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SYNTHESIS OF RUTHENIUM COMPLEXES AND ASSESSING THEIR ANTICANCER AND ANTIBACTERIAL EFFECTS

ALI ZEIZ 1, SUZANNE CHAYYA 2, ZEINAB KASSEM 3, AKRAM HIJAZI 3, GHADA KHAWAJA 1, MOHAMMAD H. EL-DAKDOUKI 2*

1Department of Biological Sciences, Faculty of Science, Beirut Arab University, P.O. Box 11-5020, Riad El Solh 11072809, Beirut, Lebanon
2Department of Chemistry, Faculty of Science, Beirut Arab University, P.O. Box 11-5020, Riad El Solh 11072809, Beirut, Lebanon
3Doctoral School of Science and Technology, Platform for Research and Analysis in Environmental Sciences (PRASE), Lebanese University, Beirut, Lebanon

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Ruthenium (Ru) complexes exhibit intriguing biological effects, including potent antibacterial and anticancer activities. The aim of this study was to prepare Ru(dppz)(DMSO)2Cl2 complex from cis-fac-dichlorotetrakis(dimethylsulfoxide)ruthenium(II) precursor (cis-Ru(DMSO)4Cl2), and assess its anticancer and antibacterial activities. The complex was characterized by NMR and FTIR spectroscopies. The physiochemical properties of the prepared complexes were predicted by employing MolSoft software and its DNA binding potential was assessed using molecular docking. The complex displayed an intercalative mode of DNA binding with a binding affinity of -15.93 kcal/mol and a hydrogen bonding of 2.5 Å. Additionally, Ru complex exhibited a promising antibacterial effect against E. coli, E. faecalis, P. aeruginosa and S. aureus at a minimum inhibitory concentration (MIC) of ~ 30 μg/mL. The cytotoxic activity of cis-Ru(DMSO)4Cl2 and Ru(dppz)(DMSO)2Cl2 complexes against colorectal (HCT-116) and breast cancer (MCF-7) cell lines was elucidated by using the MTT cell viability assay, and the latter complex displayed an intriguing low IC50 value (12.6 μM) in HCT-116 cells. The precise molecular mechanism of action of Ru(dppz)(DMSO)2Cl2 complex was deciphered by tracking the expression levels of key apoptotic proteins, namely p53, Bax and Bcl-2. Western blotting analysis showed that the anticancer activity is mediated by the complex’s ability to activate the mitochondrial apoptotic pathway, as evident by modulating the expression level of p53, Bax and Bcl-2 proteins.