Zinc and copper complexes with azacrown ethers and their comparative stability in vitro and in vivo

2020 ◽  
Vol 49 (19) ◽  
pp. 6249-6258
Author(s):  
Gleb Yu. Aleshin ◽  
Bayirta V. Egorova ◽  
Anna B. Priselkova ◽  
Lyubov S. Zamurueva ◽  
Sofia Yu. Khabirova ◽  
...  
Keyword(s):  
Copper Complexes ◽  
Zinc Complexes ◽  
Azacrown Ethers ◽  
Copper Compounds ◽  
Comparative Stability

Radiolabeled macrocyclic zinc complexes are more stable in serum than analogous copper compounds; an azacrown-derived cycle with five heteroatoms coordinates zinc, providing fast complexation and high in vivo stability.

Copper complexes as antitumor agents: in vitro and in vivo evidences

2021 ◽  
Vol 28 ◽  
Author(s):  
Lucia M. Balsa ◽  
Enrique J. Baran ◽  
Ignacio E. León
Keyword(s):  
Copper Complexes ◽  
Antitumor Agents ◽  
Essential Element ◽  
Design Synthesis ◽  
Copper Compounds ◽  
Comprehensive Knowledge ◽  
The Relationship

: Copper is an essential element for most aerobic organisms, with an important function as a structural and catalytic cofactor, and in consequence, it is implicated in several biological actions. The relevant aspects of chemistry and biochemistry and the importance of copper compounds in medicine give us a comprehensive knowledge of the multifaceted applications of copper in physiology and physiopathology. In this review, we present an outline of the chemistry and the antitumor properties of copper complexes on breast, colon, and lung cancer cells focus on the role of copper in cancer, the relationship between structure-activity, molecular targets, and the study of the mechanism of action involved in its anticancer activity. This overview is expected to contribute to understanding the design, synthesis, uses of copper complexes as antitumor agents in the most common cancers.

Comparative stability of dihydrofolate reductase mutants in vitro and in vivo

1993 ◽  
Vol 6 (1) ◽  
pp. 81-84 ◽  
Author(s):  
Vladimir V. Leontiev ◽  
Vladimir N. Uversky ◽  
Anatoly T. Gudkov
Keyword(s):  
Dihydrofolate Reductase ◽  
Comparative Stability

Complexes of 65Zn and Phe-D-Trp-Lys-Thr Tetrapeptide Conjugates with Azacrown Ethers: Synthesis, in Vitro and in Vivo Stability

INEOS OPEN ◽  
2020 ◽  
Vol 2 (6) ◽  
pp. 200-204
Author(s):  
G. Yu. Aleshin ◽  
◽  
S. Yu. Khabirova, ◽  
V. N. Osipov ◽  
D. S. Khachatryan ◽  
...  
Keyword(s):  
Azacrown Ethers

Copper(II) mixed-ligand complexes containing 1, 10-phenanthroline, adenine and thymine: Synthesis, characterization and antibacterial activities

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Copper Complexes ◽  
Antimicrobial Agents ◽  
Conductivity Measurement ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
E Coli ◽  
In Vivo Cytotoxicity

New copper complexes, [Cu(phen)2(Thy)]2Cl and [Cu(phen)2(Ad)]2Cl (phen = 1,10-phenantroline, Ad (Adenine, a purine nucleobase) and Thy (Thymine, a pyrimidine nucleobase)), were synthesized and characterized by atomic absorption spectroscopy (AAS), conductivity measurement, UV-visible and infrared (IR) techniques. The complexes were tested for their antimicrobial activity against two gram positive and two gram negative bacterial strains. The results of in vitro antimicrobial activities were compared with the commercially available antimicrobial agents (ciprofloxacin and chloramphenicol). This comparative study has demonstrated that [Cu(phen)2(Thy)]2Cl inhibited the growth of methicillin resistant Staphylococcus aureous (MRSA), Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumonia) better than chloramphenicol by 11.25%, 19.41% and 25.35%, respectively. It also showed better activities than ciprofloxacine on MRSA and K. pneumoniae by 2.50% and 12.13%, respectively. Similarly, [Cu(phen)2(Ad)]2Cl demonstrated better inhibitions than chloramphenicol against MRSA, E. coli and K. pneumoniae by 11.24%, 2.48% and 9.06%, respectively. Therefore, after in vivo cytotoxicity investigations, these complexes could be considered as potential antimicrobial agents.

scholarly journals Synthesis and Crystalline Structure of Zinc Complexes with Antihypertensive Drug Lisinopril

2018 ◽  
Vol 2018 ◽  
pp. 1-9 ◽  
Author(s):  
Márcia C. de Souza ◽  
Luan F. Diniz ◽  
Chris H. J. Franco ◽  
Renata Diniz
Keyword(s):  
Structural Investigation ◽  
Zinc Complexes ◽  
One Dimensional ◽  
1D Coordination Polymer ◽  
Structural Differences ◽  
Synthetic Routes ◽  
Solvothermal Conditions ◽  
Formation Of Complexes

The structural investigation of Zn2+ complexes with the ligand lisinopril (LIS), an inhibitor of angiotensin-converting enzyme (ACE), was performed. The main objective is to compare if Zn-LIS coordination in vitro is similar to that observed in vivo. Two zinc complexes were obtained from different synthetic routes. The synthesis of LISZn1 used stirring, while for LISZn2 involved solvothermal conditions, which favoured the full deprotonation of lisinopril ligand. In this sense, the different synthetic routes resulted in the formation of complexes with notorious chemical and structural differences. The crystal structure of LISZn2 showed that the ligand is coordinated to Zn2+ ion by oxygen and nitrogen atoms which is different from that observed in vivo. In vitro, the coordination of lisinopril occurs only by an oxygen atom of the central carboxylate group. LISZn2 forms a one-dimensional (1D) coordination polymer and presents disorder atoms in its unit cell.

In vitro and in vivo anticancer activity of tridentate thiosemicarbazone copper complexes: Unravelling an unexplored pharmacological target

2020 ◽  
Vol 194 ◽  
pp. 112266 ◽  
Author(s):  
Mauro Carcelli ◽  
Matteo Tegoni ◽  
Jennifer Bartoli ◽  
Cristina Marzano ◽  
Giorgio Pelosi ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Copper Complexes ◽  
Pharmacological Target

scholarly journals The long and short of it: the influence of N-carboxyethyl versusN-carboxymethyl pendant arms on in vitro and in vivo behavior of copper complexes of cross-bridged tetraamine macrocycles

2007 ◽  
pp. 2150 ◽  
Author(s):  
Katie J. Heroux ◽  
Katrina S. Woodin ◽  
David J. Tranchemontagne ◽  
Peter C. B. Widger ◽  
Evan Southwick ◽  
...  
Keyword(s):  
Copper Complexes ◽  
Pendant Arms

scholarly journals The radioenhancement potential of Schiff base derived copper (II) compounds against lung carcinoma in vitro

PLoS ONE ◽  
2021 ◽  
Vol 16 (6) ◽  
pp. e0253553
Author(s):  
Gohar Tsakanova ◽  
Ani Stepanyan ◽  
Elina Arakelova ◽  
Violetta Ayvazyan ◽  
Vahan Tonoyan ◽  
...  
Keyword(s):  
Cell Growth ◽  
Lung Carcinoma ◽  
Copper Complexes ◽  
Dependent Manner ◽  
Lung Carcinoma Cells ◽  
Copper Compounds ◽  
Physical Measurements ◽  
Human Lung Carcinoma ◽  
Good Potential

For the last years, copper complexes have been intensively implicated in biomedical research as components of cancer treatment. Herewith, we provide highlights of the synthesis, physical measurements, structural characterization of the newly developed Cu(II) chelates of Schiff Bases, Cu(Picolinyl-L-Tryptopahanate)2, Cu(Picolinyl-L-Tyrosinate)2, Cu(Isonicotinyl-L-Tyrosinate)2, Cu(Picolinyl-L-Phenylalaninate)2, Cu(Nicotinyl-L-Phenylalaninate)2, Cu(Isonicotinyl-L-Phenylalaninate)2, and their radioenhancement capacity at kV and MV ranges of irradiation of human lung carcinoma epithelial cells in vitro. The methods of cell growth, viability and proliferation were used. All compounds exerted very potent radioenhancer capacities in the irradiated lung carcinoma cells at both kV and MV ranges in a 100 μM concentration. At a concentration of 10 μM, only Cu(Picolinyl-L-Tyrosinate)2, Cu(Isonicotinyl-L-Tyrosinate)2, Cu(Picolinyl-L-Phenylalaninate)2 possessed radioenhancer properties at kV and MV ranges. Cu(Picolinyl-L-Tryptophanate)2 showed radioenhancer properties only at kV range. Cu(Nicotinyl-L-Phenylalaninate)2 and Cu(Isonicotinyl-L-Phenylalaninate)2 showed remarkable radioenhancer activity only at MV range. All compounds acted in dose-dependent manner at both tested energy ranges. These copper (II) compounds, in combination with 1 Gy irradiation at either 120 kV or 6 MV, are more efficient at delaying cell growth of lung cancer cells and at reducing cell viability in vitro than the irradiation administered alone. Thus, we have demonstrated that the studied copper compounds have a good potential for radioenhancement.

scholarly journals Antineoplastic Evaluation of Two Mixed Chelate Copper Complexes (Casiopeínas®) in HCT-15 Xenograft Model

2017 ◽  
Vol 57 (3) ◽  
Author(s):  
María Elena Bravo-Gómez ◽  
Ana Laura Hernández de la Paz ◽  
Isabel Gracia-Mora
Keyword(s):  
Biological Activity ◽  
Antitumor Activity ◽  
Mouse Models ◽  
Copper Complexes ◽  
Xenograft Model ◽  
Colon Adenocarcinoma ◽  
Diimine Ligand ◽  
Secondary Ligand

Casiopeínas<sup>®</sup> is a family of copper complexes with the general formulae [Cu(N-N)(N-O)]NO<sub>3</sub> and [Cu(N-N)(O-O)]NO<sub>3</sub>; where N-N = substituted aromatic diimine (2,2’-bipyridine (<em>bipy</em>) or 1,10-phenanthroline (<em>phen</em>)); N-O = α-aminoacidate or a peptide; and O-O = acetylacetonate (<em>acac</em>) or salicylaldehydate. These compounds have shown antiproliferative activity in vitro and antitumor activity in several mouse models with promissory results. Efforts have been done in order to understand the role played by ligands in the biological activity. With the aim of finding out the effect of secondary ligand (N-O or O-O), two of the most active complexes <em>in vitro</em> assays were selected to perform in vivo study on HCT-15 colon adenocarcinoma xenograft model. Both complexes, [Cu(3,4,7,8-tetramethyl-1,10-phen anthroline)(glycinato)]NO<sub>3</sub> (<strong>1</strong>) and [Cu(3,4,7,8-tetramethyl-1,10-phenanthroline)(acetylacetonato)]NO<sub>3</sub> (<strong>2</strong>) share the same diimine ligand and the secondary ligand changes from glycinate (<em>gly</em>) to <em>acac</em>. Results show that 2 is effective to reduce tumor size but <strong>1</strong> does not achieve the values required according to protocols, revealing an important difference between compounds attributable to change of ligand from <em>gly</em> to <em>acac</em>.

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