Application of Swertia Swertia Extract in the Preparation of Drugs Inhibiting Glutathione S-Transferase Activity

A technology of glutathione and extract, applied in the directions of drug combination, organic active ingredients, biochemical equipment and methods, etc., can solve the problems of complex preparation process and high cost, and achieve simple extraction process, high safety, and enhanced synergy. effect of effect

Active Publication Date: 2022-04-08
HUNAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In recent years, there have been more and more studies on GSTs inhibitors. The GSTs inhibitors currently reported mainly include ethacrynic acid and its analogs, TLK199 and its analogs, flavonoids, and bifunctional compounds. However, these GSTs inhibitors Most of them need to be obtained by artificial synthesis, and there are disadvantages such as complicated preparation process and high cost.

Method used

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  • Application of Swertia Swertia Extract in the Preparation of Drugs Inhibiting Glutathione S-Transferase Activity
  • Application of Swertia Swertia Extract in the Preparation of Drugs Inhibiting Glutathione S-Transferase Activity
  • Application of Swertia Swertia Extract in the Preparation of Drugs Inhibiting Glutathione S-Transferase Activity

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preparation example Construction

[0052] According to the present invention, the preparation method of the probe includes the following steps: under oxygen-free conditions, after mixing II with the fluorescent agent and triethylamine in the organic solvent II, and then mixing III with the quencher; wherein, the The fluorescent agent is resorufin, and the quencher is 2,4-dinitrobenzenesulfonyl chloride. Wherein, the oxygen-free condition can be realized by feeding nitrogen or argon. The inventors found that in this preferred embodiment, it is beneficial to increase the yield of probes.

[0053] In the present invention, the organic solvent used in the preparation of the probe is not particularly limited, as long as it can be used in the synthesis reaction of fluorescent agent, triethylamine and quencher. Preferably, the organic solvent II is at least one selected from tetrahydrofuran, N,N-dimethylformamide, N,N-dimethylacetamide and dimethyl sulfoxide.

[0054] The present invention does not specifically limi...

Embodiment

[0066] The preparation process of probe RP:

[0067] (1-1) in access to N 2 Under the condition of 0.28mmol of 2,4-dinitrobenzenesulfonyl chloride was dissolved in 10mL of tetrahydrofuran to obtain a quencher solution;

[0068] (1-2) in access to N 2 Under certain conditions, add 0.28mmol triethylamine into 5mL tetrahydrofuran and mix II with 0.28mmol resorufin powder, stir at 20°C for 30min, then mix III with the quencher solution obtained in step (1-1), After stirring at 20° C. for 12 h, a mixed solution was obtained;

[0069] (1-3) After evaporating the mixed solution obtained in step (1-2) to remove tetrahydrofuran, use petroleum ether-ethyl acetate mixed solution (the volume ratio of petroleum ether and ethyl acetate is 2:1) as the eluent to carry out silica gel Purification by chromatography afforded probe RP (yellow solid, 8.3 mg, yield 27.7%).

[0070] The preparation process of the extract of Swertia japonica to be screened:

[0071] (2-1) Reflux extraction with ...

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Abstract

The invention relates to the fields of biochemical analysis and drug screening, and discloses the application of an extract of Swertia japonica in the preparation of a drug for inhibiting the activity of glutathione S-transferase. The extract of Swertia japonica is selected from at least one of: and . The present invention also provides a pharmaceutical composition containing the above-mentioned extract of Swertia japonica. The extract of Swertia japonica provided by the present invention has a strong inhibitory effect on intracellular glutathione S-transferase activity, and the use of combined anti-tumor drugs can enhance the synergistic effect and significantly improve the killing efficiency of tumor cells.

Description

technical field [0001] The present invention relates to the fields of biochemical analysis and drug screening, in particular to the application of a swertia extract in the preparation of drugs for inhibiting the activity of glutathione S-transferase. Background technique [0002] Glutathione S-transferase (glutathione S-transferase, GSTs) is the key enzyme of glutathione conjugation reaction, which catalyzes the initial step of glutathione conjugation reaction. GSTs can catalyze the combination of harmful polar compounds and glutathione in the body, and can also excrete various potential carcinogens and lipophilic compounds from the body in a non-enzymatic way to achieve the purpose of detoxification. Studies have shown that the enzyme activity levels of GSTs are closely related to the drug resistance of tumors, and may be potential drug targets for the treatment of drug-resistant tumors. [0003] Previous studies have found that overexpressed GSTs can be observed in some d...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61K31/352A61K36/51A61K45/06A61P35/00C07D311/86C07J9/00C12Q1/48
CPCA61K36/51A61K31/575A61K31/352A61K45/06C12Q1/48C07J9/00C07D311/86A61P35/00G01N2333/91177A61K2236/333A61K2236/39A61K2236/53A61K2236/51A61K2236/55
Inventor 覃艳王炜彭彩云刘斌杨维易攀范家龙
Owner HUNAN UNIV OF CHINESE MEDICINE
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