Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Anti-cancer conjugate containing tetravalent platinum and preparation method and application thereof

A technology of conjugates and tetravalent platinum, which is applied in the field of anti-cancer conjugates containing tetravalent platinum and its preparation, can solve the problems of unknown safety of polymers, inability to degrade polymers, and lack of active targeting molecules in the carrier system And other issues

Active Publication Date: 2018-11-06
HUAZHONG UNIV OF SCI & TECH
View PDF5 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this kind of drug molecular conjugates mainly has the following problems: (1) the safety of drug carrier polymers is unknown, and most of the polymers cannot be degraded in the human body; (2) polymer drug conjugates need further research Only through the preparation process can nano drug-loaded particles be obtained, which may introduce toxic reagents such as ether and chloroform; (3) the above-mentioned carrier system lacks active targeting molecules, which makes it difficult to enter cells; (4) the preparation method of polymer copolymers is relatively It is cumbersome, which increases the complexity of the process and the difficulty of quality control

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Anti-cancer conjugate containing tetravalent platinum and preparation method and application thereof
  • Anti-cancer conjugate containing tetravalent platinum and preparation method and application thereof
  • Anti-cancer conjugate containing tetravalent platinum and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] The invention provides a targeted anticancer drug galactose-hydroxyethyl starch-platinum (IV) conjugate, with cisplatin as platinum (II), succinic anhydride as a connecting arm, and hydroxyethyl starch selected at 200 / 0.5 specification:

[0082] (1) Disperse cisplatin 1.00g (3.33mmol) in 25mL of water, then add 35mL of 30% hydrogen peroxide (30.0mmol), and stir and react at 50°C for 1h to obtain reaction solution A;

[0083] (2) Centrifuge the obtained reaction solution A at a speed of 9000 rpm for 5 minutes to obtain a white precipitate, which is washed with water, ethanol, and ether respectively, 50 mL each time, and then vacuum-dried at room temperature for 2 hours to obtain dry The white solid is cis-dichlorodihydroxydiammine platinum (IV);

[0084] (3) Disperse 500 mg (1.5 mmol) of the obtained cis-dichlorodihydroxydiammine platinum (IV) in 40 mL of dimethyl sulfoxide, add 150.1 mg (1.5 mmol) of succinic anhydride, and stir the reaction at 45 ° C for 12 h , to o...

Embodiment 2

[0091] The invention provides a targeted anticancer drug galactose-hydroxyethyl starch-platinum (IV) conjugate, with carboplatin as platinum (II), succinic anhydride as a connecting arm, and hydroxyethyl starch of 130 / 0.4 specifications:

[0092] (1) Disperse 1.24 g (3.33 mmol) of carboplatin in 25 mL of water, then add 35 mL of 30% hydrogen peroxide (30.0 mmol), and stir and react at 50° C. for 1 h to obtain reaction solution A;

[0093] (2) Centrifuge the obtained reaction solution A at a speed of 9000 rpm for 5 minutes to obtain a white precipitate, which is washed with water, ethanol, and ether respectively, 50 mL each time, and then vacuum-dried at room temperature for 2 hours to obtain dry The white solid is Pt(IV)-(OH)2B;

[0094] (3) Pt(IV)-(OH) to be obtained 2 Disperse 608mg (1.5mmol) of B in 40mL dimethyl sulfoxide, add 150.1mg (1.5mmol) of succinic anhydride, stir and react at 45°C for 12h, and obtain reaction solution B;

[0095] (4) Pour the obtained reaction...

Embodiment 3

[0101] The invention provides a targeted anticancer drug galactose-hydroxyethyl starch-platinum (IV) conjugate, with oxaliplatin as platinum (II), succinic anhydride as a connecting arm, and hydroxyethyl starch selected from 480 / 0.5 specifications:

[0102] (1) Disperse 1.32g (3.33mmol) of oxaliplatin in 25mL of water, then add 35mL of 30% hydrogen peroxide (30.0mmol), and stir and react at 50°C for 1h to obtain reaction solution A;

[0103] (2) Centrifuge the obtained reaction solution A at a speed of 9000 rpm for 5 minutes to obtain a white precipitate, which is washed with water, ethanol, and ether respectively, 50 mL each time, and then vacuum-dried at room temperature for 2 hours to obtain dry The white solid is Pt(IV)-(OH)2C;

[0104] (3) Pt(IV)-(OH) to be obtained 2 646 mg (1.5 mmol) of C was dispersed in 40 mL of dimethyl sulfoxide, 150.1 mg (1.5 mmol) of succinic anhydride was added, and the reaction was stirred at 45°C for 12 hours to obtain reaction solution B;

...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Diameteraaaaaaaaaa
Molecular weightaaaaaaaaaa
Login to View More

Abstract

The invention provides an anti-cancer conjugate containing tetravalent platinum and a preparation method and application thereof. The anti-cancer conjugate containing tetravalent platinum is a galactose-modification hydroxyalkyl starch-platinum (IV) conjugate; the hydroxyalkyl starch-platinum (IV) conjugate is formed by connecting a tetravalent platinum complex with hydroxyalkyl starch through anester bond. The prepared galactose-hydroxyalkyl starch-platinum (IV) conjugate can prolong circulation time of platinum drugs in blood, enhance enrichment of the platinum drugs in tumor sites and improve the curative effects of the platinum drugs on tumors.

Description

technical field [0001] The invention relates to the field of anticancer drugs, in particular to an anticancer conjugate containing tetravalent platinum and its preparation method and application. Background technique [0002] Cis-dichlorodiammine platinum (II) (referred to as cisplatin, CDDP) is a broad-spectrum anti-tumor drug, which can form a tight combination with DNA to destroy the DNA replication of tumor cells, inhibit cell division, and eventually kill Tumor cells, cisplatin has been widely used in the treatment of various malignant tumors at home and abroad. Since cisplatin was successfully marketed for 40 years, research on the development and formulation of platinum-derived drugs has never stopped. It is mainly to solve the problems of poor water solubility of cisplatin, low bioavailability, short half-life, short duration of action and relatively large toxic and side effects. Although the platinum antitumor drugs that have been developed and marketed all have c...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/61A61K33/24A61K31/555A61P35/00B82Y5/00
CPCA61K31/555A61K33/24A61K47/61A61P35/00B82Y5/00
Inventor 李子福杨祥良万江陵肖晨
Owner HUAZHONG UNIV OF SCI & TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com