set up for each group, at 37°C, 5% CO 2 Continue to incubate for 3 hours, collect the cells after washing three times with ice-cold PBS (pH 7.4), take a certain number of cells, suspend the cells with 1.2ml hydrochloric acid (0.3N)-ethanol (50%), and break the cells on a sonicator Afterwards, centrifuge at 10,000rpm for 15 minutes, take 1.0ml of the supernatant and add 2.0ml of the above-mentioned hydrochloric acid-ethanol solution, measure the fluorescence value of adriamycin with a fluorescence spectrophotometer, the excitation wavelength is 470nm, and the emission wavelength is 580nm. Content-fluorescence standard curv...

Embodiment 3

[0068] Inoculate KB, KBv200 and Bel 7402 The cells were placed on a petri dish with a diameter of 3.5 cm. After culturing for 24 hours, the unattached cells were washed away, and rhodamine 123 (final concentration: 250 ng / ml) and / or different concentrations of Schizandrin were added respectively. In the control group, only schisandrin was added. After incubating at room temperature for 30 minutes, the cells were washed twice with 0.1 M phosphate buffer, and the accumulation of rhodamine 123 in the cells was observed by laser scanning confocal microscopy. Five fields of view were randomly selected for each petri dish to observe, and the average fluorescence intensity was analyzed by computer software. At least 50 cells were analyzed per sample. The main parameters of each Petri dish are the same during image processing. see results figure 2 , 3 .

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Abstract

An application of schisandrin A in treating the drug-resistant tumor is disclosed. It can be used in conjunction with antineoplastic for increasing the sensitivity of tumor to antineoplastic.

Description

technical field [0001] The present invention relates to the new use of Schizandrin A as a multidrug resistance reversal agent, especially the combined use with antineoplastic drugs to treat multidrug resistant tumors and improve the sensitivity of tumor cells to anticancer drugs. New uses for tumors. Background technique [0002] The acquired drug resistance of tumor cells after chemotherapy and the inherent drug resistance of some tumor cells are still one of the important reasons for the failure of tumor chemotherapy. The mechanism of multidrug resistance is very complicated. The main mechanism is the overexpression of multidrug resistance glycoprotein (P-gp) on the tumor cell membrane. Many chemotherapy drugs are substrates of P-gp, such as vinblastine , anthracyclines, epipodophyllotoxins, taxanes, etc. Reversing the multidrug resistance of tumor cells so as to restore the sensitivity of tumor cells to chemotherapeutic agents has very important clinical application val...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/09A61P35/00
Inventor 刘耕陶黄敏金晶魏怀玲孙华
Owner CHANGCHUN JILIN UNIV HI TECH
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