Enantiomeric selectivity of ruthenium (II) chiral complexes with antitumor activity, in vitro and in vivo

Different enantiomers of chiral drugs show distinctive activities. Here, a pair of chiral ruthenium A-[Ru (phen)2(TPEPIP)]2+ (A-Ru), and A-[Ru(phen)2(TPEPIP)]2+ (A-Ru) (phen = 1,10-phenanthroline; TPEPIP = 2(4 '-(1,2,2-triphenylvinyl)-[1,1 '-biphenyl]-4-yl)-1H-imidazo[4,5-f][1,10]phenanthroline) compounds have been prepared and characterized. Both have aggregation-induced emission characteristics, although A-Ru exhibits much higher activity, towards duplex DNA extracted from SGC-7901 cancer cells. In vitro experiments demonstrate that both A-Ru and A-Ru can induce the apoptosis of tumor cells with A-Ru showing greater activity than A-Ru. A-Ru aggregates in the cell nucleus of SGC-7901 within 5 h which shows that nucleic acids may be the effective target of A-Ru. In vivo experiments with nude mice showed that A-Ru can inhibit the growth and proliferation of a tumor, in tumor-bearing mice as well as targeting the tumor site, as demonstrated by fluorescence. These results demonstrate the dual-function of A-Ru, which could be used for real-time visualization of a chemotherapeutic agent.

Automated summary

The chiral ruthenium compound A-Ru prepared in the study exhibits high activity against tumor cells, inducing apoptosis and effectively inhibiting tumor growth and proliferation in in vivo experiments.