Application of sanguinarine in preparation of RIPK3 activator

A sanguinarine, active technology, applied in the field of medicine, to achieve the effect of inhibiting activity, increasing the level of reactive oxygen species, and good effect

Pending Publication Date: 2022-05-27
GUANGDONG MEDICAL UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are no literature reports on the application of sanguinarine in the preparation of RIPK3 activators

Method used

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  • Application of sanguinarine in preparation of RIPK3 activator
  • Application of sanguinarine in preparation of RIPK3 activator
  • Application of sanguinarine in preparation of RIPK3 activator

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0083] Example 1 Molecular docking

[0084] The RIPK3 protein crystal structure (PDB id: 7MX3) was obtained from the PDB database (https: / / www1.rcsb.org / ), and its structure was trimmed and hydrotreated by the "Prepare Protein" module of the Discovery Studio 4.5 platform, and removed at the same time. Water of crystallization, and the docking site is automatically identified based on the position of the original ligand in the PDB co-crystal structure. The "Prepare Ligand" module of the DiscoveryStudio platform was used to minimize the energy of sanguinarine through the CHARMM force field, and the Libdock and CDOCKER methods were used to run the docking. To form a control, we re-docked the PDB pro-co-crystal ligand into the protein structure, and compared the docking scores of the two to determine whether sanguinarine has better protein binding effect. Finally, the spatial interaction of the complexes was observed with the help of the visualization software Pymol.

[0085] Th...

Embodiment 2

[0086] Example 2 The effect of sanguinarine on the activity of A549 cells

[0087] 1. Cell Culture

[0088] The well-grown A549 cells (cell line number: CCL-185) (all purchased from the American Culture Collection) were cultured, and the number of cells was 5 × 10 3 The density of cells / well was inoculated into a 96-well plate, and 100 μL of 1640 medium was added to each well, and placed in a constant temperature incubator (37°C, 5% CO). 2 ) for 24h. A549 cells were divided into control group (without any treatment, normal culture) and sanguinarine-treated group (final concentrations of sanguinarine were 0.5 μM, 1 μM, 2 μM, 4 μM, and 8 μM, respectively), and each treatment had 3 parallels, Continue to culture for 24h; use CCK-8 kit (Beyotime, catalog number: C0037) to detect the activity of A549 cells in 96-well plate, and use GraphPad prism software to calculate the IC of hemorrhizine acting on A549 cells 50 .

[0089] The result is as figure 2 As shown, the activity of...

Embodiment 3

[0090] Example 3 The effect of sanguinarine on the proliferation of A549 cells

[0091] In order to explore how sanguinarine causes the death of A549 cells, A549 cells were analyzed for death in this example.

[0092] A549 cells in good growth state were seeded in 12-well plates, 10 × 10 per well. 4 100 μL of 1640 medium was added to each well, in 5% CO. 2 , cultured in a 37°C incubator for 24 h; cells were divided into control group (without any treatment, normal culture), sanguinarine treatment group (final concentration of sanguinarine was 2 μM) and sanguinarine and necroptosis inhibitory Co-treatment group (the final concentration of sanguinarine was 2 μM and the final concentration of Nec-1 was 10 μM) (Necrostatin-1, Nec-1), 3 parallels for each treatment; The state of cells in each group was observed under an electron microscope; at the same time, the activity of A549 cells in each treatment group was detected by using CCK-8 kit (Beyotime, product number: C0037).

[0...

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Abstract

The invention belongs to the technical field of medicines, discloses application of sanguinarine in preparation of an RIPK3 activator, and particularly discloses a method for inhibiting the activity of tumor cells with a non-diagnostic or therapeutic purpose, and the method is characterized in that the tumor cells are in contact with sanguinarine or pharmaceutically acceptable salts thereof. The method provided by the invention can effectively inhibit the activity of the tumor cells only by contacting the tumor cells with sanguinarine or pharmaceutically acceptable salts thereof, is simple and easy to operate, and has a better inhibition effect on the activity of the tumor cells.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to the application of sanguinarine in the preparation of RIPK3 activator. Background technique [0002] Necroptosis is a new form of programmed cell death, which is similar to apoptosis in mechanism and necrosis in morphology. Necroptosis is mainly composed of receptor-interacting protein kinase 1 (RIPK1), receptor-interacting protein kinase 3 (RIPK3) and mixed lineage kinase domain-like proteins ( Mediated by mixed lineagekinase domain-like pseudokinas (MLKL), RIPK1 can phosphorylate RIPK3, which in turn phosphorylates MLKL, which leads to necroptosis. Necrotic mechanisms play key roles in the regulation of cancer biology, including tumorigenesis, cancer metastasis, cancer immunity, and cancer subtypes. As a combination of apoptosis and necrosis, necrosis promotes cancer metastasis and cancer progression, but necrosis has also been reported to protect tumor developmen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4741A61P35/00
CPCA61K31/4741A61P35/00
Inventor 罗连响曾凡云赖天文向静黄遵楠曾坚铭李晓玲丁睿罗辉林治平戚怡
Owner GUANGDONG MEDICAL UNIV
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