Chiral ruthenium polypyridyl complexes as mitochondria-targeted apoptosis inducers

Abstract

A series of chiral ruthenium polypyridyl complexes have been synthesized and evaluated for their in vitro anticancer activities. Λ-[Ru(bpy)2(o-tFMPIP)]Cl2·3H2O was identified as a novel complex that was able to induce mitochondria-mediated apoptosis in melanoma A375 cells through regulation of Bcl-2 family members and activation of caspases.

Preparation of Prunella vulgaris polysaccharide-zinc complex and its antiproliferative activity in HepG2 cells

“…Mitochondrial dysfunction could cause depletion of ΔΨm and the release of apoptogenic factors, thus triggering downstream apoptotic pathway (activation of caspase-3 and -9) [5,25,26]. Loss of ΔΨm is considered as an initial and irreversible step during apoptosis [5,20]. In this study, HepG2 cells treated with various concentrations of P1-Zn were stained with the mitochondrial-selective JC-1 dye and analyzed by flow cytometry.…”

“…Recently, many metal-based compounds, such as Pt, Ru and Au complexes, have been found to exhibit desirable anticancer activities and used in clinic worldwide for the treatment of various cancers [2,4,5]. However, the side effects, especially toxicity and drug resistance, limit the practical application of these drugs.…”

Polypyridyl Metal Complexes with Biological Activity

“…These derivatives have a [Ru(bpy) 2 (N-N)] 2+ structure in which the N-N is an extended phenanthroline ligand having a CF 3 substituent at different positions of the terminal phenyl group (Scheme 8). [29] The antiproliferative activity of this family of compounds depends on the position of the CF 3 group and is cell-line-specific. Furthermore, different enantiomers display different IC 50 values.…”

“…Its activity is comparable to or higher than that of cisplatin and falls in the 6-19 μm www.eurjic.org 2+ family of complexes investigated in ref. [29] range (cisplatin 7-36 μm) for the A375, HepG2, and SW620 cell lines.…”

Transferrin-functionalized nanographene oxide for delivery of platinum complexes to enhance cancer-cell selectivity and apoptosis-inducing efficacy

“…37,38 Different cells (2×10 4 cells/mL) were incubated in 96-well plates and cultivated, then different concentrations of Tf-NGO@Pt were added at different times. Subsequently, the cells was incubated with 20 mL PBS solution with MTT for 5 hours.…”