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Anti-tumor MDR (multiple drug resistance) interfering drug and preparation method

A multi-drug resistance, anti-tumor technology, applied in the field of anti-tumor drugs, can solve the problems of high cost and difficult synthesis of reversal agents

Inactive Publication Date: 2018-03-23
XIHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The invention provides an anti-tumor multi-drug resistance interfering drug and a preparation method, which solves the technical problems of difficulty in synthesis of reversal agents used in the prior art and high cost

Method used

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  • Anti-tumor MDR (multiple drug resistance) interfering drug and preparation method
  • Anti-tumor MDR (multiple drug resistance) interfering drug and preparation method
  • Anti-tumor MDR (multiple drug resistance) interfering drug and preparation method

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Embodiment Construction

[0018] In order to make the above objects, features and advantages of the present invention more comprehensible, the present invention will be further described in detail below in conjunction with the accompanying drawings and specific embodiments.

[0019] An embodiment of the present invention provides an anti-tumor multi-drug resistance interfering drug, comprising: 1-3 parts of echinocytic acid or its derivatives, and 1-2 parts of oleanolic acid.

[0020] Wherein, the structural characteristics of echinocytic acid or its derivatives are:

[0021]

[0022] Among them, the compound and the number are specifically: echinocytic acid, R1 is -OH, R2 is -COOH; compound 2 (TRSZ-2), R1 is =O, R2 is -COOH; compound 3 (TRSZ-3), R1 is =NOH, R2 is -COOH; Compound 4 (TRSZ-4), R1 is -OH, R2 is -COOCH3; Compound 5 (TRSZ-5), R1 is =O, R2 is -COOCH3; Compound 6 (TRSZ-6 ), R1 is =NOH, R2 is-COOCH3.

[0023] A preferred embodiment of the present invention is anti-tumor multi-drug resista...

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Abstract

The invention relates to the field of anti-tumor drugs and discloses an anti-tumor MDR (multiple drug resistance) interfering drug and a preparation method. The interfering drug is prepared from 1-3 parts of echinocystic acid or echinocystic acid derivatives and 1-2 parts of oleanolic acid. Echinocystic acid and the echinocystic acid derivatives are effectively utilized to inhibit P-gp (P-glycoprotein) activity of a drug-resistant strain, so that chemotherapeutic drugs pumped out of cells are reduced, effects of the chemotherapeutic drugs are enhanced, and the sensitization effect is realized.Besides, by the aid of oleanolic acid, hepatotoxicity is remarkably reduced, and therefore, the interfering drug is safer and more effective in chemotherapy.

Description

technical field [0001] The invention relates to the field of anti-tumor drugs, in particular to an anti-tumor multi-drug resistance interfering drug and a preparation method. Background technique [0002] At present, chemotherapy is still one of the main clinical treatments for malignant tumors, and the multidrug resistance (MDR) of tumor cells is an important reason for the failure of chemotherapy. MDR refers to the cross-resistance of tumor cells to other anti-tumor drugs with different structures and mechanisms of action while developing resistance to one anti-tumor drug. The main cause of MDR is the efflux of antitumor drugs by P-glycoprotein (P-gp), and other reasons include multidrug resistance-related protein (MRP), lung resistance protein (LRP), Glutathione and glutathione-S-transferase, PKC and TopoII, etc. [0003] P-gp is the expression product of MDR1 gene, which is a member of ABC (ATP-bindingcassette) family and contains two transmembrane domains and two ATP-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P35/00
CPCA61K31/56A61K2300/00
Inventor 赖朋曹旭
Owner XIHUA UNIV
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