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Application of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance

A technology of methyl dicarbonyl gibberellate and multidrug resistance is applied in the field of newly synthesized methyl gibberellate, which can solve the problems of no drug-resistant tumor anticancer drugs, inability to know the reversal of tumor drug resistance, etc. The effect of improving curative effect, few reaction steps and high product yield

Inactive Publication Date: 2011-01-05
KUNMING MEDICAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there are almost no anticancer drugs that are effective against drug-resistant tumors, let alone the mechanism of reversing tumor drug resistance [6]

Method used

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  • Application of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance
  • Application of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance
  • Application of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] The multidrug resistance characteristic and degree of embodiment one K562 / A02

[0103] 1. Drugs and preparation

[0104] The chemotherapeutic drugs ADM, EPI, and VP-16 were set at 5 test concentrations of 100, 50, 25, 12.5, and 6.25 μg / ml, which were set according to the results of the preliminary test. The specific preparation is as follows: Weigh a certain amount of medicine and add a certain amount of N.S to dissolve it, then add a certain amount of RPMI1640 complete culture medium to prepare a high-concentration solution, and the remaining concentrations are prepared by diluting in equal proportions.

[0105] 2. Experimental method

[0106] Referring to literature [13], the effect of each compound on cell proliferation was determined by the improved MTT method. Take the K562 and K562 / A02 cell lines in the logarithmic growth phase and adjust the cell suspension to a certain concentration and inoculate them in a 96-well culture plate, 90 μl / well. Immediately after s...

Embodiment 2 56

[0116] Example 2 Sensitivity of K562 / A02 cells to compound GA

[0117] 1. Drugs and preparation

[0118] ADM, VCR, VP-16, and GA are all set at 5 test concentrations of 100, 50, 25, 12.5, and 6.25 μg / ml (this concentration is set according to the results of the preliminary test), and the specific preparation method is the same as before.

[0119] 2. Experimental method

[0120] The improved MTT method is the same as before.

[0121] Results: Compound GA showed higher drug sensitivity when acting on K562 / A02 cells, IC 50 The value is only 4.43 μg / ml (Table 2), but for the other three chemotherapeutic drugs with different structures and mechanisms of action, K562 / A02 cells are not sensitive to their drug effects. It suggested that while K562 / A02 cells were resistant to a variety of chemotherapeutic drugs, they still had high sensitivity to the compound GA, which provided a basis for subsequent experiments.

[0122] Table 2 K562 / A02 cell drug sensitivity to each test substanc...

Embodiment 3

[0129] Example 3 Compound GA reverses the effect and intensity of ADM drug resistance in K562 / A02 cells

[0130] 1. Drugs and preparation

[0131] (1) Compound G

[0132] Set 12.5, 6.25, 3.125 μg / ml 3 test concentrations (this concentration is set according to the results of the preliminary test). The specific preparation is as follows: Weigh a certain amount of GA, add a certain amount of DMSO and wait for it to dissolve, then add a certain amount of RPMI1640 complete culture medium to prepare a high-concentration solution, and each low-concentration solution is prepared by diluting in proportion;

[0133] (2) Positive control VER

[0134] VER is a liquid preparation for injection with an initial concentration of 2.5 mg / ml, adding a certain amount of RPMI1640 complete culture solution to dilute it to a working solution with a concentration of 10 μg / ml;

[0135] (3)ADM

[0136] The stock solution concentration is 1 mg / ml, and a certain amount of RPMI1640 complete culture s...

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Abstract

The invention relates to application of 3,15-dicarbonyl gibberellic acid methyl ester (GA) in reversing tumor multidrug resistance. A compound GA provided in the invention has favorable activity on the reversing tumor multidrug resistance (MDR), the GA acting on K562 / A02 has higher drug susceptibility and can obviously reverse the drug resistance of the K562 / A02 for ADM (Archer Daniels Midland); the effect mechanism of the GA for reversing the multidrug resistance of K562 / A02 cells is realized by increasing the contents of chemotherapeutic drugs in the drug-resistance cells to prevent the chemotherapeutic drugs from being discharged outwards and promote the apoptosis of the drug-resistance cells, and has no obvious relevance with the expression of down-regulated drug-resistance genes mdr-1, thereby prompting that the action mechanism of the GA is relevant to the outward discharging pump function of inhibiting the drug-resistance cells P-gp and inducing the apoptosis of the drug-resistance cells; and the compound GA has lower toxicity, and therefore the compound GA has favorable application prospect on clinical tumor chemotherapy and particularly on resisting clinical tumor drug resistance.

Description

technical field [0001] The present invention relates to the use of newly synthesized gibberellic acid methyl ester, specifically the use of 3,15-dicarbonyl gibberellic acid methyl ester in reversing tumor multidrug resistance. Background technique [0002] Malignant tumors seriously endanger human life and health, and have become one of the main causes of disease death today. With the deepening of the understanding of the nature of malignant tumors, the understanding that malignant tumors are systemic rather than local diseases has been generally recognized. Therefore, compared with surgery and radiotherapy, tumor drug therapy, namely chemotherapy, has a definite and irreplaceable role in treating tumors, prolonging survival time and improving the quality of life of patients. [1] . However, the multi-drug resistance (MDR) produced during tumor chemotherapy is one of the main reasons for the failure of tumor chemotherapy. [9] . [0003] MDR refers to the cross-resistance ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P35/00A61P35/02
Inventor 卿晨仇笳熙张洪彬陈亚娟陈静波张雁丽
Owner KUNMING MEDICAL UNIVERSITY
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