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New use of rutin

A new use and disease technology, applied in the field of medicine, can solve the problems of unsatisfactory clinical MDR reversal effect, failure to effectively overcome tumor MDR, and inability of anti-tumor drugs to play a synergistic effect.

Inactive Publication Date: 2019-01-18
SICHUAN UNIV
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  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its clinical MDR reversal effect is still unsatisfactory
It may be because these inhibitors all directly act on the P-gp protein, and their action time is short, and they cannot play a good synergistic effect with anti-tumor drugs in vivo
[0008] Summarize the lessons of the failure of the development of four generations of P-gp inhibitors. Although tumor MDR is mainly caused by P-gp, directly acting on P-gp protein does not fundamentally inhibit the overexpression of P-gp, so it cannot effectively overcome the tumor. MDR

Method used

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  • New use of rutin
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Examples

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Embodiment 1

[0039] cell experiment

[0040] The inventors have proved that rutin is an inhibitor of PRMT1 at the cellular level. Taking human liver cancer cell line HepG2 cells as an example, this compound can reduce the mRNA levels of PRMT1 and P-gp in HepG2 cells. Immunoprecipitation (Co-IP: Co-Immunoprecipitation, co-immunoprecipitation technique) is a classic method for studying protein interactions based on the specific interaction between antibodies and antigens. A powerful method for determining the physiological interaction of two proteins in intact cells. Many protein-protein interactions present in intact cells are preserved when cells are lysed under non-denaturing conditions. When protein A is immunoprecipitated with an antibody to protein A pre-immobilized on magnetic beads, protein B that binds to protein A in vivo can also be precipitated together. Then through protein denaturation and separation, protein B was detected to prove the interaction between the two. The targe...

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Abstract

The present invention discloses a novel use of rutin as a PRMT1-PXR-P-gp pathway inhibitor for the preparation of a medicament or food for treating a disease associated with the regulation of the PRMT1-PXR-P-gp pathway. At the cellular level, rutin can significantly inhibit the expression of P-gp in human hepatoma cell line HepG2 by inhibiting the PRMT1-PXR-P-gp pathway, thereby reversing the increase in P-gp expression caused by long-term chemotherapy. The phenomenon of multidrug resistance of tumors increases the sensitivity of tumor cells to chemotherapeutic drugs and improves the therapeutic effect of oncology drugs.

Description

technical field [0001] The invention belongs to the field of medicine and relates to a new application of rutin, in particular to the application of rutin in the preparation of medicine or food for treating diseases related to the regulation of PRMT1-PXR-P-gp pathway. Background technique [0002] Tumor multidrug resistance (MDR) refers to the long-term exposure of tumor cells to a certain chemotherapeutic drug, which develops resistance to this chemotherapeutic drug and also to other anti-tumor drugs with completely different chemical structures, cellular targets and mechanisms of action. All showed resistance. Tumor MDR is the main cause of failure of chemotherapy for many common clinical malignant tumors such as breast cancer, ovarian cancer, lung cancer, liver cancer, gastric cancer, intestinal cancer, endometrial cancer, and various types of leukemia. [0003] The mechanism of MDR is diverse and complex, among which the overactivation of MDR-1 gene and the abnormally h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P35/00
CPCA61K31/7048A61P35/00
Inventor 王凌蒋学华余璐
Owner SICHUAN UNIV
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