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Tumor targeting metal complex, synthetic method and application

A technology of tumor targeting and metal complexes, which is applied in the field of medicine and can solve problems affecting normal body functions

Active Publication Date: 2017-06-20
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] At present, anti-tumor drugs have been widely used in the treatment of cancer, but these drugs are selective for tumor cells and normal cells, while treating cancer cells, they also affect normal body functions

Method used

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  • Tumor targeting metal complex, synthetic method and application
  • Tumor targeting metal complex, synthetic method and application
  • Tumor targeting metal complex, synthetic method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Example 1 Preparation and Characterization of Tumor Targeting Complexes

[0116] 1. Preparation of tumor-targeting ruthenium complexes

[0117] (1) Synthesis of ligand 1: as figure 1 As shown, 3.04g (20mmol) of 3,4-diaminobenzoic acid was dissolved in 100mL of absolute ethanol in a single-necked flask, and 2.14g (20mmol) of pyridine-2-carbaldehyde was added dropwise within 20min using a separatory funnel. After reacting at room temperature for 2 hours, evaporate part of the ethanol to 50 mL, add 200 mL of ice water to precipitate a yellow solid, filter to obtain the solid, and then use silica gel column chromatography (silica gel particles 100-200 mesh, purchased from Aladdin Reagent Co., Ltd., the column diameter is 1 cm high) ×10cm, the same below) to purify the above product, dissolve the sample with 3mL ethyl acetate and load the sample, each time the sample volume is 1g, the eluent is a mixed solvent of ethyl acetate and methanol, the volume ratio is 3-1:1, Gradi...

Embodiment 2

[0152] The selective absorption of embodiment 2 ruthenium complexes

[0153] This example detects the targeting of ruthenium complexes to tumor cells from the cell level:

[0154] HeLa cervical cancer cells (purchased from American Type Culture Collection) with high expression of tumor cell biotin receptors and L02 normal liver cells with low expression of biotin receptors (purchased from Nanjing KGI Biotechnology Development Co., Ltd.) were selected to study drug absorption. Cells were cultured in DMEM medium (Gibco, containing 10% (v / v) bovine serum albumin, 100 units / mL penicillin and 50 units / mL streptomycin), placed in a 37°C cell culture incubator (95% relative humidity, Contains 5% (v / v) CO 2 ).

[0155] To demonstrate the tumor-targeting efficacy of the complexes, we used ICP-MS (Inductively Coupled Plasma Mass Spectrometry) to detect the uptake of different selenium-containing drugs. After HeLa and L02 cells were incubated with different selenium-containing compoun...

Embodiment 3

[0157] The antitumor mechanism of embodiment 3 ruthenium complexes

[0158] 1. The cell viability was determined by MTT method:

[0159] HeLa cells, A549 cells, MCF-7 cells, MB231 cells and HepG2 cells, the above tumor cells were purchased from the American Culture Collection; L02 cells were purchased from Nanjing Kaiji Biotechnology Development Co., Ltd.; the above cells were cultured in DMEM medium (containing 10% (v / v) bovine serum albumin, 100units / mL penicillin and 50units / mL streptomycin);

[0160] NCM460 cells were purchased from INCELL, USA, and cultured with INCELL's enriched M3:10 medium;

[0161] All cells were placed in a 37°C cell culture incubator (95% relative humidity, 5% (v / v) CO 2 ).

[0162] Take the above-mentioned various cells of logarithmic growth, and divide them into 2×10 4 The concentration of cells / mL was inoculated in a 96-well plate, and the cells were placed in a 37°C cell culture incubator in DMEM medium. Incubate for 24 hours and wait for t...

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Abstract

The invention discloses a tumor targeting metal complex, a synthetic method and application. The synthetic method comprises the steps of connecting a ligand with a substituent group and a targeting molecule, complexing the ligand and metal ions, and synthesizing to obtain the tumor targeting metal complex, wherein the ligand is one of a phenanthroline derivative, a dipyridyl derivative, a benzimidazole derivative, a phenyl-pyridine derivative and a thiophene-pyridine derivative; the targeting molecule is one of biotin, folic acid, integrin, transferrin, cell-penetrating peptide, octa-poly-L-arginine, MUC-1 attached membrane protein, galactosamine, neovascular targeting peptide and a granulocyte-macrophage colony-stimulating factor; the metal ions are ruthenium, osmium, rhodium or iridium ions. The complex obtained by the method provided by the invention can be selectively absorbed by tumor cells, and induces apoptosis of the tumor cells. In a nude mouse tumor-bearing model, the tumor targeting metal complex can image and treat tumors, and the toxicity of organs and tissues is reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a tumor-targeting metal complex, a synthesis method and an application. Background technique [0002] The morbidity and mortality of cancer in China have been rising, and since 2010, it has become the leading cause of death and a major public health problem in China and the world. According to statistics, 4,292,000 new cancer cases and 2,814,000 cancer deaths are expected to occur in 2015. Among the many strategies for treating cancer, tumor diagnosis and treatment is a comprehensive treatment strategy that combines therapy and diagnostic imaging, which can simultaneously achieve precise medical diagnosis and drug treatment. [B Kumar, et al, Journal of the American Chemical Society, 2014, 136, 17836-17843] Among many materials and compounds, metal complexes with phosphorescent properties have attracted widespread attention in the research of therapeutic agents. Bec...

Claims

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Application Information

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IPC IPC(8): C07F15/00A61K31/555A61P35/00C09K11/06G01N21/64
CPCC07F15/0033C07F15/0053C09K11/06C09K2211/185G01N21/6486
Inventor 陈填烽招振楠
Owner JINAN UNIVERSITY
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