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Application of quinoid chalcone compound in preparation of antitumor drugs

An anti-tumor drug, chalcone technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations, etc., can solve the problems of clinical patients with tumor recurrence or metastasis, inability to completely remove B16-OVA cells, and death.

Active Publication Date: 2019-07-05
稷冲(北京)医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Killing T cells are used in vitro to kill cancer cells. Theoretically speaking, the larger the number of T cells, the more significant the killing effect. However, the inventors of this case found in the study of melanoma B16-OVA cells that the killing T cells The killing effect of cells on cancer cells increases with the increase of concentration, however, even if the number of T cells is increased after reaching a certain ratio, B16-OVA cells cannot be completely eliminated
This phenomenon suggests that there are a group of dormant cells in cancer cells that cannot be killed by specific T cells during clinical treatment, and these dormant cancer cells have buried hidden dangers in tumor patients. Dormant cancer cells, so that clinical patients have the risk of tumor recurrence or metastasis leading to death

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  • Application of quinoid chalcone compound in preparation of antitumor drugs
  • Application of quinoid chalcone compound in preparation of antitumor drugs
  • Application of quinoid chalcone compound in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] Example 1: Single use of the quinoidal chalcone compound of the present invention can effectively induce apoptosis of solid tumor and leukemia cells under 3D culture conditions.

[0068] 1. Experimental steps

[0069] Use 3D glue technology to culture A375, A549, HepG2, MCF-7, PANC-1 and HL-60 cells, the number of cells is about 10,000 per well, observe the state of the cells after 2 days, under good conditions, each cultured cells are separated according to The following groups were dosed:

[0070] Control group (control): common medium (such as RPMI-1640 medium) supplemented with glutamine;

[0071] Experimental group: 10 μmol / ml HB-2, HB-3, HB-7, HB-19, HB-25, HB-31, HB- 33. HB-46, DMF was used as positive control.

[0072]When adding the drug, the drug and the medium were evenly mixed and then added to each group of experimental cells. The start of adding the drug was recorded as day 0, and the cells in the 3D glue were detected for apoptosis at 96 hours (day 4)....

Embodiment 2

[0075] Example 2: Inhibitory growth of solid tumors and leukemias in vivo by small molecule inhibitor HB-2 and its structural analogues.

[0076] 1. Experimental steps

[0077] (1) Construction of A375 tumor-bearing mice: NON-SCID mice were subcutaneously inoculated with 1×10 5 A375 cells, when the tumor grows to 5mm x 5mm, the tumor-bearing mice were randomly divided into 10 groups, with 7 mice in each group, and the tumor-bearing mice were given the following different treatments:

[0078] Control group (control): intragastric administration of PBS;

[0079] Positive control group: intragastric administration of DMF (10 mg / kg), once every two days.

[0080] Experimental group (8 groups): Each group was given HB-2, HB-3, HB-7, HB-19, HB-25, HB-31, HB-33, HB-46 by intragastric administration, 10mg / kg body weight, Administer once every two days;

[0081] After the mice were sacrificed on the 21st day, the subcutaneous tumors were peeled off, and the tumor weights of each gr...

Embodiment 3

[0112] Example 3: The combination of IFN-β and HB-2 significantly induces the apoptosis of solid tumor cells and leukemia cells under 3D culture conditions.

[0113] 1. Experimental steps

[0114] Solid tumor cells A375, A549, HepG2, MCF-7, PANC-1, and leukemia cells HL-60 were cultured in 3D gel (24-well plate, cell density: 8000 / well), and the cell status and cell survival were observed the next day. In good condition, dosing treatment according to the following groups:

[0115] Control group 1 (control): common medium and drug solvent;

[0116] Control group 2 (IFNβ): add 6 ng / ml mouse or 10 ng / ml human IFNβ to normal culture medium;

[0117] Experimental group 3 (HB-2): adding 10 μmol / ml of HB-2 to normal culture medium;

[0118] Experimental group 4 (IFNβ+DMF): add 6ng / ml mouse or 10ng / ml human IFNβ and 20μmol / mlμM DMF to normal medium;

[0119] Experimental group 5 (IFNβ+HB-2): add 6 ng / ml mouse or 10 ng / ml human IFNβ and 10 μmol / ml HB-2 to normal medium;

[0120] W...

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Abstract

The present invention provides an application of a quinoid chalcone compound in preparation of antitumor drugs. The quinoid chalcone is the quinoid chalcone compound with an A ring having an isopentenyl group. The present invention also provides an application of the compound in treatment of tumor diseases as a single drug or a combination drug. The quinoid chalcone itself has relatively strong anti-tumor ability, can kill differentiated tumor cells and also kill dormant tumor stem cells when combined with anti-tumor drugs of interferon, etc., and has an effect of completely removing the tumorcells.

Description

technical field [0001] The present invention relates to the application of a quinone chalcone compound in the preparation of antitumor drugs, and also relates to the application of this type of compound as a combined drug in the treatment of tumor diseases, and a combination of antitumor drug preparations. Background technique [0002] Malignant tumor is a disease caused by abnormal proliferation of cells. Cancer stem cells play an important role in the survival, proliferation, metastasis and recurrence of tumors. Essentially, cancer stem cells maintain the vitality of tumor cell populations through self-renewal and unlimited proliferation, and their ability to move and migrate endows tumor cells with the ability to invade and metastasize distantly. Research reports in recent years have shown that during clinical treatment, tumor stem cells can remain in a dormant state for a long time and up-regulate the expression of multiple drug-resistant molecules, but are insensitive t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K38/21A61P35/00A61P37/02A61P35/02
CPCA61K31/122A61K38/215A61K38/217A61K2300/00
Inventor 黄波
Owner 稷冲(北京)医药有限公司
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