| Title |
Impact of aromaticity on anticancer activity of polypyridyl ruthenium(II) complexes: synthesis, structure, DNA/protein binding, lipophilicity and anticancer activity
|
|---|---|
| Published in |
JBIC Journal of Biological Inorganic Chemistry, July 2017
|
| DOI | 10.1007/s00775-017-1479-7 |
| Pubmed ID | |
| Authors |
Petar Čanović, Ana Rilak Simović, Snežana Radisavljević, Ioannis Bratsos, Nicola Demitri, Marina Mitrović, Ivanka Zelen, Živadin D. Bugarčić |
| Abstract |
With the aim of assessing how the aromaticity of the inert chelating ligand can influence the activity of ruthenium(II) polypyridyl complexes, two new monofunctional ruthenium(II) complexes, [Ru(Cl-Ph-tpy)(phen)Cl]Cl (1) and [Ru(Cl-Ph-tpy)(o-bqdi)Cl]Cl (2) (where Cl-Ph-tpy = 4'-(4-chlorophenyl)-2,2':6',2″-terpyridine, phen = 1,10-phenanthroline, o-bqdi = o-benzoquinonediimine), were synthesized. All complexes were fully characterized by elemental analysis and spectroscopic techniques (IR, UV-Vis, 1D and 2D NMR, XRD). Their chemical behavior in aqueous solution was studied by UV-Vis and NMR spectroscopy showing that both compounds are relatively labile leading to the formation of the corresponding aqua species 1a and 2a. (1)H NMR spectroscopy studies performed on complexes 1 and 2 demonstrated that after the hydrolysis of the Cl ligand, they are capable to interact with guanine derivatives (i.e., 9-methylguanine (9MeG) and 5'-GMP) through the N7, forming monofunctional adduct. The kinetics and the mechanism of the reaction of complexes 1 and 2 with the biologically more relevant 5'-GMP ligand were studied by UV-Vis spectroscopy. DNA/protein interactions of the complexes have been examined by photophysical studies, which demonstrated a bifunctional binding mode of the complexes with DNA and the complexes strongly quench the fluorescence intensity of bovine serum albumin (BSA) through the mechanism of both static and dynamic quenching. Complexes 1 and 2 strongly induced apoptosis of treated cancer cells with high percentages of apoptotic cells and negligible percentage of necrotic cells. In addition, both ruthenium complexes decreased Bcl-2/Bax ratio causing cytochrome c mitochondrial release, the activation of caspase-3 and induction of apoptosis. |
X Demographics
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Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 1 | 100% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Members of the public | 1 | 100% |
Mendeley readers
The data shown below were compiled from readership statistics for 43 Mendeley readers of this research output. Click here to see the associated Mendeley record.
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 43 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Ph. D. Student | 11 | 26% |
| Researcher | 9 | 21% |
| Student > Master | 5 | 12% |
| Professor > Associate Professor | 3 | 7% |
| Unspecified | 2 | 5% |
| Other | 4 | 9% |
| Unknown | 9 | 21% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 21 | 49% |
| Biochemistry, Genetics and Molecular Biology | 3 | 7% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 2% |
| Unspecified | 1 | 2% |
| Agricultural and Biological Sciences | 1 | 2% |
| Other | 3 | 7% |
| Unknown | 13 | 30% |
Attention Score in Context
This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 16 December 2017.
All research outputs
#21,180,380
of 23,842,189 outputs
Outputs from JBIC Journal of Biological Inorganic Chemistry
#590
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Outputs of similar age
#274,645
of 314,251 outputs
Outputs of similar age from JBIC Journal of Biological Inorganic Chemistry
#6
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