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A kind of berberine anti-tumor platinum (ii) complex and its synthesis method and application

An anti-tumor drug, anti-tumor technology, applied in the direction of anti-tumor drugs, platinum-based organic compounds, platinum-based organic compounds, etc., to achieve the effects of mild reaction conditions, targeted inhibition of proliferation, and high yield

Active Publication Date: 2021-09-07
YULIN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, there have been no related reports on the synthesis of metal complexes and their mechanism of action using berberine (berberine) derivatives as active ingredients of traditional Chinese medicine.

Method used

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  • A kind of berberine anti-tumor platinum (ii) complex and its synthesis method and application
  • A kind of berberine anti-tumor platinum (ii) complex and its synthesis method and application
  • A kind of berberine anti-tumor platinum (ii) complex and its synthesis method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] In high temperature pressure tube were weighed 1.0mol derivative 1,0.8mol 3.20mol of potassium iodide and dimethyl pyridine amine, 5.0 ml of acetonitrile was added, the solvent was added to dissolve the solid test just completed, more fully reacted, in 90 after 12 hours of reaction at ℃, to give a yellow solid powder B-TFA ligand, a yield of 94.0%.

[0036] Weigh ligand B-TFA 1.0mol dichloride and bis (dimethyl sulfoxide) platinum (II) 1.0mol 100.0mL pressure bottle was placed in a high temperature, was added 25.0 mL of acetonitrile, at 60 deg.] C for coordination reaction 4.0h, washed with acetonitrile and dried in vacuo at 45 ℃, i.e. to give the desired product as a yellow Pt1. The yield was 90.8%.

[0037] Berberine present invention antitumor platinum (II) complex scheme is as follows:

[0038]

Embodiment 2

[0040] Unlike Example 1, except that the ligand weighed B-TFA (1.0mol) dichloride and bis (dimethyl sulfoxide) platinum (II) (1.0mol) was placed in a high temperature pressure 100.0mL flask, a solution of 10.0 mL of acetonitrile, is coordinated reaction of 4.0h at 60 deg.] C, washed with acetonitrile and dried in vacuo at 45 ℃, i.e. to give the desired product as a yellow Pt1. The yield was 85.6%.

Embodiment 3

[0042] Unlike Example 1, except that the ligand weighed B-TFA (1.0mol) dichloride and bis (dimethyl sulfoxide) platinum (II) (1.0mol) was placed in a high temperature pressure 100.0mL flask, 75.0 mL of acetonitrile, is coordinated reaction of 4.0h at 60 deg.] C, washed with acetonitrile and dried in vacuo at 45 ℃, i.e. to give the desired product as a yellow Pt1. The yield was 80.0%.

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Abstract

The invention relates to a berberine anti-tumor platinum (II) complex, its synthesis method and the application of the complex in the preparation of anti-tumor drugs. The synthesis method of the berberine anti-tumor platinum (II) complex comprises the following steps: (1) dissolving the brominated berberine derivative, potassium halide and lutidine amine in a solvent, and reacting at 90° C. to obtain B ‑TFA ligand; (2) the B‑TFA ligand prepared in step (1) and dichlorobis(dimethylsulfoxide) platinum (II) are dissolved in acetonitrile solution, and carry out coordination reaction 4~6 Hours, the product was washed and dried to obtain. The present invention uses the brominated berberine derivative B-TFA as the active ligand for the first time to synthesize its platinum complex, which exhibits superior anti-tumor activity and targeting in vivo and in vitro, has potential medicinal value, and is expected to be used in various Preparation of antineoplastic drugs. The structural formula of the berberine anti-tumor platinum (II) complex is as follows:

Description

Technical field [0001] The present invention relates to a high active platinum complexes, and synthetic methods, in particular to a berberine antitumor platinum (II) complexes and their synthesis. The present invention further relates to berberine antitumor platinum (II) was prepared with the application of anti-tumor drugs. Background technique [0002] Since cisplatin is found, there have been Nida, oxaliplatin, Shu platinum and platinum music four anti-cancer drugs on the market to use, but still unsatisfactory in improving the efficacy, reduced toxicity and overcome terms of cross-resistance . Scientists and researchers to platinum by various structural modifications, trying to synthesize a new class of anti-tumor platinum complexes, hoping to find more active, less toxic platinum anti-cancer drugs by such an attempt. [0003] The main chemical composition of yellow vine yellow vine alkaloids, mainly located in the region of Guangxi, Yunnan and Guangdong, which is one of the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F15/00A61P35/00
CPCA61P35/00C07F15/0093
Inventor 覃其品王振凤黄小玲
Owner YULIN NORMAL UNIVERSITY
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