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Heteroleptic arene Ru(II) dipyrrinato complexes: DNA, protein binding and anti-cancer activity against the ACHN cancer cell line.
- Source :
-
Dalton transactions (Cambridge, England : 2003) [Dalton Trans] 2016 Apr 28; Vol. 45 (16), pp. 7163-77. - Publication Year :
- 2016
-
Abstract
- Four organometallic complexes [(η(6)-C6H6)RuCl(pmpzdpm)], 1; [(η(6)-C6H6)RuCl(pypzdpm)], 2; [(η(6)-C10H14)RuCl(pmpzdpm)], 3 and [(η(6)-C10H14)RuCl(pypzdpm)], 4 containing 5-(2-pyrimidyl-piperazine)phenyldipyrromethene (pmpzdpm) and 5-(2-pyridylpiperazine)phenyldipyrromethene (pypzdpm) have been designed and synthesized. The complexes 1-4 have been fully characterized by elemental analyses and spectroscopic studies (ESI-MS, IR, (1)H, (13)C NMR, UV-vis). Their electrostatic/intercalative interaction with CT DNA has been investigated by UV-vis and competitive ethidium bromide displacement studies while their protein binding affinity toward bovine serum albumin (BSA) was realized by UV-vis, fluorescence, synchronous and three dimensional (3D) fluorescence studies. The interaction with DNA and protein has further been validated by in silico studies. Cellular uptake, in vitro cytotoxicity and flow cytometric analyses have been performed to determine the mode of cell death against the kidney cancer cell line ACHN. Cell cycle analysis suggested that the complexes cause cell cycle arrest in the subG1 phase and overall results indicated that the in vitro antitumor activity of 1-4 lies in the order of 3 >4 >1 >2 (IC50, 7.0 1; 8.0 2; 2.0 3; 4.0 μM,4 ).
- Subjects :
- Animals
Antineoplastic Agents chemistry
Apoptosis drug effects
Cattle
Cell Line, Tumor
Cell Survival drug effects
DNA chemistry
Humans
Molecular Docking Simulation
Nucleic Acid Conformation
Organometallic Compounds chemistry
Protein Binding
Protein Conformation
Serum Albumin, Bovine chemistry
Antineoplastic Agents metabolism
Antineoplastic Agents pharmacology
DNA metabolism
Organometallic Compounds metabolism
Organometallic Compounds pharmacology
Ruthenium chemistry
Serum Albumin, Bovine metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1477-9234
- Volume :
- 45
- Issue :
- 16
- Database :
- MEDLINE
- Journal :
- Dalton transactions (Cambridge, England : 2003)
- Publication Type :
- Academic Journal
- Accession number :
- 27009608
- Full Text :
- https://doi.org/10.1039/c6dt00446f