In vitro and in vivo anti-proliferative activity and ultrastructure investigations of a copper(II) complex toward human lung cancer cell NCI-H460

In Vitro and In Vivo Relevant Antineoplastic Activity of Platinum(II) Complexes toward Triple-Negative MDA-MB-231 Breast Cancer Cell Line

“…In our previous paper [ 24 ], we showed the synthesis, physicochemical characterizations, and general biological activity of complex ( 3 ) and ( 4 ); in this work, we first investigated the potential anticancer activity these platinum(II) complexes and compared their in vitro cytotoxicity with CDDP in a panel of five cell lines derived from different human cancers. Similar results were observed for complexes containing Cu(II) and Pt(II), as previously reported by us [ 22 , 23 , 24 ]. We also showed the striking difference in cytotoxicity of complex ( 4 ) in contrast to CDDP, the chemotherapeutic reference (IC 50 8.1 ± 1.1 µM vs. 63.1 ± 1.2 µM), which was at least eightfold lower for the MDA-MB-231 cancer cell line.…”

“…The cells were washed three times with PBS and post-fixed for 20 min in a 1:1 solution of osmium tetroxide (1%) and potassium ferricyanide (0.8%). The samples were then prepared for SEM and TEM following routine procedures, as reported previously [ 22 ].…”

“…Groups of female BALB/c nude mice (six mice per group) were subcutaneously inoculated with 3 × 10 6 MDA-MB-231 cells in a volume of 50 μL of PBS in the back of the animals. This experiment was performed according to methodology described by Maciel et al [ 22 ]. Briefly, BALB/c nude mice bearing tumor nodules (±3 mm) were divided into three groups of six animals.…”

“…Our group has been evaluating the cytotoxic activities of a series of coordination compounds containing different metal ions both in vitro and in vivo [ 20 , 21 , 22 , 23 , 24 ]. We previously showed the synthesis, characterization, and cytotoxic activity of four complexes containing platinum(II) as a metallic coordinating center ( Scheme 1 ), where treatment against U937 cell line with complex ( 3 ) [Pt(HL3)Cl]·H 2 O could induce the activation of both intrinsic and extrinsic apoptotic cascades, as well as perturbations in cell cycle and dysfunction of mitochondrial membrane potential [ 24 ].…”

Induction of Redox-Mediated Cell Death in ER-Positive and ER-Negative Breast Cancer Cells by a Copper(II)-Phenolate Complex: An In Vitro and In Silico Study

“…Aiming at these desired pharmacodynamic profiles, diimines, tetradentate ligands and substituted derivatives as ligands are currently attractive in the discovery of metal-based drugs for different cancers [ 25 , 26 ]. These coordinated or transition metal complexes have been found to be potent as cell cycle inhibitors [ 27 , 28 , 29 ], DNA topoisomerase inhibitors [ 30 , 31 ], pro- and anti-apoptotic protein modulators (p53, Bax and Bcl-2) [ 32 , 33 , 34 ], etc. Particularly, these metal complexes bring about cancer cell death through inhibition of DNA synthesis [ 14 , 26 , 28 , 35 ], alteration of mitochondrial membrane potential and/or suppression of inhibitors of apoptosis [ 26 , 36 , 37 ].…”