Synthesis, Spectral Properties and DFT Calculations of new Ruthenium (II) Polypyridyl Complexes; DNA Binding Affinity and in Vitro Cytotoxicity Activity

Abstract

In this paper a novel ligand debip (2-(4-N,N-diethylbenzenamine)1H-imidazo[4,5-f] [1, 10]phenanthroline) and its Ru(II) polypyridyl complexes [Ru(L)(debip)], (L = phen (1), bpy (2) and dmb (3)) have been synthesized and characterized by spectroscopic techniques. The DNA binding studies for all these complexes were examined by absorption, emission, quenching studies, viscosity measurements and cyclic voltammetry. The light switching properties of complexes 1-3 have been evaluated. Molecular docking, Density Functional Theory (DFT) and time dependent DFT calculations were performed. The Ru(II) complexes exhibited efficient photocleavage activity against pBR322 DNA upon irradiation and exhibited good antimicrobial activity. Also investigated 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) reduction assay, lactate dehydrogenase (LDH) release assay and reactive oxygen species (ROS) against selected cancer cell lines (HeLa, PC3, Lancap, MCF-7 and MD-MBA 231).

Antitumor Activity of Ruthenium(II) Terpyridine Complexes towards Colon Cancer Cells In Vitro and In Vivo

“…The LDH levels increased up to 36.43% for CT26 cells following Ru-1 treatment, and up to 33.07% for SW480 cells following Ru-2 treatment at a concentration of 300 μM and only 2.20% for SW480 cells after 24 h treatment with oxaliplatin at the same concentration, which is in line with previous studies [ 24 ]. These results are in accordance with previous reports that ruthenium(II) polypyridyl complexes at lower concentrations do not affect the release of LDH enzyme from various tumor cells (HeLa, PC3, LanCap, MCF-7, and MD-MBA 231), but when the cells were treated with higher concentrations of ruthenium(II) polypyridyl complexes, the LDH activity in the culture media increased significantly [ 25 ]. However, the percentages of necrotic cells remain generally low after exposure of colorectal tumor cells to piplartine and arene ruthenium(II) complexes [ 26 , 27 ].…”

Antineoplastic activity of a novel ruthenium complex against human hepatocellular carcinoma (HepG2) and human cervical adenocarcinoma (HeLa) cells

“…Several experimental drugs have also been reported to act primarily on mitochondria to induce cancer cell death [42,44]. The modulation of key enzymes that are involved in the energetic metabolism of cancer cells, such as lactate dehydrogenase (LDH), hexokinase II (HK-II), and 6-phosphofructo-1-kinase (PFK-1) [45], may compromise cellular bioenergetics, leading to the loss of membrane integrity, the loss of recovery capacity, and ultimately cell death as apoptosis/necrosis [46]. Tumor necrosis was reported previously in Walker-256 cells in tumor-bearing rats that were treated with RuC (10 mg/kg, i.p.)…”