Amphipathic oxaliplatin precursor, preparation method and application thereof

An oxaliplatin, amphiphilic technology, applied in the field of amphiphilic oxaliplatin precursors, can solve ototoxicity, neurotoxicity and bone marrow toxicity, reduction of the actual efficacy of oxaliplatin, gastrointestinal reactions, etc. question

Active Publication Date: 2016-10-26
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, platinum-based antineoplastic drugs are likely to cause severe gastrointestinal reactions, nephrotoxicity, ototoxicity, neurotoxicity, and bone marrow toxicity during clinical use.
At the same time, oxalipla

Method used

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  • Amphipathic oxaliplatin precursor, preparation method and application thereof
  • Amphipathic oxaliplatin precursor, preparation method and application thereof
  • Amphipathic oxaliplatin precursor, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1. Preparation of oxidized oxaliplatin

[0040] Weigh 500 mg of oxaliplatin, suspend it in 10 ml of deionized water, add 3 ml of 30% hydrogen peroxide, place it in a 50 ml round bottom flask, stir and react in the dark at 30 degrees Celsius for 12 hours, remove the solvent by rotary evaporation, add methanol to dissolve the resulting substance, Precipitate with ether and dry in vacuum to obtain oxaliplatin oxide. The resulting material was characterized by proton nuclear magnetic resonance spectroscopy, and the results were as follows: figure 1 shown.

Embodiment 2

[0041] Embodiment 2. Preparation of monocarboxylated oxaliplatin

[0042] Take 215 mg of oxidized oxaliplatin prepared in Example 1, dissolve it in 5 ml of anhydrous dimethyl sulfoxide, add 50 mg of succinic anhydride, react at 25°C for 12 hours, precipitate with ether, dissolve the obtained substance in methanol, and then remove it by rotary evaporation Methanol, the resulting precipitate was washed with ether, and vacuum-dried to obtain monocarboxylated oxaliplatin. The resulting material was characterized by proton nuclear magnetic resonance and mass spectrometry, and the results were as follows: figure 2 shown.

Embodiment 3

[0043] Example 3. Alkylation of Monocarboxylated Oxaliplatin

[0044] Take 60 mg of the monocarboxylated oxidized oxaliplatin prepared in Example 2, dissolve it in 3 ml of anhydrous N,N-dimethylformamide, add 45.33 mg of hexadecyl isocyanate, and place it at 25° C. to stir the reaction Concentrate overnight by rotary evaporation, wash the resulting substance with ether, and dry in vacuo to obtain monocarboxylated and alkylated oxaliplatin. The resulting material was characterized by proton nuclear magnetic resonance and mass spectrometry, and the results were as follows: image 3 shown.

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Abstract

The invention discloses an amphipathic oxaliplatin precursor and a preparation method thereof. The amphipathic oxaliplatin precursor comprises an oxaliplatin unit and hydrophobic and hydrophilic functional groups. The amphipathic oxaliplatin precursor can be self-assembled solely into a micelle in water, the hydrophobic functional group of the amphipathicoxaliplatin precursor can form a hydrophobic core through hydrophobic interaction, the hydrophilic functional group forms a hydrophilic shell layer to maintain colloid stability of the self-assembled micelle. In addition, the invention further discloses application of the amphipathic oxaliplatin precursor. The amphipathicoxaliplatin precursor is mainly used for preparing cancer treatment drugs.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and in particular relates to an amphiphilic oxaliplatin precursor, its preparation method and application. Background technique [0002] Chemotherapy is one of the main means of current cancer treatment, among which (divalent) platinum drugs have the characteristics of good anti-cancer effect and wide indications, so at present, cisplatin (Cisplatin), carboplatin (Carboplatin) and oxalate are mainly used clinically. Oxaliplatin is used to treat various malignant tumors. However, most platinum antineoplastic drugs are likely to cause severe gastrointestinal reactions, nephrotoxicity, ototoxicity, neurotoxicity and bone marrow toxicity during clinical use. At the same time, oxaliplatin can easily lead to acquired drug resistance, which seriously reduces the actual curative effect of oxaliplatin and significantly narrows the scope of indications, thereby limiting the clinical...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/0093
Inventor 于海军李亚平冯兵周方圆付元磊崔智睿
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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