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Method for inhibiting cell activity through intracellular polymerization and prodrug for implementing method

A technology of prodrugs and polymerization inhibition, which is applied in the direction of drug combination, organic active ingredients, antineoplastic drugs, etc., can solve the problems of low uptake efficiency, high molecular weight polymer molecule difficulty, and cell toxicity, etc., to reduce cell activity, Achieve highly controllable and selective effects

Pending Publication Date: 2021-10-12
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is generally believed that high-molecular-weight polymers have higher biocompatibility than small molecules. This is because high-molecular-weight polymer molecules are difficult to be directly absorbed by cells, and the larger the molecular weight, the lower the uptake efficiency. The effect on cells requires in situ synthesis of polymer molecules in cells, but so far there is no relevant report on whether it can be toxic to cells through intracellular polymerization

Method used

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  • Method for inhibiting cell activity through intracellular polymerization and prodrug for implementing method
  • Method for inhibiting cell activity through intracellular polymerization and prodrug for implementing method
  • Method for inhibiting cell activity through intracellular polymerization and prodrug for implementing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Embodiment 1: RAFT chain transfer agent 2-(butylthiocarbonylthiothiolthio) propionic acid (RAFTCTA) synthetic steps

[0071] Within 30min, add 50mL THF solution containing 16.0g n-butanol dropwise to 150mL THF suspension containing 9.0g KOH, stir at room temperature for 30min, then add dropwise 50mL solution containing 17.0g CS 2 After stirring at room temperature for 24 hours, the THF solution was concentrated to 50 mL under reduced pressure. Under stirring, 50 mL of THF solution containing 22.4 g of n-propylammonium bromide was added dropwise to the above concentrated solution. After stirring at room temperature for 24 hours, the solvent was removed under reduced pressure to obtain the target crude product. The product was further purified by silica gel column chromatography to obtain the target product as bright yellow crystals.

Embodiment 2

[0072] Example 2: CCK-8 test characterizes cell viability

[0073] In the CCK-8 test, HeLa cells were first treated with 1x 10 4 The density was inoculated in a 96-well cell culture plate and incubated at 37°C and 4% carbon dioxide for 18 hours at a constant temperature to ensure that the cells adhered to the wall; 2), and continue to incubate at constant temperature for 24 hours; after 24 hours, suck out the original medium and wash the cells with PBS for 3 times, add 100 μL of diluted CCK-8 solution (ratio to medium: 1:10) to each well, incubate at constant temperature for 4 hours and use The microplate reader detects the ultraviolet absorption at 450nm in each well, and compares the absorbance of the treated cells with the untreated cells to obtain the cell activity value.

Embodiment 3

[0074] Example 3: Effects of 470nm illumination at different times on the activity of HeLa cells

[0075] HeLa cells at 1x 10 4 The densities were inoculated in three 96-well cell culture plates, and incubated at 37°C and 4% carbon dioxide for 18 hours at a constant temperature; then, 470nm LED blue light was irradiated vertically from the bottom of the three culture plates for 5, 10, and 20 minutes respectively.

[0076] Cell viability before and after light exposure can be quantitatively characterized by the CCK-8 assay as described above. (2-(2-Methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfonic acid phenyl)-2H-tetrazole monosodium salt, It can be catalyzed and reduced by enzymes in the mitochondria of cells, and the amount of reduction is proportional to the number of cells, so it is widely used in the test of cell activity).

[0077] Such as figure 2 As shown, the cell viability remained above 88% after the cells were irradiated with blue light for 5-10 minutes...

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Abstract

The invention discloses a method for inhibiting cell activity through intracellular polymerization and a prodrug for implementing the method. The prodrug is prepared from N,N-dimethylacrylamide, an RAFT chain transfer agent 2-(butylthiocarbonothioylthio)propionic acid and a photoinitiator eosin Y. The precursor drug and cells are incubated together, and polymerization reaction in the cells is initiated by illumination to realize in-situ synthesis of a high-molecular polymer in the cells. The intracellular in-situ synthesized high-molecular polymer can effectively influence the cell viability and induce cell apoptosis and autophagy.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to a method for inhibiting cell activity and a prodrug for realizing the method, in particular, to a method of in situ synthesizing a linear polymer in a cell to cause toxicity to cells, Thereby inhibiting cellular activity and prodrugs to accomplish this. Background technique [0002] Prodrugs, that is, low-activity substances that can be activated in situ in vivo by enzymes or chemical stimuli (to generate highly active drug molecules), can significantly improve the water solubility of many traditional drugs through targeted modification of drug molecules, chemical / Biological stability, oral absorption efficiency, in vivo circulation time, systemic toxicity and many other clinical problems. 5-7% of all drugs currently on the market can be identified as prodrugs, and this proportion is still growing, which shows that it plays an important role in the development and application...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/785A61P35/00C08F120/54C08F2/38C08F2/48
CPCA61K31/785A61P35/00C08F120/54C08F2/38C08F2/48C08F2438/03
Inventor 耿晋张一川高权连前进何荣坤
Owner SHENZHEN INST OF ADVANCED TECH
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