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Application of polyphyllin VII in preparation of MSN protein inhibitor

A technology of protein inhibitors and papaya saponins, which is applied in the field of medicine, can solve the problems such as the unclear function of the target protein

Active Publication Date: 2021-02-26
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In summary, PP7 is a broad-spectrum antitumor drug with important potential for clinical development, but the role of PP7 in multiple myeloma and cancer stem cells and the role of target proteins are still unclear

Method used

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  • Application of polyphyllin VII in preparation of MSN protein inhibitor
  • Application of polyphyllin VII in preparation of MSN protein inhibitor
  • Application of polyphyllin VII in preparation of MSN protein inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023]Example 1: Fructus saponins VII was identified as an ideal natural compound monomer for the treatment of multiple myeloma

[0024]The saponins of the saponins series of saponins of saponins saponins VII (PP7), saponins Ⅵ (PP6) and saponins Ⅰ (PP1) (all purchased from Selleck Biotechnology Co., Ltd.) have anti-tumor activity. We first treated MM cells MM.1S (from ATCC), ARP1, ANBL6 and ANBL6-BR cells (all from Professor Zhou Wen from the Tumor Research Institute of Central South University) at a concentration of 2 μM with these three monomers. Natural product monomer with the best anti-tumor activity. After it was proved that the anti-tumor effect of C. saponins Ⅶ was the most significant, CCK-8 method was used to detect the effects of C. saponins VII on immortalized B lymphocytes (from the Genetics Laboratory of the School of Life Sciences, Central South University), MM cell lines, and normal human PBMC cells ( From Xiangya Hospital of Central South University) and original CD138...

Embodiment 2

[0051]Example 2: Fructus saponins VII inhibits multiple myeloma stem cell-like cells and targets side population cells.

[0052]Flow cytometry was used to detect the effect of saponins Ⅶ on the side population ratio of ARP1 and RPMI-8226 cells, and qPCR was used to detect the effect of saponins Ⅶ on the stemness genes Oct4, Nanog, Sox2, Lin28 and Klf4 of ARP11 and RPMI-8226 cells. After flow cytometric separation of the side population and main population of ARP1 cells, CCK-8 was used to detect the effect of saponins Ⅶ on the survival rate of side population cells and main population cells, and the soft agar clone formation experiment was used to detect the saponins Ⅶ contralateral side population cells. And the clonogenic ability of main population cells. And through the flow cytometric detection of saponins Ⅶ, the primary CD138 of MM+The effect of cell side population cell ratio.

[0053]The experimental steps are as follows:

[0054]1. Flow cytometric detection of the effect of saponins Ⅶ...

Embodiment 3

[0095]Example 3: Saponins saponins of Rhizoma Polygoni VII inhibits MSN protein

[0096]DARTS (Drug Affinity Reaction Target Stability Method) was used to find the target protein of Saponins VII. After processing the samples with the DARTS method and CETSA (Cell Thermal Transition Analysis) method, WB verifies whether the MSN protein is the target protein of Saponins VII, and then WB detects the difference in the expression of MSN in normal human immortalized B lymphocytes and MM cell lines. WB directly detects the changes of MSN protein after ARP1 and MM.1S cells are treated with Saponins Ⅶ. Studies have found that the combination of small molecule drugs and proteins will stabilize the protein conformation and make it resistant to protease hydrolysis. The DARTS method was invented based on this principle. The drug ligand also induces the thermal stability of the target protein. The CETSA method was invented based on this principle.

[0097]1. DARTS method to find the target protein of sa...

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Abstract

The invention discloses application of polyphyllin VII in preparation of an MSN protein inhibitor. A series of experiments prove that the polyphyllin VII has the activity of resisting multiple myeloma; and furthermore, the polyphyllin VII exerts the activity of resisting multiple myeloma by directly inhibiting the MSN protein level to target multiple myeloma stem cell-like cell side population cells. The polyphyllin VII can be used as an inhibitor of MSN protein to treat diseases, such as multiple myeloma, caused by increase of expression of the MSN protein, and is expected to be developed into a novel anti-tumour drug.

Description

Technical field[0001]The present invention relates to a new use of saponins saponins saponins Ⅶ, and specifically relates to applications of saponins saponins Ⅶ in preparation of MSN protein inhibitor. It belongs to the field of medical technology.Background technique[0002]MSN (moesin) is a member of the ezrin-radixin-moesin (ERM) protein family, a protein that connects the actin cytoskeleton with transmembrane receptors. The physiological role of ERM protein is related to the structure of cell cortex and is involved in cell differentiation and morphogenesis. MSN is up-regulated in a variety of human cancers, including breast cancer, prostate cancer, pancreatic cancer, lung and melanoma, etc. MSN is the dominant ERM protein in lymphocytes and is related to the outflow of T and B cells from secondary lymphoid organs. CD44 can provide a connection between the plasma membrane and the actin cytoskeleton by binding to ERM proteins (Ezrin, radixin, moesin). The MSN-CD44 interaction is a p...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P19/08A61P35/00
CPCA61K31/7048A61P19/08A61P35/00
Inventor 刘静王海勤萧小鹃朱林李珍珍易慧
Owner CENT SOUTH UNIV
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