Ruthenium complex and preparation method thereof and purpose of product as histone deacetylase inhibitor

A technology of ruthenium complexes and compounds, applied in the field of ruthenium complexes with excellent anti-tumor activity and its preparation, can solve the problems of histone hypoacetylation and achieve good anti-tumor activity

Inactive Publication Date: 2015-07-15
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, in the state of cell transformation, the activity of HDACs is significantly enhanced. Current studies have confirmed that there are overexpressions of different HDACs family proteins in various tumor cell samples, so that most of the histones in tumor cells are hypoacetylated. state

Method used

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  • Ruthenium complex and preparation method thereof and purpose of product as histone deacetylase inhibitor
  • Ruthenium complex and preparation method thereof and purpose of product as histone deacetylase inhibitor
  • Ruthenium complex and preparation method thereof and purpose of product as histone deacetylase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] (1) Preparation of ligands:

[0055] Add 5-amino-1,10-phenanthroline (0.629 g, 3.226 mmol) and methyl 8-chloro-8-oxooctanoic acid (1 g, 4.839 mmol) into the reaction flask, and add catalytically metered DMAP , then stirred at room temperature in 45 ml of DMF solvent for 12 h, then rotary evaporated to remove most of the DMF, added a large amount of ether, filtered to obtain a light yellow solid, then added 50% aqueous hydroxylamine solution (the amount of the substance added to the aqueous hydroxylamine solution was light yellow 20 times that of the solid), methanol as the solvent (4 mL), add 1N NaOH solution (2 mL) and stir at room temperature for 30 min, adjust the pH to neutral with 1N HCl, you can see a light yellow precipitate formed, filter The ligand was obtained with a yield of 40%.

[0056] Elemental Analysis C 20 h 22 N 4 o 3 (Molecular weight is 366.4), theoretical value: C 65.56%, H 6.05%, N 15.29%; experimental value: C 65.17%, H 6.01%; N 14.96%. ESI-...

Embodiment 2

[0066] Example 2 Inhibition test of Ru(Ⅱ) complexes on histone deacetylase

[0067] HDAC enzyme activity test: the ability of ruthenium complexes to inhibit histone deacetylase is mainly detected by a fluorescent HDAC activity assay kit. The operation steps are roughly as follows. Add 0.5 μL of HeLa nuclear extract to a 96-well culture plate , then add HDAC substrate, 100 μL HDAC assay buffer, the negative control is without HeLa nuclear extract and HDAC substrate, and the wells where 1 μM Trichostatin A is added are set as positive control. Incubate the above reaction mixture in a 37°C incubator for 30 min, then add 10 μL of lysine developer to terminate the reaction, continue to incubate in a 37°C incubator for 30 min, take it out, and place the plate on a multi-functional microplate reader for determination For fluorescence values, the excitation wavelength was set to 340 nm and the emission wavelength was set to 460 nm. Histone deacetylase activity is expressed as relativ...

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Abstract

The invention discloses a ruthenium complex and preparation method thereof and purpose of product as histone deacetylase inhibitor, specifically speaking, the invention discloses a ruthenium complex with histone deacetylase inhibitor effect [Ru(N-N)2L](PF6)2, wherein, L is N1-hydroxy-N8-(1,10 phenanthroline) octanedioyl amine, N-N=2,2 ' -dipyridine is the complex 1, N-N=1, 10-phenanthroline is the complex 2, N-N=4, 7-dibenzyl-1, 10-orthophenanthrolene is the complex 3 and the structural formula is shown in the formula (I). The anticancer activity and histone deacetylase activity of the ruthenium complex are researched, and the complex 3 not only can inhibit the activity of the histone deacetylase, but also has an excellent antineoplastic activity.

Description

technical field [0001] The invention relates to a ruthenium complex with histone deacetylase inhibitor function and a preparation method thereof, in particular to a ruthenium complex with excellent antitumor activity and a preparation method thereof. Background technique [0002] Epigenetics is the study of heritable phenotypic changes in gene expression without changes in the genomic DNA sequence. There are many epigenetic phenomena, such as DNA methylation, histone modification, genome imprinting, chromosome inactivation, and non-coding RNA. As an important part of epigenetics, histone modification has attracted more and more attention in recent years. The disorder of histone modification can lead to abnormal gene expression, which affects the important physiological functions of cells, and then leads to the formation of tumors. Among them, the acetylation level of histones is closely related to the occurrence and proliferation of tumors, and the expression levels of onc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D471/04C07F15/00A61K31/4745A61P35/00
Inventor 谭彩萍叶瑞绒毛宗万黄华珍计亮年
Owner SUN YAT SEN UNIV
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