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Polydithioacetal and preparation method and application thereof

A technology of polydithioacetal and hydroxyethyl disulfide, which is applied in the field of polymer materials, can solve the problems of limiting tumor treatment effect, affecting the survival and quality of life of patients, and achieves good biocompatibility and good degradability. sex, the effect of amplifying oxidative stress levels

Active Publication Date: 2020-09-29
SOUTH CHINA UNIV OF TECH
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  • Application Information

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Problems solved by technology

[0002] During the course of chemotherapy, cancer cells will continue to evolve and produce multidrug resistance (MDR), which will seriously limit the effect of tumor treatment and affect the survival and quality of life of patients

Method used

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  • Polydithioacetal and preparation method and application thereof
  • Polydithioacetal and preparation method and application thereof
  • Polydithioacetal and preparation method and application thereof

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Embodiment

[0050] A kind of polydithioacetal, its preparation method comprises the following steps (synthetic route figure is as follows figure 1 shown):

[0051] 1) 2.0g (15.13mmol) of cinnamaldehyde (CA), 3.21g (30.26mmol) of trimethyl orthoformate and 80mg (0.42mmol) of p-toluenesulfonic acid monohydrate were dispersed in 50mL of methanol, heated Reflux for 3h, then dilute the reaction solution with saturated sodium bicarbonate solution, then extract twice with ethyl acetate, collect the organic layer, wash with saturated sodium chloride solution for three times, collect the organic layer, dry with anhydrous magnesium sulfate, and then use The solvent is spin-dried by a rotary evaporator to obtain cinnamaldehyde methyl acetal (CA-acetal);

[0052] 2) Disperse 4.63g (30mmol) of 2-hydroxyethyl disulfide in 30mL of benzene, then disperse 10mg (0.05mmol) of p-toluenesulfonic acid monohydrate in 3.5mL of ethyl acetate, and then The two solutions were mixed, then 1.78g (10mmol) of cinnama...

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Abstract

The invention discloses polydithioacetal and a preparation method and application thereof. The polydithioacetal has the advantages that the biocompatibility and the degradability are good; nano-particles can be formed by self-assembly in a water phase and can be used as a transport carrier of hydrophobic anti-cancer drugs; in an environment with lysosome acidity and high glutathione content in tumor cells, a hydrophobic anti-cancer drug in a particle core can be rapidly released, and the oxidative stress level in the tumor cells is amplified so that the drug resistance is effectively reversed,and huge clinical application potential is achieved.

Description

technical field [0001] The invention relates to a polydithioacetal and its preparation method and application, belonging to the technical field of polymer materials. Background technique [0002] During the course of chemotherapy, cancer cells will continue to evolve and produce multidrug resistance (MDR), which will seriously limit the effect of tumor treatment and affect the survival and quality of life of patients. In the method of reversing multidrug resistance, regulating the level of reactive oxygen species (ROS) is a relatively effective method to kill multidrug-resistant cancer cells with diverse mechanisms. Reactive oxygen species in cancer cells play an important role in regulating and inducing apoptosis, and are closely related to the proliferation, survival and drug resistance of cancer cells. Compared with non-resistant cancer cells and normal cells, the ROS levels and antioxidant enzyme activities of drug-resistant cancer cells were significantly increased, th...

Claims

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Application Information

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IPC IPC(8): C08G18/73C08G18/66C08G18/32C08G18/48A61K9/51A61K47/34A61P35/00
CPCA61K9/5146A61K47/34A61P35/00C08G18/283C08G18/3863C08G18/73
Inventor 袁友永宗庆瑜王可伟肖炫姜茂麟李佶锶
Owner SOUTH CHINA UNIV OF TECH
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