scholarly journals Novel Benzimidazole Derived Imine-Based Ligand and its Co(III), Ni(II), Cu(II) and Pt(II) Complexes: Chemical Synthesis, Structure, Antimicrobial, DNA Interaction Studies and Nuclease Activity

2020 ◽  
Vol 9 (4) ◽  
pp. 1655-1672
Keyword(s):  
Metal Complexes ◽  
Plasmid Dna ◽  
Hematological Parameters ◽  
Nuclease Activity ◽  
Dna Interaction ◽  
Molecular Structures ◽  
Spectral Studies ◽  
Supercoiled Plasmid ◽  
Pbr322 Dna

Herein, we report the synthesis of a Schiff base ligand, 2-((E)-((1H-benzo[d]imidazol-2-yl)methylimino)methyl)-4,6-dichlorophenol (BMDC) and its Co(III), Ni(II), Cu(II) and Pt(II) coordinated compounds (henceforth named as M1, M2, M3, and M4, respectively). The synthesized compounds were subjected to various analytical and physical characterization techniques to confirm their molecular structures. Further, the DNA binding and cleavage propensity of the as-prepared metal complexes were evaluated using calf thymus DNA (CT-DNA) and supercoiled plasmid DNA (pBR322). The DNA interaction results revealed that the tested metal complexes bind with DNA through the covalent and non-covalent mode of interaction, which is investigated using absorption and fluorescence spectral studies followed by viscosity measurement. The scission of supercoiled plasmid DNA by the metal complexes suggested the potentiality of the molecules toward the cleavage of pBR322 DNA. Furthermore, the compounds were screened for in vitro antiproliferative activity, tested against the various cell lines such as A549, EAC, SIHA, and NIH3T3. Results revealed that compound M4 exhibited marked anti-proliferative activity against EAC cell line with a significant IC50 value of 10 µm compared to its parent ligand, BMDC, and other metal transition complexes under study. In addition, various hematological parameters (alkaline phosphate, creatinine, urea, RBC, and WBC) were studied, and significant results are obtained from the experiments.

scholarly journals Effect of Chromatographic Conditions on Supercoiled Plasmid DNA Stability and Bioactivity

2019 ◽  
Vol 9 (23) ◽  
pp. 5170 ◽  
Author(s):  
G.M. Azevedo ◽  
J.F.A. Valente ◽  
A. Sousa ◽  
A.Q. Pedro ◽  
P. Pereira ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Plasmid Dna ◽  
P53 Protein ◽  
Metabolic Stress ◽  
Suppressor Gene ◽  
Experimental Conditions ◽  
P53 Expression ◽  
Supercoiled Plasmid ◽  
Protein P53

The dysfunction of the tumor suppressor gene TP53 has been associated with the pathogenesis of the majority of the cases of cancer reported to date, leading the cell to acquire different features known as the cancer hallmarks. In normal situations, the protein p53 protects the cells against tumorigenesis. By detecting metabolic stress or DNA damage in response to stress, p53 can lead the cell to senescence, autophagy, cell cycle arrest, DNA repair, and apoptosis. Thus, in the case of p53 mutations, it is reasonable to assume that the reestablishment of its function, may restrain the proliferation of cancer cells. The concept of cancer gene therapy can be based on this assumption, and suitable biotechnological approaches must be explored to assure the preparation of gene-based biopharmaceuticals. Although numerous procedures have already been established to purify supercoiled plasmid DNA (sc pDNA), the therapeutic application is highly dependent on the biopharmaceutical’s activity, which can be affected by the chromatographic conditions used. Thus, the present work aims at comparing quality and in vitro activity of the supercoiled (sc) isoform of the p53 encoding plasmid purified by three different amino acids-based chromatographic strategies, involving histidine–agarose, arginine–macroporous, and histidine–monolith supports. The B-DNA topology was maintained in all purified pDNA samples, but their bioactivity, related to the induction of protein p53 expression and apoptosis in cancer cells, was higher with arginine–macroporous support, followed by histidine–monolith and histidine–agarose. Despite the purity degree of 92% and recovery yield of 43% obtained with arginine–macroporous, the sc pDNA sample led to a higher expression level of the therapeutic p53 protein (58%) and, consequently, induced a slightly higher apoptotic effect (27%) compared with sc pDNA samples obtained with histidine–monolithic support (26%) and histidine–agarose support (24%). This behavior can be related to the mild chromatographic conditions used with arginine–macroporous support, which includes the use of low salt concentrations, at neutral pH and lower temperatures, when compared to the high ionic strength of ammonium sulfate and acidic pH used with histidine-based supports. These results can contribute to field of biopharmaceutical preparation, emphasizing the need to control several experimental conditions while adapting and selecting the methodologies that enable the use of milder conditions as this can have a significant impact on pDNA stability and biological activity.

scholarly journals Cu(II) and Ni(II) Complexes with New Tridentate NNS Thiosemicarbazones: Synthesis, Characterisation, DNA Interaction, and Antibacterial Activity

2019 ◽  
Vol 2019 ◽  
pp. 1-14 ◽  
Author(s):  
Dorian Polo-Cerón
Keyword(s):  
Metal Complexes ◽  
Dna Cleavage ◽  
Thermal Analyses ◽  
Dna Interaction ◽  
Antimicrobial Activities ◽  
Tridentate Ligand ◽  
Bacterial Strains ◽  
Azomethine Group ◽  
Broth Microdilution Method

This paper reports the synthesis and detailed characterisation of copper(II) and nickel(II) complexes with tridentate thiosemicarbazone ligands H2L1 and H2L2 derived from 2-acetylpyrazine. The ligands and their metal complexes were characterised by different physicochemical techniques, including elemental and thermogravimetric analysis; UV-Vis, IR, 1H-NMR, and 13C-NMR spectroscopy; molar conductance measurements; and mass spectrometry. The crystal structure of the H2L1 ligand was determined by single crystal X-ray diffraction studies. The spectral data showed that the thiosemicarbazone behaves as an NNS tridentate ligand through the nitrogen atoms of the azomethine group and pyrazine ring and the sulphur atom of the thioamide group. Elemental and thermal analyses indicated that the obtained metal complexes had a 1 : 1 stoichiometry (metal-ligand). The interactions between these complexes and calf thymus DNA (CT-DNA) were studied by electronic absorption and viscosity measurements. The activities of these compounds against oxidative DNA cleavage were examined by agarose gel electrophoresis. Cu(II) and Ni(II) complexes can wind DNA strands through groove interactions and promote strand breakage of the plasmid pmCherry under oxidative stress conditions. Moreover, all the complexes could interact more strongly with DNA than could with the free ligands. Finally, the antibacterial activities of the ligands and their complexes were determined by in vitro tests against Gram-positive bacterial strains (S. aureus ATCC 25923, L. monocytogenes ATCC 19115, and B. cereus ATCC 10876) and Gram-negative bacterial strains (E. coli ATCC 25922, S. typhimurium ATCC 14028, and K. pneumoniae ATCC BAA-2146) using the broth microdilution method. The metal complexes showed greater antimicrobial activities than the precursor ligands against some of the microorganisms.

scholarly journals Synthesis, Characterization and Biological Evaluation of Fe(III) and Cu(II) Complexes with 2,4-Dinitrophenyl hydrazine and Thiocyanate Ions

2019 ◽  
Vol 31 (4) ◽  
pp. 780-784
Author(s):  
P. Manimaran ◽  
S. Balasubramaniyan
Keyword(s):  
Antioxidant Activity ◽  
Metal Complexes ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Free Ligand ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Diffusion Method ◽  
Spectral Studies

The metal complexes of Fe(III) and Cu(II) were prepared by using 2,4-dinitrophenyl hydrazine (DNPH) and thiocyanate (SCN) with stirrer refluxed for about 6 h. The prepared Fe(III) and Cu(II) complexes were characterized by elemental analysis, molar conductance, magnetic susceptibility and electronic spectrum, FT-IR spectral studies. The result suggested the octahedral geometry for Fe(III) and Cu(II) complexes. Powder X-ray diffraction indicate the crystalline nature of the metal complexes. The antimicrobial activities of the Fe(III) and Cu(II) complexes were tested with various micro organisms by disc diffusion method. The antimicrobial results indicate that the metal complexes are highly active with compared to the free ligand. The in vitro antioxidant activity of the free ligand and its metal complexes was assayed by radical scavenging activity (DPPH). The result proposed that Fe (III) and Cu(II) complexes exhibited strong antioxidant activity than that of the ligand.

scholarly journals Synthesis and Spectral Studies of 4,4′-(Hydrazine-1,2-diylidenedimethylylidene)-bis-(2- methoxyphenol) and Its Transition Metal Complexes with Promising Biological Activities

2020 ◽  
Vol 32 (7) ◽  
pp. 1768-1772
Author(s):  
Anita Rani ◽  
Manoj Kumar ◽  
Hardeep Singh Tuli ◽  
Zahoor Abbas ◽  
Vinit Prakash
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Schiff Base Ligand ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Analytical Techniques ◽  
Spectral Studies

The study describes the synthesis, characterization and biological activity of a novel Schiff base ligand and its transition metal complexes. The Schiff base ligand was obtained by a condensation reaction between 4-hydroxy-3-methoxybenzaldehyde (p-vanillin) and hydrazine hydrate using ethanol as solvent. A new series of Ni(II) and Fe(III) complexes were also derived by reaction of prepared Schiff base ligand with NiCl2 and FeCl3. Both the ligand and its metal complexes were characterized by solubility, melting point and elemental analysis. These compounds were further identified by analytical techniques, FTIR, NMR and mass spectrometry. The ligand and its transition metal complexes were also subjected to in vitro biological activities i.e. antimicrobial, antiangiogenic and DNA photo cleavage. For antimicrobial activity compounds were tested against two strains of bacteria and two strains of fungi. Different concentrations of prepared compounds were treated with fertilized chicken eggs and plasmid DNA to find out antiangiogenic and DNA photocleavage activity, respectively.

scholarly journals Synthesis, Spectroscopic, and Antimicrobial Studies on Bivalent Nickel and Copper Complexes of Bis(thiosemicrbazone)

2007 ◽  
Vol 2007 ◽  
pp. 1-7 ◽  
Author(s):  
Sulekh Chandra ◽  
Smriti Raizada ◽  
Monika Tyagi ◽  
Archana Gautam
Keyword(s):  
Metal Complexes ◽  
Metal Ion ◽  
Copper Complexes ◽  
Free Ligand ◽  
Antimicrobial Properties ◽  
Molar Conductance ◽  
Spectral Studies ◽  
Central Metal ◽  
Antimicrobial Studies

A series of metal complexes of Cu(II) and Ni(II) having the general composition[M(L)X2]with benzil bis(thiosemicarbazone) has been prepared and characterized by element chemical analysis, molar conductance, magnetic susceptibility measurements, and spectral (electronic, IR, EPR, mass) studies. The IR spectral data suggest the involvement of sulphur and azomethane nitrogen in coordination to the central metal ion. On the basis of spectral studies, an octahedral geometry has been assigned for Ni(II) complexes but a tetragonal geometry for Cu(II) complexes. The free ligand and its metal complexes have been tested in vitro against a number of microorganisms in order to assess their antimicrobial properties.

scholarly journals Synthesis, Characterization, Antimicrobial, DNA Cleavage, andIn VitroCytotoxic Studies of Some Metal Complexes of Schiff Base Ligand Derived from Thiazole and Quinoline Moiety

2014 ◽  
Vol 2014 ◽  
pp. 1-17 ◽  
Author(s):  
Nagesh Gunvanthrao Yernale ◽  
Mruthyunjayaswamy Bennikallu Hire Mathada
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Schiff Base Ligand ◽  
Dna Cleavage ◽  
Biological Activities ◽  
Artemia Salina ◽  
Spectral Studies ◽  
Antibacterial And Antifungal Activities ◽  
Pyramidal Geometry

A novel Schiff base ligandN-(4-phenylthiazol-2yl)-2-((2-thiaxo-1,2-dihydroquinolin-3-yl)methylene)hydrazinecarboxamide(L)obtained by the condensation ofN-(4-phenylthiazol-2-yl)hydrazinecarboxamide with 2-thioxo-1,2-dihydroquinoline-3-carbaldehyde and its newly synthesized Cu(II), Co(II), Ni(II), and Zn(II) complexes have been characterized by elemental analysis and various spectral studies like FT-IR,1H NMR, ESI mass, UV-Visible, ESR, TGA/DTA, and powder X-ray diffraction studies. The Schiff base ligand(L)behaves as tridentate ONS donor and forms the complexes of type [ML(Cl)2] with square pyramidal geometry. The Schiff base ligand(L)and its metal complexes have been screenedin vitrofor their antibacterial and antifungal activities by minimum inhibitory concentration (MIC) method. The DNA cleavage activity of ligand and its metal complexes were studied using plasmid DNA pBR322 as a target molecule by gel electrophoresis method. The brine shrimp bioassay was also carried out to study thein vitrocytotoxicity properties for the ligand and its metal complexes againstArtemia salina. The results showed that the biological activities of the ligand were found to be increased on complexation.

scholarly journals SYNTHESIS, BIOLOGICAL STUDY, DNA INTERACTION OF MANNICH BASE METAL COMPLEXES DERIVED FROM BENZAMIDE

2021 ◽  
pp. 60-64
Author(s):  
SIVAKAMI SUDHASANKAR
Keyword(s):  
Metal Complexes ◽  
Mannich Base ◽  
Dna Interaction ◽  
Mannich Bases ◽  
Molar Conductance ◽  
Biological Study ◽  
Spectral Studies ◽  
Mass Spectral ◽  
Calf Thymus ◽  
Uv Visible

Objective: Coordination compounds occur widely in nature and they comprise a large share of current inorganic research. The Mannich reaction is a classic method for the preparation of Mannich bases, namely, β amino compounds, which are heterocyclic. Methods: A novel Mannich base of N-((3,4-dimethoxyphenyl)(2,5-dioxopyrrolidin-1-yl) methyl)benzamide and its coordination complexes with transition metals Mn and Co have been synthesized and characterized by elemental analysis, molar conductance, magnetic susceptibility measurements, UV-Visible, IR, NMR, and Mass spectral studies. Results: Based on the magnetic moment and UV-Visible spectral data, octahedral geometries were assigned for the metal complexes. The metal complexes were screened for antifungal activity. Conclusion: the metal complexes have shown good activity than the ligand. The binding of selected metal complexes with calf thymus DNA was investigated. It is found that the cobalt (II) metal complex of the ligand showed efficient DNA binding ability.

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