Ruthenium(II) bipyridine complexes: From synthesis and crystal structures to electrochemical and cytotoxicity investigation
Creators
- 1. Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, 11 000 Belgrade, Serbia
- 2. Innovation Center of the Faculty of Chemistry, University of Belgrade, Studentski trg 12-16, 11 000 Belgrade, Serbia
- 3. Institute for Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia
- 4. XStruct, Department of Inorganic and Physical Chemistry, Ghent University, Krijgslaan 281-S3
Description
Complexes 1-4, [Ru(L)(bpy)2]PF6, where bpy = 2,2′-bipyridine; L = 3-methylpyridine-2-
carboxylic acid (L1), 6-methylpyridine-2-carboxylic acid (L2), 5-bromopyridine-2-carboxylic
acid (L3) and 6-bromopyridine-2-carboxylic acid (L4), were synthesized and characterized. The
electrochemical character of the complexes was investigated by cyclic voltammetry revealing
two reversible reduction waves in the negative range of potentials, most likely due to a reduction
of the bipyridine moiety. Cytotoxicity studies by MTT assay for 72 h of drug action revealed that
2-4 exhibited moderate activity in cervical human tumor cells (HeLa). Complex 2 exhibited low
activity in colon cancer LS-174 cells (180 ± 10), while all complexes were devoid of activity in
lung cancer A549 and non-tumor MRC-5 cells, up to 200 μM. Combinational studies of the most
active complex 2, with pharmacological modulators of cell redox status, L-buthioninesulfoximine
(L-BSO) or N-acetyl-L-cysteine (NAC), showed that when L-BSO potentiated, 2
induced a sub-G1 peak of the cell cycle in the HeLa cell line. UV-vis and cyclic voltammetry
were performed in order to investigate the binding mode of 2 to DNA and suggested
intercalation for the complex-DNA interaction.
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Additional details
Related works
- Is part of
- 0095-8972 (ISSN)
- gnd:1029-0389 ( (gnd)
Funding
- Pharmacodynamic and pharmacogenomic research of new drugs in the treatment of solid tumors 41026
- Ministry of Education, Science and Technological Development
- FCUB-ERA – Reinforcement of the Faculty of Chemistry, University of Belgrade, towards becoming a Center of Excellence in the region of WB for Molecular Biotechnology and Food research 256716
- European Commission