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
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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 m

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  • 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

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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;

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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

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Application Information

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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
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