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Application of iridium complex in preparing mitochondria targeted anti-tumor drugs

A technology of anti-tumor drugs and iridium complexes, applied in the field of anti-tumor drugs, can solve the problems of poor recognition of differences between normal cells and tumor cells, toxic and side effects of tumor patients, etc.

Inactive Publication Date: 2018-10-12
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Due to the excellent cytotoxicity of traditional chemotherapy drugs, chemotherapy has become an important means of clinical treatment of tumor diseases. However, due to its poor ability to recognize the difference between normal cells and tumor cells, it has caused serious harm to tumor patients in clinical applications. Toxic side effects, which are the leading cause of treatment discontinuation and treatment failure

Method used

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  • Application of iridium complex in preparing mitochondria targeted anti-tumor drugs
  • Application of iridium complex in preparing mitochondria targeted anti-tumor drugs
  • Application of iridium complex in preparing mitochondria targeted anti-tumor drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0013] Example 1 Determination of Antitumor Activity of Iridium Complexes in Vitro

[0014] Screened cell lines include: tumor cells HeLa, A-549, HepG2, MCF-7, and cisplatin-resistant strain CP / R-A549, and normal human embryonic liver cells L02 were used as control cells. Cisplatin was used as positive control drug. The determination adopts bromide tetrazolium blue (MTT) method, its principle is: bromide tetrazolium blue [MTT,3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide] is A dye that can accept hydrogen atoms. The dehydrogenase associated with NADP in the mitochondria of living cells can convert yellow MTT into insoluble blue-purple formazan in cells, while dead cells have no such function. After dissolving formazan with dimethyl sulfoxide (DMSO), measure the optical density value with a microplate reader at a certain wavelength, and the survival rate of the cells can be quantitatively measured. Experimental procedure: Take tumor cells in the logarithmic gr...

Embodiment 2

[0019] Example 2 Mitochondria targeting

[0020] Take the HeLa cells in the logarithmic growth phase and adjust the concentration to 1×10 4 / mL, inoculate into 35mm cell culture dish, wait for the cells to grow to 60% confluence, add iridium complex and mitochondria-specific fluorescent probe Mito-Tracker, incubate for 30 minutes, and detect with laser confocal microscope (Zeiss Axio Observer D1) The iridium complex is localized in the cell, the experimental results are as follows figure 1 Shown (A is the iridium complex (green fluorescence), B is the mitochondria-specific fluorescent probe (red fluorescence), C is the nuclear dye DAPI image (blue fluorescence), D is the superposition of A, B and C). Experiments show that, figure 1 -D shows that the green fluorescence emitted by the iridium complex and the red fluorescence emitted by the mitochondria-specific fluorescent probe are superimposed to present orange fluorescence, which proves that the iridium complex can be targe...

Embodiment 3

[0021] Example 3 Iridium complex induces tumor cell apoptosis

[0022] Flow cytometry Annexin-V staining method was used for the measurement. The principle is: Phosphatidylserine (PS) is normally located on the inner side of the cell membrane, but in the early stage of apoptosis, PS can be turned from the inner side of the cell membrane to the surface of the cell membrane. exposed to the extracellular environment. Annexin-V is a Ca 2+ Dependent phospholipid-binding protein, which can specifically bind to PS with high affinity. The Annexin-V is labeled with fluorescein (FITC), and the labeled Annexin-V is used as a fluorescent probe to detect the occurrence of apoptosis by flow cytometry. Experimental procedure: HeLa cells in the logarithmic growth phase were mixed with 5x 10 4 Cells / mL were seeded in a 6-well plate, 2 mL per well, placed at 37°C, 5% CO 2 After culturing in a saturated humidity incubator for 24 hours, different concentrations of iridium complexes were added...

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Abstract

The invention discloses application of an iridium complex in preparing mitochondria targeted anti-tumor drugs. The structural formula of the iridium complex is [Ir(ppy)2(HPIP)]C1, wherein ligand represented by ppy is 2-phenylpyridine, ligand represented by HPIP is 3-(1H-imidazole[4,5-f][1,10]phenanthroline-2-yl)phenol. The iridium complex has the high inhibiting effect on human tumor cells HeLa, HepG2, A-549 and a cisplatin resistant strain CP / R-A549, mitochondria in tumor cells can be stored up, tumor cell apoptosiss can be induced, and the iridium complex can serve as the new anti-tumor drugtaking tumor cell mitochondria as target sites.

Description

technical field [0001] The invention belongs to the technical field of anti-tumor drugs, and in particular relates to the application of an iridium complex in the preparation of mitochondria-targeted anti-tumor drugs. Background technique [0002] About 7.6 million people die of cancer every year in the world, accounting for 13% of the total death toll. Every year, 12.7 million cancer patients are diagnosed worldwide. In my country, about 1.5 million people die of cancer every year, and the trend is gradually increasing every year. Tumor treatment mainly includes three aspects: surgery, radiation therapy and chemotherapy. Chemotherapy is the method of treating diseases with chemically synthesized drugs. Due to the excellent cytotoxicity of traditional chemotherapy drugs, chemotherapy has become an important means of clinical treatment of tumor diseases. However, due to its poor ability to recognize the difference between normal cells and tumor cells, it has caused serious h...

Claims

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Application Information

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IPC IPC(8): A61K31/555A61P35/00C09K11/06
CPCA61K31/555A61P35/00C09K11/06C09K2211/185
Inventor 肖秋妙王金全
Owner GUANGDONG PHARMA UNIV
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