Journal
JOURNAL OF INORGANIC BIOCHEMISTRY
Volume 216, Issue -, Pages -Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/j.jinorgbio.2020.111339
Keywords
Chiral complexes; Ruthenium; Fluorescent probes; AIE; Anticancer
Funding
- National Natural Science Foundation of China [21401002]
- Natural Science Foundation of Anhui Province, China [1508085QB37]
- Major Science and Technology Project of Anhui Province [17030701023]
- Australian Research Council [DP170103477]
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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.
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.
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