Progress in Copper Complexes as Anticancer Agents

Tabti, Redouane; Tounsi, Nassera; Gaiddon, Christian; Bentouhami, Embarek; Désaubry, Laurent

doi:10.4172/2161-0444.1000445

Cited by 74 publications

(42 citation statements)

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“…To date several copper(II) complexes have been tested as a potential anticancer agents. The main benefit of copper(II) complexes lies in their ability to be selectively reduced to copper(I) complexes in malignant cells to induce cell death . In the light of this information, our group focused on the in vitro cytotoxic activity of complexes 1 – 3 .…”

Section: Resultssupporting

confidence: 75%

Methyl substituent effect on one‐dimensional copper(II) coordination polymers containing biologically active ligands: Synthesis, characterization, DNA interactions and cytotoxicities

Şenel

İnci

Aydın

et al. 2019

Applied Organom Chemis

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Three novel water‐soluble copper(II) complexes – {[Cu(phen)(trp)]ClO4·3H2O}n (1), {[Cu(4‐mphen)(trp)]ClO4·3H2O}n (2) and [[Cu(dmphen)(trp)(MeOH)][Cu(dmphen)(trp)(NO3)]]NO3 (3) (phen: 1,10‐phenanthroline; 4‐mphen: 4‐methyl‐1,10‐phenanthroline; dmphen: 4,7‐dimethyl‐1,10‐phenanthroline; trp: l‐tryptophan) – have been synthesized and characterized using various techniques. Complexes 1 and 2 are isostructural, and exist as one‐dimensional coordination polymers. Complex 3 consists of two discrete copper(II) complexes containing [Cu(trp)(dmphen)(MeOH)]+, [Cu(trp)(dmphen)(NO3)] and one nitrate anion. The binding interaction of the complexes with calf thymus DNA (CT‐DNA) was investigated using thermal denaturation, electronic absorption and emission spectroscopic methods, revealing that the complexes could interact with CT‐DNA via a moderate intercalation mode. The binding activity of the complexes to CT‐DNA follows the order: 3 > 2 > 1. The pUC19 DNA cleavage activity of the complexes was investigated in the absence and presence of external agents using the agarose gel electrophoresis method. Especially, in the presence of H2O2 as an activator, the pUC19 DNA cleavage abilities of the complexes are clearly enhanced at low concentration. Addition of hydroxyl radical scavenger dimethylsulfoxide shows a marked inhibition of the pUC19 DNA cleavage activity of the complexes. In vitro cytotoxic effect of the complexes was examined on human tumor cell lines (Caco‐2, A549 and MCF‐7) and healthy cells (BEAS‐2B). The potent cytotoxic effect of complex 3, with IC50 values of 1.04, 1.16 and 1.72 μM, respectively, is greater relative to clinically used cisplatin (IC50 = 22.70, 31.1 and 22.2 μM) against the Caco‐2, A549 and MCF‐7 cell lines.

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Section: Resultssupporting

confidence: 75%

Methyl substituent effect on one‐dimensional copper(II) coordination polymers containing biologically active ligands: Synthesis, characterization, DNA interactions and cytotoxicities

Şenel

İnci

Aydın

et al. 2019

Applied Organom Chemis

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“…Copper complexes are promising new anticancer agents which may be used for treatment of cancer resistant to cisplatin [7–9, 18]. CuHQTS is a new copper complex with anticancer activity on prostate cancer cells in vitro [16], in addition to potent anticancer activity on cisplatin-resistant neuroblastoma cells [12].…”

Section: Discussionmentioning

confidence: 99%

“…Cisplatin is a potent metallotherapeutic drug, but clinical application of cisplatin for treatment of prostate cancer is limited by side effects and acquired cisplatin-resistance of metastatic prostate cancer [3–6]. In addition to synthesizing and testing new organic molecules or compounds for anti-prostate cancer activities, there are continued efforts to develop new metallotherapeutic drugs for treatment of patients suffered from metastatic prostate cancer that are resistant to cisplatin or other anticancer drugs currently available [7–9]. …”

Section: Introductionmentioning

confidence: 99%

Anti-prostate cancer activity of 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazide copper complexes in vivo by bioluminescence imaging

2018

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Copper 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazide complex (CuHQTS) is a copper complex with strong anticancer activity against cisplatin-resistant neuroblastoma and prostate cancer cells in vitro by cell proliferation assay or fluorescent microscopic imaging. This study aimed to evaluate anti-prostate cancer activity of CuHQTS in vivo by bioluminescence imaging (BLI) and tumor size measurement, using athymic nu/nu mice implanted with prostate cancer cells carrying luciferase reporter gene (Luc-PC3). Growth of Luc-PC3 cells (1 × 10 cells) implanted in athymic nu/nu mice treated with CuHQTS for 2 weeks was suppressed by measurement of luciferase signals (6.18 × 10 to 5.36 × 10 p/s/cm/sr) with BLI, compared with luciferase signals of Luc-PC3 cells (4.66 × 10 to 1.51 × 10 p/s/cm/sr, p < 0.05) in the mice treated with normal saline of placebo control. Moreover, the size of PC-3 xenograft tumor (126.5 ± 34.2 mm) in athymic nu/nu mice treated with CuHQTS was significantly smaller than the size of PC-3 xenograft tumor (218.6 ± 48.0 mm, p < 0.05) in athymic nu/nu mice treated with normal saline of placebo control, suggesting in vivo tumor growth inhibition activity of CuHQTS on prostate cancer. The findings of this study support further investigation of CuHQTS as a promising new anticancer agent for the treatment of metastatic prostate cancer refractory to anticancer drugs currently available.

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“…Therapies based on the copper(II)‐ l ‐His supplementation are operative in the treatment of Menkes disease . Besides, the copper chelation therapy for treatment of neurodegenerative disorders (such as Parkinson, Alzheimer, Creutzfeldt Jakob) and several types of cancers has been under development in the last decades …”

Section: Introductionmentioning

confidence: 98%

Conformational Analyses of Physiological Binary and Ternary Copper(II) Complexes with l‐Asparagine and l‐Histidine; Study of Tridentate Binding of Copper(II) in Aqueous Solution

et al. 2019

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This study explores the structural properties and energy landscapes of the physiologically important bis( l ‐asparaginato)copper(II) [Cu( l ‐Asn) 2 ] and ( l ‐histidinato)( l ‐asparaginato)copper(II) [Cu( l ‐His)( l ‐Asn)]. The conformational analyses in the gas phase and implicitly modeled water medium, and magnetic parameters of electron paramagnetic resonance spectra were attained using density functional theory calculations. The apical Cu II coordination and hydrogen bonding were analyzed. Predicted lower‐energy structures enabled the confirmation and, for apical bonding, also the refinement of structural proposals from literature. Available experimental results were indecisive regarding the amido‐group binding in the Cu II equatorial plane in solutions, but the examination of the relative stability of Cu( l ‐Asn) 2 conformers in 30 binding modes confirms the glycine‐like mode as the most stable one. Previously reported experimental results for Cu( l ‐His)( l ‐Asn) were interpreted for l ‐His to have a tridentate histamine‐like mode. However, the aqueous conformers with l ‐His in the glycinato mode are also predicted to have low energies, which does not contradict the tridentate l ‐His binding. The predicted magnetic parameters of conformers with an apical oxygen atom (intramolecular or from a water molecule) can reproduce the experimental data. An extent of conformational flexibility and abundance of l ‐His‐containing ternary copper(II) amino acid complexes under physiological conditions may be related.

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Progress in Copper Complexes as Anticancer Agents

Cited by 74 publications

References 0 publications

Methyl substituent effect on one‐dimensional copper(II) coordination polymers containing biologically active ligands: Synthesis, characterization, DNA interactions and cytotoxicities

Methyl substituent effect on one‐dimensional copper(II) coordination polymers containing biologically active ligands: Synthesis, characterization, DNA interactions and cytotoxicities

Anti-prostate cancer activity of 8-hydroxyquinoline-2-carboxaldehyde-thiosemicarbazide copper complexes in vivo by bioluminescence imaging

Conformational Analyses of Physiological Binary and Ternary Copper(II) Complexes with l‐Asparagine and l‐Histidine; Study of Tridentate Binding of Copper(II) in Aqueous Solution

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