Screen method of sensitization tumour cell pharmaceutical product and use thereof

Abstract

The invention discloses an enhancement tumor cell medicament screening method and its application mainly for effectively overcoming the multidrug resistance to improve the anti-cancer drug treatment effect in a tumor chemotherapy process. The invention screens an inhibitor which can effectively inhibiting the induction action through luciferase activity detection by using an Nrf2 as a cell drug screen platform of a molecular target and a tBHQ as an Nrf2 inducer, and the inhibitor is a medicament of the enhancement tumor cell. The medicament obtained by the screen is a small molecular compound ZDAK02 (coralyne sulfoacetate coralyne thioacetate). The combined use of the medicament of the invention with the anti-cancer drug Chlorambucil or anti-cancer drug oxaliplatin can enhance the toxicity of the anti-cancer drug to the cancer cells and be helpful for easing even reversing the multidrug resistance to the anti-cancer drugs.

Description

technical field [0001] The invention relates to a drug capable of alleviating or even reversing the resistance of tumors to anti-tumor drugs and its screening technology. Background technique [0002] At present, the most clinically used anticancer drugs are alkylating agents and oxidation-reduction cyclers, and these two types of drugs include cyclophosphamide (CTX), ifosfamide, mephalan, cephine, and thiotepa , Maryland, nitrosourea drugs, cisplatin and more than ten kinds of anticancer drugs. Alkylating agent anti-tumor drugs have high chemical activity, can directly act on key parts of proteins, enzymes, and nucleic acids that are important for tumor cell growth, and form alkyl groups with amino groups, sulfhydryl groups, carboxyl groups, and phosphate groups in these tissues. The chemical reaction can denature the protein, enzyme and nucleic acid of the cell, and change the structure or physiological function, thereby preventing the proliferation of tumor cells and cau...

AI Technical Summary

Problems solved by technology

But the most important and common one is P-gp, also known as typical MDR, which is a protein widely present on the cell membrane of various tumor cells, and is responsible for pumping intracellular drugs out of the cell, thereby causing tumor cell death. Multidrug resistance reduces efficacy of cancer chemotherapy

On the other hand, it may be due to the increase in the expression or activity of some drug-resistant proteins, which leads to the enhancement of the viability of the cells themselves, so that the tumor cells develop drug resistance.

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