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

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.

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.

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 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>.

scholarly journals Copper complexes as prospective anticancer agents: in vitro and in vivo evaluation, selective targeting of cancer cells by DNA damage and S phase arrest

RSC Advances ◽  
2018 ◽  
Vol 8 (30) ◽  
pp. 16973-16990 ◽  
Author(s):  
Dharmasivam Mahendiran ◽  
Sethu Amuthakala ◽  
Nattamai S. P. Bhuvanesh ◽  
Raju Senthil Kumar ◽  
Aziz Kalilur Rahiman
Keyword(s):  
Dna Damage ◽  
Anticancer Agents ◽  
Copper Complexes ◽  
S Phase ◽  
In Vivo Evaluation ◽  
Phase Arrest ◽  
Selective Targeting ◽  
S Phase Arrest

The thiosemicarbazone-based copper(i) complexes causing S phase arrest and apoptosis involving the mitochondrial controlled pathway has been investigated.

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.

scholarly journals In vitro evaluation of antileishmanial activity of copper (I) complexes

2021 ◽  
Vol 5 (1) ◽  
pp. 1
Author(s):  
Ana Flávia Da Silva Chagas ◽  
Marina Porchia ◽  
Francesco Tisato ◽  
Pauline De Faria Soldera ◽  
Claudia Dantas Comandolli Wyrepkowski ◽  
...  
Keyword(s):  
Copper Complexes ◽  
New Drugs ◽  
In Vivo Studies ◽  
In Vitro Assays ◽  
American Tegumentary Leishmaniasis ◽  
Infected Cells ◽  
Prevalent Species ◽  
Phosphine Complex

In the research for the development of new drugs for the therapy of American tegumentary leishmaniasis, copper has been studied for its antileishmania activity. This study aims to report the activity of three copper(I) complexes on parasites of the species L. amazonensis and L. guyanensis. The metal complexes were tested according to in vitro antileishmanial assays, against promastigote and amastigote forms of the most prevalent species in the state of Amazonas, Brazil. Cytotoxicity of the complexes was evaluated in murine macrophage-like cell line (MJ774). The results of the in vitro assays indicated that, among the copper complexes tested, the homoleptic phosphine complex [Cu(thp)4][PF6](thp=tris-hydroxymethylphosphine) presented promising activity against the evolutionary forms of L. amazonensis, and obtained a IC50 of  26.45 and 24.61 µM in a period of 48 and 72 h, respectively. The results for copper complex at concentration 160 µM in amastigote forms showed a decrease in the infection index (32% of infected cells) and, in the cytotoxicity assay with MJ774, 52.43% of cell viability was observed. The results showed that the complex [Cu(thp)4][PF6] presented significant biological activity, indicating a need for future in vivo studies.

Induction and Differentiation of Dental Epithelium in Vivo and in Vitro

1982 ◽  
Vol 40 ◽  
pp. 142-145
Author(s):  
E. J. Kollar
Keyword(s):  
Connective Tissue ◽  
Oral Mucosa ◽  
Basal Lamina ◽  
Functional Derivatives ◽  
Specific Source ◽  
Dental Epithelium ◽  
Connective Tissue Stroma

The differentiation and maintenance of many specialized epithelial structures are dependent on the underlying connective tissue stroma and on an intact basal lamina. These requirements are especially stringent in the development and maintenance of the skin and oral mucosa. The keratinization patterns of thin or thick cornified layers as well as the appearance of specialized functional derivatives such as hair and teeth can be correlated with the specific source of stroma which supports these differentiated expressions.

Ultrastructural Correlations between Clonal Human Tumor Colonies and in Vivo Neoplasms

1982 ◽  
Vol 40 ◽  
pp. 210-211
Author(s):  
M.J. Murphy ◽  
R.R. Price ◽  
J.C. Sloman
Keyword(s):  
Cultured Cells ◽  
Human Tumor ◽  
Cell Type ◽  
Tumor Mass ◽  
Initial Cell ◽  
Cloning Assay ◽  
Human Tumor Cloning ◽  
The Relationship

The in vitro human tumor cloning assay originally described by Salmon and Hamburger has been applied recently to the investigation of differential anti-tumor drug sensitivities over a broad range of human neoplasms. A major problem in the acceptance of this technique has been the question of the relationship between the cultured cells and the original patient tumor, i.e., whether the colonies that develop derive from the neoplasm or from some other cell type within the initial cell population. A study of the ultrastructural morphology of the cultured cells vs. patient tumor has therefore been undertaken to resolve this question. Direct correlation was assured by division of a common tumor mass at surgical resection, one biopsy being fixed for TEM studies, the second being rapidly transported to the laboratory for culture.

Ultrastructure of melanocyte-keratinocyte interactions and pigment transfer in vitro

1978 ◽  
Vol 36 (2) ◽  
pp. 650-651
Author(s):  
Raul I. Garcia ◽  
Evelyn A. Flynn ◽  
George Szabo
Keyword(s):  
Direct Injection ◽  
Skin Pigmentation ◽  
Freeze Fracture ◽  
Pigment Granule ◽  
Time Lapse ◽  
Ultrastructural Level ◽  
Lanthanum Tracer ◽  
A Cell

Skin pigmentation in mammals involves the interaction of epidermal melanocytes and keratinocytes in the structural and functional unit known as the Epidermal Melanin Unit. Melanocytes(M) synthesize melanin within specialized membrane-bound organelles, the melanosome or pigment granule. These are subsequently transferred by way of M dendrites to keratinocytes(K) by a mechanism still to be clearly defined. Three different, though not necessarily mutually exclusive, mechanisms of melanosome transfer have been proposed: cytophagocytosis by K of M dendrite tips containing melanosomes, direct injection of melanosomes into the K cytoplasm through a cell-to-cell pore or communicating channel formed by localized fusion of M and K cell membranes, release of melanosomes into the extracellular space(ECS) by exocytosis followed by K uptake using conventional phagocytosis. Variability in methods of transfer has been noted both in vivo and in vitro and there is evidence in support of each transfer mechanism. We Have previously studied M-K interactions in vitro using time-lapse cinemicrography and in vivo at the ultrastructural level using lanthanum tracer and freeze-fracture.

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