Cell oncosis induction iridium complexes, and preparation method and antitumor application thereof

An iridium complex and reaction technology, applied in the field of biomedicine, can solve the problems of cell apoptosis and other problems, and achieve the effects of strong growth inhibition ability, good inducing activity and small lethality

Inactive Publication Date: 2017-07-11
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is another way of death, cell proliferation and death, which is rarely studied at home and abroad

Method used

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  • Cell oncosis induction iridium complexes, and preparation method and antitumor application thereof
  • Cell oncosis induction iridium complexes, and preparation method and antitumor application thereof
  • Cell oncosis induction iridium complexes, and preparation method and antitumor application thereof

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Experimental program
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Effect test

Embodiment 1

[0084] The synthesis of embodiment 1 cyclometalation Ir (III) complexes

[0085] The synthetic approach of the cyclometalated Ir(III) complex of the present invention is as follows figure 2 As shown, the specific method is as follows:

[0086] (1) The synthesis method of the main ligand 4,4'-dibenzothiazole-2,2'-bipyridine (BBTB):

[0087] 1) Synthesis of 4,4'-dicarboxy-2,2'-bipyridine (BCB):

[0088] First, dissolve 4,4'-dimethyl-2,2'-bipyridine (1.0g) in 50mL of concentrated sulfuric acid, slowly add 5.0g of potassium dichromate solid to oxidize while maintaining the temperature, and the reaction produces a dark green mixed liquid. The reaction solution was poured into 80 mL of ice water to produce a light yellow precipitate, which was filtered and washed with water, and the solid was placed in 30 mL of 50% nitric acid for reflux reaction for 4 hours. Pour the reaction solution into ice cubes and add 800mL of water to dilute, filter with suction to obtain a large amount...

Embodiment 2

[0099] Example 2 Cell Subcellular Organelle Targeting Experiment of Cyclometallated Ir(III) Complexes

[0100] 1. After the cyclometalated iridium (III) complex of the present invention absorbs light of 380nm to 405nm and is irradiated, electrons transition from the ground state to 3 The MLCT orbital is in an excited state, and then emits phosphorescence during the transition back to the ground state (eg image 3 shown).

[0101] 2. In addition, using this property, the distribution state of the complex in the cell can be observed by laser confocal microscopy. Co-staining of this series of complexes with the commercial mitochondrial dye MitoTracker Green FM showed that the series of complexes ([Ir(ppy)BBTB]Cl, [Ir(DFppy)BBTB]Cl, [Ir(2pq)BBTB]Cl, [Ir (pbt)BBTB]Cl) is mainly located in the mitochondria of cells, and its colocalization coefficients (Pearson's Colocalization Coefficients) are 0.83, 0.85, 0.92, 0.87 respectively, and the coincidence rate is relatively high (such ...

Embodiment 3

[0103] Example 3 Cytotoxicity MTT experiment of cyclometalated Ir(III) complexes

[0104] 1. Experimental method

[0105] (1) Experimental samples:

[0106] Ir(III) complexes, the control is the commonly used anti-tumor complex cisplatin CDDP (Pt(NH 3 ) 2 Cl 2 ).

[0107] (2) method

[0108] Tumor or normal cells in the logarithmic growth phase were taken, and the cell density was adjusted to 5×10 3 Each sample / ml was inoculated in a 96-well culture plate, and a total of 5 concentrations were added to each sample in the experiment by logarithmic dilution. Three replicate holes were set for each concentration, and more than eight replicate holes were set for the control.

[0109] Experimental samples were dissolved with DMSO and diluted with DMEM culture medium. After 24 hours of attachment to the wall, add the sample, and still place the cells at 37°C, 5% CO 2 Continue culturing in the incubator for 48 hours, then add MTT, continue culturing for another 4 hours, absor...

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Abstract

The invention discloses cell oncosis induction cyclometallated iridium complexes, and a preparation method and an antitumor application thereof. The structural formula of the cyclometallated iridium complexes is shown in the description. The cyclometallated iridium complexes have very strong growth inhibition ability to various human cancer cells comprising drug-resistant strains, and the action mechanism is based on a new mechanism for inducing cell oncosis not apoptosis based on mitochondrial targeting not traditional nuclear targeting. The complexes overcome the defect of the drug resistance of tumor cells during tumor therapy, and have very good application prospect in the development of high-efficiency antitumor drugs.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to a kind of iridium complex that induces cell growth and death, its preparation method and anti-tumor application. Background technique [0002] Cancer is gradually becoming the number one disease that threatens human survival and quality of life, bringing a heavy burden to patients' families and society. Tumor treatment mainly includes surgical treatment, chemotherapy, and radiotherapy. Among them, chemotherapy, that is, chemotherapy, is one of the most widely used means for treating tumors. Chemotherapy refers to the targeted treatment of cancer with chemical drugs to kill tumor cells. More than 50 chemotherapeutic drugs currently used generally have strong toxic and side effects, and tumor cells are prone to develop drug resistance after long-term use. In addition to organic compound tumor drugs, metal complexes have also been widely used as anti-tumor dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61P35/00
CPCC07F15/0033
Inventor 巢晖关瑞麟计亮年
Owner SUN YAT SEN UNIV
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