Journal
JOURNAL OF ORGANOMETALLIC CHEMISTRY
Volume 801, Issue -, Pages 68-79Publisher
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jorganchem.2015.10.008
Keywords
Organometallic complexes; Benzimidazole; DNA and protein binding; Cytotoxicity; Anticancer activity; Molecular docking
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Funding
- Department of Science and Technology (DST), New Delhi, India [SR/S1/IC-25/2011]
- Council of Scientific and Industrial Research (CSIR), New Delhi, India [09/013(0330)/2009-EMR-I]
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Synthesis, characterization, DNA and protein binding as well as anticancer activity of the organometallic complexes [(eta(6)-C6H6)RuCl(APBI)]Cl (1), [(eta(6)-p-MeC6H4Pri)RuCl(APBI)] Cl (2), [(eta(6)-C6Me6)RuCl(APBI)]Cl (3), [(eta(5)-C5Me5)RhCl(APBI)]Cl center dot H2O (4) and [(eta(5)-C5Me5)IrCl(APBI)]Cl center dot H2O (5) containing 2-aminophenyl benzimidazole (APBI) have been described. The complexes 1-5 exhibited strong DNA, protein binding and anticancer activity against cervical cancer (SiHa) cell line. Their binding with calf thymus DNA (CT-DNA) and bovine serum albumin (BSA) have been examined by absorption and emission spectral studies. Strong interactions between complexes and CT-DNA have been affirmed by absorption spectral and EthBr displacement studies, while interaction with BSA via static quenching explored by fluorescence titration, synchronous and 3D fluorescence spectroscopy. The interactions between 1-5 and DNA has also been scrutinized by H-1 NMR spectral studies using guanosine as a model for DNA. These results have been supported by DFT calculations and molecular docking studies. Cytotoxicity, apoptosis and in vitro anticancer activity of 1-5 toward SiHa cell line have been investigated by MTT assay and acridine (AO)/ethidium bromide (EthBr) fluorescence staining. Overall results revealed that DNA and protein binding, as well as anticancer activity of 1-5 follows the order as 5 > 3 > 2 > 1 > 4. (C) 2015 Elsevier B.V. All rights reserved.
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