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Anti-tumor active polymer with pH and glutathione sensitivity and preparation method thereof

An anti-tumor activity, glutathione technology, applied in the direction of anti-tumor drugs, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of easy generation of drug resistance and high doses

Active Publication Date: 2020-01-17
NORTHWEST NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the carrier encapsulating a single anticancer drug still has many disadvantages, such as high dose and easy drug resistance, etc.

Method used

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  • Anti-tumor active polymer with pH and glutathione sensitivity and preparation method thereof
  • Anti-tumor active polymer with pH and glutathione sensitivity and preparation method thereof
  • Anti-tumor active polymer with pH and glutathione sensitivity and preparation method thereof

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Embodiment Construction

[0055] The synthesis of the anti-tumor active polymer DOX@5-FU@ZnO@CdSe@Dex-PTA-PBA of the present invention will be further described below through specific examples.

[0056] (1) Preparation of 3-(7H-purin-6-ylthio)acrylic acid (PTA)

[0057] 6-MP (0.17 g, 1 mmol), sodium methoxide (0.2 g, 3.7 mmol) and propiolic acid (0.07 g, 1 mmol) were added to 20 mL of anhydrous methanol solution under stirring, and the mixture was refluxed for 24 hours before adding 4 mL water to quench the reaction. Excess HCl solution (1 M) was then added to precipitate the product; the precipitate was redissolved in NaOH (1 M) and reprecipitated in HCl (1 M) to give brown-yellow PTA (0.12 g, 54%). 1 H NMR (600 MHz, DMSO- d 6 ) : δ 8.80 (d, J =19.9Hz,1H)-COOH-CH-CH-S-C-N-C H -N,8.77(d,10.1Hz,1H)-COOH-CH-C H -S-C-N-CH-N,8.57(s,1H)-COOH-CH-CH-S-C-C-NH-C H -N,6.29 (d, J =10.1Hz,1H)-COOH-CH -CH-S-C-N-CH-N.

[0058] (2) Preparation of Dex-PTA-PBA

[0059] PTA (0.10g, 0.45mmol), PBA (0.05g, 0.30m...

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Abstract

The invention provides an anti-tumor active polymer with pH and glutathione sensitivity. Natural polymer glucan is used as a main chain and is linked toan anti-cancer drug 6-mercaptopurine through a glutathione-sensitive carbonyl vinylthioether bond; and through the coordination of quantum dots ZnO with DOX, 5-FU and 6-MP, the delivery of three anticancer drugs is achieved. Meanwhile, by using phenylboronic acid as a targeting substance and through coordination of quantum dots CdSe with 6-MP, fluorescence imaging is performed. In vitro release results show that the polymer can be released in the environment of slight acid and glutathione. In vitro cell experiments show that the simultaneous use of the three anticancer drugs can better reduce the survival rate of B16F10 cells and solve thedisadvantages of high dose and high drug resistance caused by a single drug delivery system. The product of the invention is a drug delivery system with wide application prospects.

Description

technical field [0001] The present invention relates to an anti-tumor active polymer, in particular to a pH- and glutathione-sensitive anti-tumor active polymer and a preparation method thereof, belonging to the technical field of compound synthesis and the field of drug delivery. Background technique [0002] Cancer has developed into the number one killer of human health. At present, the use of cytotoxic drugs to kill cancer cells (chemotherapy) is still the main method of cancer treatment, but due to the characteristics of cancer cells easy to transfer and drug resistance, chemotherapy often fails. Due to the ability of nanoparticles (NPs) to prolong blood circulation time and improve the bioavailability of anticancer drugs, nano drug delivery systems (NDDS) have been widely used in recent years. However, the carrier encapsulating a single anticancer drug still has many disadvantages, such as high dosage and easy drug resistance. Adverse effects caused by single-drug ch...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/61A61K31/704A61K31/513A61K31/52A61P35/00A61K49/00
CPCA61K47/61A61K31/704A61K31/513A61K31/52A61P35/00A61K49/0067A61K2300/00
Inventor 袁建超彭立聪祁芊芊周苗伏金平张海亮
Owner NORTHWEST NORMAL UNIVERSITY
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