Synthesis, Characterization and Bioactivity of Three Carboxylic Arylhydrazone Compounds

2020 ◽  
Vol 42 (1) ◽  
pp. 149-149
Author(s):  
Fengying Chen Fengying Chen ◽  
Wangting Wu Wangting Wu ◽  
Zhenguo Jin Zhenguo Jin ◽  
Shuiyang He Shuiyang He ◽  
Chengfang Qiao and Fei Yuan Chengfang Qiao and Fei Yuan

Three novel carboxylic arylhydrazone compounds named 2- oxo propionic acid terephthalal acyl dihydrazone (1), 2-ketoglutaric acid terephthalal acyl dihydrazone (2) and 2-ketoglutaric acid salicyl- hydrazone (3) were prepared and characterized by elemental analysis, IR and 1H NMR. The antibacterial activities of 1 and 2 against wheat rust and coliform were investigated. The results showed that 1 had more excellent antibacterial properties than 2 against both wheat rust and coliform. In addition, the title compounds interaction with calf-thymus DNA (CT-DNA) were measured by fluorescence spectra method which indicating that they combined with CT-DNA by groove binding through hydrogen bonds.

2016 ◽  
Vol 2016 ◽  
pp. 1-11
Author(s):  
Raj Kaushal ◽  
Sheetal Thakur ◽  
Kiran Nehra

Five structurally related titanium (IV) heteroleptic complexes, [TiCl2(bzac)(L1–4)] and [TiCl3(bzac)(HL5)]; bzac = benzoylacetonate; L1–5 = benzohydroximate (L1), salicylhydroximate (L2), acetohydroximate (L3), hydroxyurea (L4), and N-benzoyl-N-phenyl hydroxylamine (L5), were used for the assessment of their antibacterial activities against ten pathogenic bacterial strains. The titanium (IV) complexes (1–5) demonstrated significant level of antibacterial properties as measured using agar well diffusion method. UV-Vis absorption spectroscopic technique was applied, to get a better insight into the nature of binding between titanium (IV) complexes with calf thymus DNA (ct-DNA). On the basis of the results of UV-Vis absorption spectroscopy, the interaction between ct-DNA and the titanium (IV) complexes is likely to occur through the same mode. Results indicated that titanium (IV) complex can bind to calf thymus DNA (ct-DNA) via an intercalative mode. The intrinsic binding constant (Kb) was calculated by absorption spectra by using Benesi-Hildebrand equation. Further, Gibbs free energy was also calculated for all the complexes.


2011 ◽  
Vol 26 (4-5) ◽  
pp. 289-296
Author(s):  
Fei Ma ◽  
Jing Tang ◽  
Chao Yang ◽  
Yu-Ying Feng ◽  
Shao-Hua Wei ◽  
...  

The interaction of Elsinochrome A (EA) with calf thymus DNA (CT-DNA) has been investigated by UV-vis spectra and fluorescence spectra. The results show that EA can bind with CT-DNA and binding sites are destroyed after irradiation by visible light, which indicates that EA is a promising candidate for photodynamic therapy. In addition, the binding mechanism is studied using fluorescence quenching test and ethidium bromide (EB) replace assay experiments. The results suggest that EA and CT-DNA are binding with a strong force and the major binding mode of EA with DNA could be the electrostatic binding.


2009 ◽  
Vol 7 (1) ◽  
pp. 105-110 ◽  
Author(s):  
Jian-Ping Cheng ◽  
Qiu-Yue Lin ◽  
Hu Rui-Ding ◽  
Wen-Zhong Zhu ◽  
Hua-Qiong Li ◽  
...  

AbstractTwo novel complexes, [La(HL)(H2O)2NO3] · NO3 · H2O and [Gd(HL)(H2O)2NO3] · NO3 · H2O, where HL is a Schiff base derived from o-vanillin and lysine, have been synthesized and characterized by elemental analysis, conductivity measurements, IR, 1H NMR and thermogravimetric analyses (TGA). The Schiff base ligand behaves as a tetradentate, coordinating through azomethine nitrogen, phenolic oxygen and two carboxylic oxygen atoms. The interaction of these complexes with calf thymus DNA (CT-DNA) was also investigated by spectrometric titration and viscometric measurements. The faint hypochromism of the complexes in the absorption spectra, the remarkable reduction of fluorescence intensity of ethidium bromide (EB) bound DNA, together with a small decrease in the viscosity of the DNA suggest that a partial intercalation may be the preferred binding mode between these two complexes and DNA. The antibacterial activity testing revealed that the complexes and their precursor Schiff base show a weak to moderate activity against Bacillus subtilis, Staphylococcus aureus and Escherichia coli.


Author(s):  
Nagaraj Karuppiah ◽  
◽  
Muthukumaran Pakkirisamy ◽  
Gunasekaran Gladwin ◽  

The interaction of cis-[Co(phen)2(TA)2](ClO4)3, a cationic surfactant complex (phen = 1-10 phenanthroline, TA= Tetradecylamine), with calf thymus DNA has been studied by physici-chemical techniques. The spectroscopic studies together with cyclic voltammetry and viscosity experiments support that the surfactant-cobalt(III) complex binds to calf thymus DNA (CT DNA) by intercalation through the aliphatic chain present in the complex into the base pairs of DNA. The presence of phenanthroline ligand with larger -frame work may also enhance intercalation. Besides the effect of binding of surfactant cobalt(III) complex to DNA in presence of -cyclodextrin has also studied. In presence of -cyclodextrin the binding occur through surface and (or) groove binding. The complex was investigated as one of the potential


2011 ◽  
Vol 26 (6) ◽  
pp. 357-365 ◽  
Author(s):  
Hamid Dezhampanah ◽  
Termeh Darvishzad ◽  
Mehrnaz Aghazadeh

The interaction between anionic form of copper (II) N,N',N",N'"-tetrasulfonated phthalocyanine Cu (tspc) and to calf thymus deoxyribonucleic acid (ct-DNA) is investigated by measuring UV-vis absorption and fluorescence spectroscopy in phosphate buffer. The binding constant and stoichiometry were determined by analysis of optical absorption spectra of phthalocyanine at various ct-DNA concentrations using SQUAD software. The static mode of fluorescence quenching of phthalocyanine by calf thymus deoxyribonucleic acid indicates the formation of a ground-state complex. The formation of ground-state complex is a spontaneous molecular interaction procedure in which outside groove binding through the formation of an axial bond between the base pairs of nucleotide and Cu in the central core of phthalocyanine.


2015 ◽  
Vol 11 (2) ◽  
pp. 522-531 ◽  
Author(s):  
Tarique Sarwar ◽  
Mohammed Amir Husain ◽  
Sayeed Ur Rehman ◽  
Hassan Mubarak Ishqi ◽  
Mohammad Tabish

Minor groove binding of esculetin with Ct-DNA was established by a series of in vitro experiments and in silico analyses.


2019 ◽  
Vol 2019 ◽  
pp. 1-7
Author(s):  
Shiva Mehran ◽  
Yousef Rasmi ◽  
Hamid Reza Karamdel ◽  
Ramin Hossinzadeh ◽  
Zafar Gholinejad

Introduction. Wortmannin (WTN) is a steroid metabolite that inhibits phosphatidylinositol 3-kinase and other signaling pathways. Structurally, the WTN consists of a cyclopentanophenanthrene-like structure with several oxygen-rich moieties which have the potential to interact with deoxyribonucleic acid (DNA) molecules. Methods. We aim to evaluate the WTN and calf thymus DNA (ct-DNA) interaction with molecular docking using the AutoDock 4.2 software. UV and fluorescence spectroscopy and viscosity techniques were performed to confirm the in silico analysis. Results. Molecular docking showed that the WTN interacted with ct-DNA via hydrogen bonds at guanine-rich sequences. The number of hydrogen bonds between the WTN and DNA was 1-2 bonds (average 1.2) per WTN molecule. The in silico binding constant was 2 × 103 M−1. UV spectroscopy showed that the WTN induced a hyperchromic feature without wavelength shifting. The WTN and DNA interaction led to quenching of DNA-emitted fluorescence. The different concentrations of WTN had no effect on DNA viscosity. Taken together, our results demonstrated WTN interacts with DNA in the nonintercalating mode, which is considered as a new mechanism of action. Conclusion. These results suggest that the WTN may exert its biological effects, at least in part, via interaction with DNA.


2011 ◽  
Vol 2011 ◽  
pp. 1-11 ◽  
Author(s):  
Hassan Mansouri-Torshizi ◽  
Maryam Saeidifar ◽  
Fatemeh Khosravi ◽  
Adeleh Divsalar ◽  
Ali Akbar Saboury ◽  
...  

The two water-soluble designed platinum(II) complex, [Pt(Oct-dtc)(bpy)]NO3(Oct-dtc = Octyldithiocarbamate and bpy = 2,2′ -bipyridine) and palladium(II) complex, [Pd(Oct-dtc)(bpy)]NO3, have been synthesized and characterized by elemental analyses, molar conductivity measurements, IR,1HNMR, and electronic spectra studies. Studies of antitumor activity of these complexes against human cell tumor lines (K562) have been carried out. They show Ic50values lower than that of cisplatin. The complexes have been investigated for their interaction with calf thymus DNA (CT-DNA) by utilizing the electronic absorption spectroscopy, fluorescence spectra, and ethidium bromide displacement and gel filtration techniques. Both of these water-soluble complexes bound cooperatively and intercalatively to the CT-DNA at very low concentrations. Several binding and thermodynamic parameters are also described.


2016 ◽  
Vol 20 (05) ◽  
pp. 624-638 ◽  
Author(s):  
Su-Hong Peng ◽  
Biao-Biao Lv ◽  
Atif Ali ◽  
Jia-Min Wang ◽  
Xiao Ying ◽  
...  

The first oxidative cleavage of DNA by manganese [Formula: see text]-confused porphyrin [chloro(2-aza-2-methyl-5,10,15,20-tetrakis([Formula: see text]-chlorophenyl)-21-carbaporphyrin)manganese(III), 1] using H2O2 as oxidant agent and its magnetic, calf thymus DNA(ct-DNA)- and human serum albumin (HSA) binding properties were investigated. The magnitude of the axial (D) zero-field splitting for the mononuclear Mn(III) center in 1 was determined to be approximately 2.71 cm[Formula: see text] by paramagnetic susceptibility measurements. The DNA- and HSA binding experimental results showed that 1 bound to ct-DNA via an outside groove binding mode and the hydrophobic cavity located in subdomain IIA of HSA with the binding constant of 4.144 × 105 M[Formula: see text] and [Formula: see text] 106 M[Formula: see text], respectively. Thermodynamic parameters revealed that both DNA- and HSA binding were spontaneous process. The main driven forces were the hydrogen bond and van der Waals for the former, but hydrophobic interaction for the latter, which were further confirmed by molecular docking modeling. Manganese [Formula: see text]-confused porphyrin 1 could cleave the supercoiled plasmid DNA efficiently in the presence of hydrogen peroxide. Hydroxyl radical ([Formula: see text]OH) was found the active species for oxidative damage of DNA.


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