In vitro biological properties and predicted DNA–BSA interaction of three new dicyanidoargentate(i)-based complexes: synthesis and characterization

2018 ◽  
Vol 42 (6) ◽  
pp. 4679-4692 ◽  
Author(s):  
Ahmet Karadağ ◽  
Nesrin Korkmaz ◽  
Ali Aydın ◽  
Şaban Tekin ◽  
Yusuf Yanar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Properties ◽  
Synthesis And Characterization ◽  
Drug Candidates ◽  
Bsa Interaction

The synthesis, characterization and biological activity of three novel dicyanidoargentate(i)-based complexes are reported. The in vitro results show that these complexes may be potent antiproliferative drug candidates.

Synthesis and characterization of two novel dicyanidoargentate(i) complexes containing N-(2-hydroxyethyl)ethylenediamine exhibiting significant biological activity

2014 ◽  
Vol 38 (10) ◽  
pp. 4760-4773 ◽  
Author(s):  
Nesrin Korkmaz ◽  
Ahmet Karadağ ◽  
Ali Aydın ◽  
Yusuf Yanar ◽  
İsa Karaman ◽  
...  
Keyword(s):  
Biological Activity ◽  
Synthesis And Characterization ◽  
Anticancer Activities

Two novel cyanido-complexes having very significant antibacterial, antifungal and anticancer activities in vitro were synthesized and characterized using various techniques.

scholarly journals Coordination Compounds of Platinum and Palladium with Mixed Ligands (Usnic Acid and 1-(o-Tolyl) Biguanide) � Synthesis, Spectral Characterization and Biological Activity

2020 ◽  
Vol 71 (4) ◽  
pp. 336-346
Author(s):  
Mirela Calinescu ◽  
Ovidiu Oprea ◽  
Catalina Stoica ◽  
Mihai Nita-Lazar ◽  
Madalina Mihalache
Keyword(s):  
Staphylococcus Aureus ◽  
Pseudomonas Aeruginosa ◽  
Biological Activity ◽  
Coordination Compounds ◽  
Antitumor Agents ◽  
Biological Activities ◽  
Usnic Acid ◽  
Biological Properties ◽  
Mixed Ligands

Four coordination compounds of Pd(II), Pt(II) and Pt(IV) with usnic acid (H3AU) and 1-(o-tolyl)biguanide (TB) as ligands have been synthesized in view of their potential as antimicrobial, antifungal and antitumor agents. The metal complexes have been characterized by elemental and thermogravimetrical analyses, infrared and electronic spectra. Based on these studies, the following formulas have been proposed for the complexes: [Pd(TB)(H3AU)]PdCl4 (C1), [Pd(TB)(H2AU)] CH3COO (C2), [Pt(TB)(H2AU)Cl2]Cl (C3) and [Pt(TB)(H2AU)]Cl (C4), where H2AU is deprotonated usnic acid. The in vitro biological activities of the new complexes were tested against Staphylococcus aureus ATCC 25923, Pseudomonas aeruginosa ATCC 27853, Candida albicans ATCC 10231 and HeLa tumor cells. All complexes were found to have good biological properties and therefore they can be further explored in therapeutic applications.

In vitro biological activity of copper(II) complexes with NSAIDs and nicotinamide: Characterization, DNA- and BSA-interaction study and anticancer activity

2021 ◽  
pp. 111696
Author(s):  
Flóra Jozefíková ◽  
Spyros Perontsis ◽  
Katarína Koňáriková ◽  
Ľubomír Švorc ◽  
Milan Mazúr ◽  
...  
Keyword(s):  
Biological Activity ◽  
Anticancer Activity ◽  
Interaction Study ◽  
Bsa Interaction

The prediction of the spectrum of biological activity and antimicrobial properties of diaminoazoles

2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antimicrobial Properties ◽  
Biological Properties ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Wide Range ◽  
Alternative Drugs

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.

scholarly journals Synthesis and characterization some complexes of azo dye of pyrimidyniyl and evaluating their biological activity

2019 ◽  
Vol 24 (3) ◽  
Author(s):  
Yareeb Jwad Sahar ◽  
Hasan Shamran Mohammed
Keyword(s):  
Biological Activity ◽  
Cell Line ◽  
Azo Dye ◽  
Mass Spectra ◽  
Molar Conductivity ◽  
Synthesis And Characterization ◽  
E Coli ◽  
Mcf 7

The present study involves fabrication a heterocyclic azo dye:  2-[4-diamino-3-benzaldehyde diazenyl]pyrimidine (L). The dye was synthesized by reacting 2-aminopyrimidine with 4-diaminobenzaldehyde (in situ). The complexes of ([Ag(L)(H2O)]NO3, [Cd(L)2]Cl2 and [Hg(L)2]Cl2) dyes were prepared and characterized by elemental analysis; mass spectra, molar conductivity and spectroscopies of infrared and UV-Vis. The L dye ligand is tridentate. The Cd(II) and Hg(II) are octahedral with mole ratio Metal:Ligand equal to 1:2 while Ag(I) complex is tetrahedral with mole ratio Metal:Ligand equal to 1:1. The molar conductivity indicates that Ag(I) complex is electrolyte (1:1) and Cd(II) and (II) are electrolytes with ratio 2:1. The synthesized ligand (L) and its complexes showed interest biological activity against E-coli and Staph-aureus bacteria and Aspergillus Niger and Pinicillium.sp fungi. The anti-activity of [Ag(L)(H2O)]NO3 complex against MCF-7 cell line and its cytotoxicity against WRL cell line were interesting in vitro.

scholarly journals A Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as Potential Chemotherapeutic Agent: From Synthesis to In Vivo Studies

2019 ◽  
Author(s):  
Anna Notaro ◽  
Angelo Frei ◽  
Riccardo Rubbiani ◽  
Marta Jakubaszek ◽  
Uttara Basu ◽  
...  
Keyword(s):  
Chemotherapeutic Agent ◽  
Biological Properties ◽  
In Vivo Studies ◽  
Drug Candidate ◽  
Paramagnetic Resonance ◽  
In Vivo Models ◽  
Drug Candidates ◽  
X Ray Crystallography

Chemotherapy remains one of the dominant treatments to cure cancer. However, due to the many inherent drawbacks, there is a surge for new chemotherapeutic drugs. More specifically, the discovery of new drug candidates able to overcome severe side effects, the occurrence of resistance and the inefficacy toward metastatic tumours is highly desirable. In this work, we designed a new chemotherapeutic drug candidate against cancer, namely [Ru(DIP)2(sq)]PF6 (Ru-sq) (DIP = 4,7-diphenyl-1,10-phenanthroline; sq = semiquinonate ligand). The aim was to combine the great potential expressed by Ru(II) polypyridyl complexes and the singular redox and biological properties associated to the catecholate moiety. Several pieces of experimental evidence (e.g., X-ray crystallography, electron paramagnetic resonance, electrochemistry) demonstrate that the semiquinonate is the preferred oxidation state of the dioxo ligand in this complex. The biological activity of Ru-sq was then scrutinised in vitro and in vivo, and the results highlight the tremendous potential of this complex as a chemotherapeutic agent against cancer. Ru-sq was notably found have a much higher cytotoxic activity than cisplatin on several cell lines (i.e. in the nanomolar range), and, contrary to cisplatin, to have mitochondrial disfunction as one of its modes of action. The multicellular targets of Ru-sq could potentially be the key to overcome one of the main drawbacks of cisplatin i.e. the occurrence of resistance. Moreover, Ru-sq exhibited impressing activity on Multi Cellular Tumour Spheroids (MCTS) model, leading to a growth inhibition of the tumour even 13 days after treatment (20 μM). Very importantly, using two different in vivo models, it could be demonstrated that this compound is extremely well-tolerated by mice and has a very promising activity, curing, in some cases, tumour-bearing mice.<br>

scholarly journals A Ruthenium(II) Complex Containing a Redox-Active Semiquinonate Ligand as Potential Chemotherapeutic Agent: From Synthesis to In Vivo Studies

2019 ◽  
Author(s):  
Anna Notaro ◽  
Angelo Frei ◽  
Riccardo Rubbiani ◽  
Marta Jakubaszek ◽  
Uttara Basu ◽  
...  
Keyword(s):  
Chemotherapeutic Agent ◽  
Biological Properties ◽  
In Vivo Studies ◽  
Drug Candidate ◽  
Paramagnetic Resonance ◽  
In Vivo Models ◽  
Drug Candidates ◽  
X Ray Crystallography

Chemotherapy remains one of the dominant treatments to cure cancer. However, due to the many inherent drawbacks, there is a surge for new chemotherapeutic drugs. More specifically, the discovery of new drug candidates able to overcome severe side effects, the occurrence of resistance and the inefficacy toward metastatic tumours is highly desirable. In this work, we designed a new chemotherapeutic drug candidate against cancer, namely [Ru(DIP)2(sq)]PF6 (Ru-sq) (DIP = 4,7-diphenyl-1,10-phenanthroline; sq = semiquinonate ligand). The aim was to combine the great potential expressed by Ru(II) polypyridyl complexes and the singular redox and biological properties associated to the catecholate moiety. Several pieces of experimental evidence (e.g., X-ray crystallography, electron paramagnetic resonance, electrochemistry) demonstrate that the semiquinonate is the preferred oxidation state of the dioxo ligand in this complex. The biological activity of Ru-sq was then scrutinised in vitro and in vivo, and the results highlight the tremendous potential of this complex as a chemotherapeutic agent against cancer. Ru-sq was notably found have a much higher cytotoxic activity than cisplatin on several cell lines (i.e. in the nanomolar range), and, contrary to cisplatin, to have mitochondrial disfunction as one of its modes of action. The multicellular targets of Ru-sq could potentially be the key to overcome one of the main drawbacks of cisplatin i.e. the occurrence of resistance. Moreover, Ru-sq exhibited impressing activity on Multi Cellular Tumour Spheroids (MCTS) model, leading to a growth inhibition of the tumour even 13 days after treatment (20 μM). Very importantly, using two different in vivo models, it could be demonstrated that this compound is extremely well-tolerated by mice and has a very promising activity, curing, in some cases, tumour-bearing mice.<br>

scholarly journals Tantalum Nanoparticles Reinforced PCL Scaffolds Using Direct 3D Printing for Bone Tissue Engineering

2021 ◽  
Vol 8 ◽  
Author(s):  
Zixuan Xiong ◽  
Wenbin Liu ◽  
Hu Qian ◽  
Ting Lei ◽  
Xi He ◽  
...  
Keyword(s):  
Gene Expression ◽  
Tissue Engineering ◽  
Biological Activity ◽  
Cell Adhesion ◽  
3D Printing ◽  
Orthopedic Implants ◽  
Biological Properties ◽  
Related Gene ◽  
Clinical Potential

Polycarbonate (PCL) has been widely used in tissue engineering, but its hydrophobicity and low biological activity limit its further promotion and application. By adding nanoparticles, the hydrophilicity and biological activity of PCL can be improved. In this study, different amounts of Ta (1–10%wt) were added to PCL, and then their mechanical and biological properties were studied in vitro. XRD found that 5%Ta-PCL has the highest crystallinity. At the same time, cell experiments CCK8, cell adhesion, osteogenic differentiation, and osteogenesis related gene expression showed that Ta can enhance the mechanical and biological properties of PCL, while 5% Ta-PCL showed the best mechanical and biological properties. This composite of tantalum and PCL could have a clinical potential for orthopedic implants.

COMPARATIVE STUDIES OF THE POTENTIATION OF CORTICOTROPHIN ACTIVITY BY SEVERAL INACTIVE DERIVATIVES

1963 ◽  
Vol 42 (2) ◽  
pp. 209-213 ◽  
Author(s):  
Arthur I. Cohen ◽  
Edward H. Frieden
Keyword(s):  
Biological Activity ◽  
Comparative Studies ◽  
Free Amino ◽  
Hormonal Activity ◽  
Amino Groups

ABSTRACT A number of corticotrophin analogues have been prepared, some of which potentiate the biological activity of the untreated hormone in vitro. The free amino groups of corticotrophin appear to be essential not only for hormonal activity, but also for the interaction of the analogues with the tissue corticotrophin inactivating system which is assumed to account for the potentiating effect.

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