Microwave-Assisted Synthesis, Characterisation, and DNA-Binding Properties of RuII Complexes Coordinated by Norfloxacin as Potential Tumour Inhibitors

2019 ◽  
Vol 72 (5) ◽  
pp. 400
Author(s):  
Xukui Liu ◽  
Xuanhao Zhao ◽  
Yumei Li ◽  
Kangdi Zheng ◽  
Qiong Wu ◽  
...  
Keyword(s):  
Dna Binding ◽  
Electrostatic Interactions ◽  
13C Nmr Spectroscopy ◽  
Microwave Assisted Synthesis ◽  
1H And 13C Nmr ◽  
Ionisation Mass Spectrometry ◽  
Calf Thymus ◽  
Viscosity Study ◽  
Lung Adenocarcinoma A549 ◽  
Dna Binding Properties

Three novel norfloxacin-based ruthenium(ii) complexes, [Ru(bpy)2(NFLX)]Cl·2H2O (1), [Ru(phen)2(NFLX)]Cl·2H2O (2), and [Ru(dmbpy)2(NFLX)]Cl·2H2O (3) (bpy=2,2′-bipyridine, phen=1,10-phenanthroline, dmbpy=4,4′-dimethyl-2,2′-bipyridine, and NFLX=norfloxacin), were synthesised and characterised with electrospray ionisation mass spectrometry and 1H and 13C NMR spectroscopy. The antitumour properties were evaluated by MTT assay, and the data revealed that 2 can inhibit the growth of human lung adenocarcinoma A549 efficiently. Furthermore, the DNA-binding behaviours of these complexes were investigated by a multiple spectroscopy assay and viscosity study. The results indicated that these complexes interact with calf thymus DNA through electrostatic interactions with a strong binding affinity in the order 2>3>1. Therefore, these results suggested that 2 might be a suitable anticancer agent due to its excellent DNA-binding abilities.

scholarly journals Structural basis for osmotic regulation of the DNA binding properties of H-NS proteins

2019 ◽  
Author(s):  
Liang Qin ◽  
Fredj Ben Bdira ◽  
Yann G. J. Sterckx ◽  
Alexander N. Volkov ◽  
Jocelyne Vreede ◽  
...  
Keyword(s):  
Dna Binding ◽  
Electrostatic Interactions ◽  
Intramolecular Interactions ◽  
Structural Basis ◽  
Binding Properties ◽  
Family Protein ◽  
Low Salt ◽  
Functional States ◽  
Mechanistic Basis ◽  
Dna Binding Properties

AbstractH-NS proteins act as osmotic sensors translating changes in osmolarity into altered DNA binding properties, thus, regulating enterobacterial genome organization and genes transcription. The molecular mechanism underlying the switching process and its conservation among H-NS family members remains elusive.Here, we focus on the H-NS family protein MvaT from P. aeruginosa and demonstrate experimentally that its protomer exists in two different conformations, corresponding to two different functional states. In the half-opened state (dominant at low salt) the protein forms filaments along DNA, in the fully opened state (dominant at high salt) the protein bridges DNA. This switching is a direct effect of ionic strengths on electrostatic interactions between the appositively charged DNA binding and N-terminal domains of MvaT. The asymmetric charge distribution and intramolecular interactions are conserved among the H-NS family of proteins. Therefore, our study establishes a general paradigm for the molecular mechanistic basis of the osmosensitivity of H-NS proteins.

scholarly journals Screening of Natural Deep Eutectic Solvents for Green Synthesis of 2-methyl-3-substituted Quinazolinones and Microwave-Assisted Synthesis of 3-aryl Quinazolinones in Ethanol

2020 ◽  
Vol 92 (4) ◽  
pp. 511-517
Author(s):  
Mario Komar ◽  
Maja Molnar ◽  
Anastazija Konjarević
Keyword(s):  
Green Synthesis ◽  
Anthranilic Acid ◽  
Deep Eutectic Solvents ◽  
13C Nmr Spectroscopy ◽  
Microwave Assisted Synthesis ◽  
One Pot ◽  
1H And 13C Nmr ◽  
Microwave Assisted ◽  
Natural Deep Eutectic Solvents ◽  
Quinazolinone Derivatives

In this study, two fast and efficient protocols for green synthesis of 3-substituted quinazolinones were perfomed. A synthesis of 2-methyl-3-substituted quinazolinones was performed in natural deep eutectic solvents, while 3-aryl quinazolinones were obtained by using microwave assisted synthesis. Benzoxazinone, which was used as an intermediate in the synthesis of 2-methyl-3-substituted quinazolinones, was prepared conventionally from anthranilic acid and acetic anhydride. In order to find the most appropriate synthetic path, twenty natural deep eutectic solvents were applied as a solvent in these syntheses. Choline chloride:urea (1 : 2) was found to be the most efficient solvent and was further used in the synthesis of 2-methyl quinazolinone derivatives (2–12). 3-Aryl quinazolinones (13–17), on the other hand, were synthesized in one-pot microwave-assisted reaction of anthranilic acid, different amines and trimethyl orthoformate. All compounds were synthesized in good to excellent yields, characterized by LC-MS/MS spectrometry and 1H- and 13C-NMR spectroscopy.

Determination of the DNA binding properties of a novel PARP inhibitor MK-4827 with calf-thymus DNA by molecular simulations and detailed spectroscopic investigations

2019 ◽  
Vol 43 (17) ◽  
pp. 6702-6711 ◽  
Author(s):  
Hongqin Yang ◽  
Qingle Zeng ◽  
Ze He ◽  
Di Wu ◽  
Hui Li
Keyword(s):  
Dna Binding ◽  
Deoxyribonucleic Acid ◽  
Parp Inhibitor ◽  
Molecular Simulations ◽  
Binding Interaction ◽  
Binding Properties ◽  
Calf Thymus ◽  
Polymerase Inhibitor ◽  
Dna Binding Properties

The binding interaction of niraparib (MK-4827), a poly(ADP-ribose) polymerase inhibitor, with calf thymus deoxyribonucleic acid (ctDNA) has been explored by various theoretical and experimental techniques.

scholarly journals Structural basis for osmotic regulation of the DNA binding properties of H-NS proteins

2020 ◽  
Vol 48 (4) ◽  
pp. 2156-2172 ◽  
Author(s):  
Liang Qin ◽  
Fredj Ben Bdira ◽  
Yann G J Sterckx ◽  
Alexander N Volkov ◽  
Jocelyne Vreede ◽  
...  
Keyword(s):  
Dna Binding ◽  
Electrostatic Interactions ◽  
Intramolecular Interactions ◽  
Structural Basis ◽  
Binding Properties ◽  
Family Protein ◽  
Low Salt ◽  
Mechanistic Basis ◽  
Oppositely Charged ◽  
Dna Binding Properties

Abstract H-NS proteins act as osmotic sensors translating changes in osmolarity into altered DNA binding properties, thus, regulating enterobacterial genome organization and genes transcription. The molecular mechanism underlying the switching process and its conservation among H-NS family members remains elusive. Here, we focus on the H-NS family protein MvaT from Pseudomonas aeruginosa and demonstrate experimentally that its protomer exists in two different conformations, corresponding to two different functional states. In the half-opened state (dominant at low salt) the protein forms filaments along DNA, in the fully opened state (dominant at high salt) the protein bridges DNA. This switching is a direct effect of ionic strength on electrostatic interactions between the oppositely charged DNA binding and N-terminal domains of MvaT. The asymmetric charge distribution and intramolecular interactions are conserved among the H-NS family of proteins. Therefore, our study establishes a general paradigm for the molecular mechanistic basis of the osmosensitivity of H-NS proteins.

Synthesis, crystal structure, DNA-binding and magnetism of copper 15-metallacrown-5 complexes based on glycinehydroxamic acid ligand

RSC Advances ◽  
2016 ◽  
Vol 6 (53) ◽  
pp. 47196-47202 ◽  
Author(s):  
Yanxia Meng ◽  
Hua Yang ◽  
Dacheng Li ◽  
Suyuan Zeng ◽  
Guifang Chen ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Circular Dichroism ◽  
Dna Binding ◽  
Fluorescence Spectroscopy ◽  
Calf Thymus Dna ◽  
Binding Properties ◽  
Acid Ligand ◽  
Calf Thymus ◽  
Dna Binding Properties ◽  
Circular Dichroïsm

Six lanthanide 15-MC-5 complexes based on glycinehydroxamic acid were synthesized. DNA-binding properties of the six complexes with calf thymus DNA were investigated using fluorescence spectroscopy and circular dichroism studies.

Synthesis, Characterization, DNA Binding, and Photocleavage of [Ru(bpy)2(MFIP)]2+ and [Ru(phen)2(MFIP)]2+

2008 ◽  
Vol 61 (9) ◽  
pp. 725 ◽  
Author(s):  
Lifeng Tan ◽  
Sheng Zhang ◽  
Xiaohua Liu ◽  
Yue Xiao
Keyword(s):  
Mass Spectrometry ◽  
Dna Binding ◽  
1H Nmr Spectroscopy ◽  
Binding Properties ◽  
Experimental Conditions ◽  
Spectrophotometric Methods ◽  
Calf Thymus ◽  
Pbr322 Dna ◽  
Ct Dna ◽  
Dna Binding Properties

The new ligand 2-(5-methyl-furan-2-yl)imidazo[4,5-f][1, 10]phenanthroline (MFIP) and its complexes [Ru(bpy)2(MFIP)]2+ 1 (bpy = 2,2′-bipyridine) and [Ru(phen)2(MFIP)]2+ 2 (phen = 1,10-phenanthroline) were synthesized and characterized by elemental analysis, mass spectrometry, and 1H NMR spectroscopy. The DNA binding properties of the two complexes were investigated by different spectrophotometric methods and viscosity measurements. The results suggest that both complexes bind to calf thymus DNA (CT-DNA) through intercalation, and both complexes can enantioselectively interact with CT-DNA. The Λ enantiomers of both complexes are slightly predominant for binding to CT-DNA over the Δ enantiomer. When irradiated at 400 nm, the two complexes promote the photocleavage of pBR322 DNA, and complex 2 cleaves DNA more effectively than complex 1 under comparable experimental conditions. Furthermore, mechanism studies reveal that singlet oxygen (1O2) plays a significant role in the photocleavage.

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