Imaging Nuclei of MDA-MB-231 Breast Cancer Cells by Chiral Ruthenium(II) Complex Coordinated by 2-(4-Phenyacetylenephenyl)-1H-imidazo[4,5f][1,10]phenanthroline

Abstract

A pair of chiral ruthenium(II) complexes, Λ- and Δ-[Ru(bpy)2(p-BEPIP)](ClO4)2 [Λ- and Δ-RM0627; bpy = 2,2-bipyridine; p-BEPIP = 2-(4-phenyacetylenephenyl)-1H-imidazo[4,5f][1,10]phenanthroline], were prepared using the Sonogashira coupling reaction under microwave irradiation. The study shows that Λ-RM0627 emitted strong phosphorescence in the range 500-700 nm with a maximum at 594 nm when excited at 365 nm (the Stokes shift is about 227 nm), which was mainly located in the cell nucleus with red phosphorescence. Further studies using real-time phosphorescence observation confirmed that Λ-RM0627 can be taken up quickly by MDA-MB-231 cells and enriched in the nucleus. The in vitro and in vivo toxicities of Λ-RM0627 were also evaluated, and it was found that Λ-RM0627 slightly inhibited the growth of MDA-MB-231 breast cancer cells and HaCaT normal human epidermal cells and had little influence on the development of Zebrafish embryos at low concentration. In conclusion, the levoisomer of chiral ruthenium complexes can act as a potential phosphorescent probe that targets nuclei of living cells with low toxicity.

Cytotoxicity and anti-tumor effects of new ruthenium complexes on triple negative breast cancer cells

“…To give few examples, co-treatment cells with RuPOP and TRAIL effectively triggered apoptosis through the activation of caspases-3/-8/-9 and cleaved PARP in MDA-MB-231 cells at concentrations as low as 2μM [ 40 ]. In contrast, Zeng and co-workers [ 41 ] found that 40μM of Λ-RM0627 exhibited little apoptosis inducing effect on MDA-MB-231 cells, with only 6.2% cells in the late stage and 21.8% cells in the early stage of apoptosis.…”

Enantioselective cellular localisation of europium(iii) coordination complexes

“…The two enantiomers of certain chiral ruthenium( ii ) complexes exhibited slightly different localisation patterns with the Δ -enantiomer appearing in the cytosol, while the Λ -enantiomer seemed to concentrate around the nucleus of HepG2 cells (human liver cancer cells) and MDA-MB-231 breast cancer cells. 34 , 35 Toxicity tests with these cationic complexes showed about 60–70% cell survival at 80 μM dose, after 24 h.…”

The development of anticancer ruthenium(ii) complexes: from single molecule compounds to nanomaterials

“…Their study showed that the complex Λ - 11 , mainly located in the cell nucleus, slightly inhibited the growth of MDAMB-231 cancer cells. 198 However, Δ - 11 was mainly enriched in the cytoplasm and produced no significant cytotoxicity in MDAMB-231 cells. These results demonstrated that the ligands can affect the anticancer efficacy of Ru(II) complexes by affecting their uptake and intracellular localization.…”