Ruthenium complex and application thereof

A ruthenium complex and reaction technology, applied in the field of ruthenium complexes, can solve the problems of large toxic and side effects, low selectivity, etc., and achieve the effects of high selectivity, good anticancer activity, and low normal cytotoxicity

Inactive Publication Date: 2016-05-25
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such ruthenium complexes have the disadvantages of large toxic side effects and low selectivity.

Method used

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  • Ruthenium complex and application thereof
  • Ruthenium complex and application thereof
  • Ruthenium complex and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1 mononuclear ruthenium complex [Ru(phen) 2 ( HIPMP )] (ClO 4 ) 2 Synthesis

[0038] (1) Dissolve 1,10-phenanthroline-5,6-dione, ammonium acetate and 5-methyl salicylaldehyde in an appropriate amount of glacial acetic acid at a ratio of 1:20:1, inert The mixture was mixed and heated to reflux for 4 hours under gas protection. After the mixture was cooled to room temperature, water was added, neutralized with 25% ammonia water, filtered with suction, and the yellow precipitate was washed with water and diethyl ether to obtain the corresponding crude product. The crude product was dissolved with a small amount of ethanol, packed into a column with silica gel (60-100 mesh), and ethanol was used as eluent, and the yellow fraction was collected and rotary evaporated to obtain a yellow powder 2-(1 H- imidazo-[4,5-f][1,10]phenanthrolin-2-yl)-4-methylphenol (the intermediate HIPMP ). Yield: 83%. Anal. Calcd for C 20 h 14 N 4 O:C,73.61;H,4.32;...

Embodiment 2

[0041] Example 2 Inhibitory effect of mononuclear ruthenium (II) complexes on proliferation of tumor cells HeLa, A549, HepG2 and CNE-1

[0042] Cytotoxicity test: MTT method was used to study the in vitro toxicity test of the complex. First, place the experimental cells at 37°C, 5.0% CO 2 Grow to the logarithmic phase in the incubator, digest the cells with 0.25% trypsin, and adjust the concentration of the cell suspension so that the cell density is about 1×10 4 Cells / mL, 100mL per well was inoculated in a 96-well plate, and the cell density was about 3-5×10 3 pc / well, placed at 37℃, 5%CO 2 cultured in an incubator for 24 h. Change the medium, add drugs with different concentration gradients, make 3 parallel samples for each concentration, set up blank zero-adjustment group (medium, MTT, DMSO), blank group (medium, cells, drug dissolution medium with the same concentration, MTT, DMSO), positive control group (medium, cells, different concentrations of cisplatin, MTT, DM...

Embodiment 3

[0047] Example 3 Mononuclear ruthenium (II) complex using AnnexinV and PI double staining method to study HeLa cell apoptosis experiment

[0048] Alexafluor ? 488annexinV / PI double staining method is a semi-quantitative cell apoptosis analysis method detected by flow cytometry (Vermes, C.Haanen, H.Steffens-Nakken and C.Reutellingsperger, J.Immunol.Methods, 1995,184,39 -51.), the specific experimental steps are as follows: collect logarithmic phase cells, adjust the concentration of cell suspension, 1 × 10 per well in a 6-well plate 5 cells. Placed at 37°C, 5% CO 2 Cultivate for about 24 hours in an incubator. Change the medium, add 1mL of different concentrations (10, 20, 40μM) of drugs, three parallel wells for each concentration, and set a blank control well with the same concentration of drug dissolution medium at the same time, and continue to incubate for 24h. Carefully suck off the supernatant, collect the cells by digesting with 0.25% trypsin, and adjust the conce...

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Abstract

The invention discloses a ruthenium complex and application thereof. The cation part of the ruthenium complex is [Ru(phen)2(HIPMP)]<2+>, and the anion part is (ClO4)[-] or Cl[-]. The mononuclear ruthenium complex has favorable anticancer activities, and has obvious treatment effects on cervical cancer cells, liver cancer cells, lung cancer cells nasopharyngeal carcinoma cells and other cancers. The tumor cell apoptosis induction of the mononuclear ruthenium complex mainly relates to endogenous endoplasmic reticulum channels, and has important meanings for researching high-efficiency ruthenium antineoplastic drugs.

Description

technical field [0001] The invention specifically relates to a ruthenium complex and its application. Background technique [0002] Cancer is one of the most important diseases threatening human health and life safety. About 12.7 million people are diagnosed with cancer every year in the world, and the number of people who die from cancer accounts for 13% of the total number of deaths worldwide every year. About 1.5 million people die of cancer every year in my country, and the trend is increasing year by year. Since cisplatin was found to have anticancer activity, the application and research of platinum-based metal anticancer drugs have developed rapidly. Among them, the anti-tumor mechanism of platinum-based drugs mainly uses DNA as the main target, destroying DNA replication and inhibiting cell division to inhibit the growth of tumor cells. However, the long-term use of platinum-based drugs has the disadvantages of large toxic and side effects, strong drug resistance ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/555A61P35/00
CPCC07F15/0053
Inventor 徐丽刘钰颖钟南京赖显春邹健
Owner GUANGDONG PHARMA UNIV
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