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Application of bis-imidazolium salt and drug loading system as anticancer preparation and anticancer preparation

A technology of bis-imidazole salt and bis-imidazole, which is applied in the field of anticancer preparations and can solve the problems of large molecular weight and technical difficulties of competing glycosyltransferases

Pending Publication Date: 2021-12-21
JILIN UNIV
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Problems solved by technology

However, the current gene drugs that inhibit glycosyltransferases still have risks, and the molecular weight of competing glycosyltransferases is large, and there are still technical difficulties in using them as anticancer agents, so anticancer agents with small molecular weights are needed

Method used

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  • Application of bis-imidazolium salt and drug loading system as anticancer preparation and anticancer preparation
  • Application of bis-imidazolium salt and drug loading system as anticancer preparation and anticancer preparation
  • Application of bis-imidazolium salt and drug loading system as anticancer preparation and anticancer preparation

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Embodiment 1

[0066] 1. Experimental materials

[0067] Phosphate buffered saline (PBS, Thermo Fisher Scientific, Shanghai, China) and trypsin-EDTA solution (Xin Saimei, Beijing, China).

[0068] Antibodies such as Bcl-2, Bax, Caspase-3, Caspace-8 and Caspace-9 were obtained from Affinity (Beijing, China).

[0069] Anti-LewisA, Lewis B, Sle X and Lewis Y antibodies were obtained from Abcam (USA).

[0070] TRAIL apoptosis-inducing factor was obtained from Santa Cruz Biotechnology, Inc. (Canada).

[0071] Super ECL detection reagent (Yeasen Biotech Co, Ltd), apoptosis detection kit (TransDetect Annexin V-FITC / PI, Yeasen Biotech, Shanghai, China) and cell cycle detection kit (PI staining, Shanghai, China).

[0072] 2. Synthesis of C20 / C22

[0073] According to the literature (PMID: 23375091), the synthesis of C20 / C22 was carried out, followed by 1 H NMR and LC-ESI-MS analyzed the structure of the compound, and completed the research on the inhibitory activity of various glycosyltransferas...

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Abstract

The invention provides application of bis-imidazolium salt and a drug loading system as an anticancer preparation and the anticancer preparation, and relates to the technical field of anticancer drugs. The invention provides the bis-imidazolium salt C20 / C22 as a glycosyl transferase inhibitor and the drug loading system containing the bis-imidazolium salt C20 / C22, and researches the selective cytotoxicity of the bis-imidazolium salt C20 / C22 on a human umbilical vein endothelial cell (HUVEC) lines and a series of cancer cell lines; and results show that the C20 / C22 and the drug loading system containing the C20 / C22 have clinical potential as the novel anticancer preparation, and are worthy of further development as an auxiliary anticancer drug.

Description

technical field [0001] The invention belongs to the technical field of anticancer drugs, and in particular relates to the application of a bisimidazolium salt and a drug-carrying system as an anticancer agent and an anticancer preparation. Background technique [0002] Cancer is a life-threatening disease. At present, most of the drugs used to treat cancer are broad-spectrum chemotherapeutic drugs. Because of their obvious killing effect on normal cells, they will seriously reduce the quality of life of cancer patients. Therefore, the discovery of new anticancer drugs with selective cytotoxicity, new mechanism of action and less toxic side effects is urgently needed. [0003] Protein glycosylation is the most important post-translational modification process. According to incomplete statistics, more than half of human proteins are glycosylated (PMID: 24339177). Biological dysfunction of the body and abnormal protein folding will lead to abnormal glycosylation; abnormal glyc...

Claims

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Application Information

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IPC IPC(8): A61K31/4178A61K9/51A61K47/42A61P35/00A61P35/04B82Y5/00B82Y40/00
CPCA61K31/4178A61K9/5169A61P35/00A61P35/04B82Y5/00B82Y40/00
Inventor 高印栾雪
Owner JILIN UNIV
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