Abstract：
:PDT is a well-established therapeutic modality for many types of cancer. Photoluminescent cyclometalated iridium(III) complexes are one of the most commonly used classes of organometallic compounds with potential beneficial applications in bioimaging and as promising anticancer agents. In the present study, three new cyclometalated iridium(III) complexes (Ir1-Ir3) containing guanidinium ligands were found to exert excellent cytotoxic effects on different types of cancer cells upon light irradiation at 425 nm. Notably, Ir1 conferred almost no dark toxicity (IC50 > 100 μM) to HepG2 cells, but the value decreased by 387-fold to 0.36 μM following 10 min of light irradiation (425 nm). Further mechanistic investigation revealed that complex Ir1 could induce apoptosis via the activation of reactive oxygen species (ROS)-mediated mitochondrial signaling pathways in the presence or absence of light irradiation. In vivo studies demonstrated that Ir1 significantly inhibited tumor growth in HepG2 xenograft-bearing mice under light irradiation at 425 nm. Taken together, these findings indicate that designing PDT-based Ir(III) complexes may hold a great deal of promise for anticancer drug development.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Song XD,Chen BB,He SF,Pan NL,Liao JX,Chen JX,Wang GH,Sun Jdoi
10.1016/j.ejmech.2019.06.045subject
Has Abstractpub_date
2019-10-01 00:00:00pages
26-37eissn
0223-5234issn
1768-3254pii
S0223-5234(19)30572-0journal_volume
179pub_type
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