FerriIridium: A Lysosome‐Targeting Iron(III)‐Activated Iridium(III) Prodrug for Chemotherapy in Gastric Cancer Cells

Abstract

Reported is the Fe III -activated lysosome-targeting prodrug FerriIridium for gastric cancer theranostics.I tc ontains ameta-imino catechol group that can selectively bond to, and be oxidized by,f ree Fe III inside the cell. Subsequent oxidative rearrangement releases Fe II and hydrolyses the amine bond under acidic conditions,f orming an aminobipyridyl Ir complex and 2-hydroxybenzoquinone.Thus,F e II catalyzesthe Fenton reaction, transforming hydrogen peroxide into hydroxyl radicals,t he benzoquinone compounds interfere with the respiratory chain, and conversion of the prodrug into the Ir complex leads to an increase in phosphorescence and toxicity. These properties,c ombined with the high Fe III content and acidity of cancer cells,m ake FerriIridium as elective and efficient theranostic agent (IC 50 = 9.22 mm for AGSc ells vs. > 200 mm for LO2 cells). FerriIridium is the first metal-based compound that has been developed for chemotherapyu sing Fe III to enhance both selectivity and potency.Supportinginformation and the ORCID identification number(s) for the author(s) of this article can be found under: https://doi.

A Mitochondrion‐Localized Two‐Photon Photosensitizer Generating Carbon Radicals Against Hypoxic Tumors

“…As expected, the fluorescence of DCF was only observed for Ir4 after two‐photon ( λ ex =730 nm) irradiation (Figure 3 C). As ROS generation by mitochondrial photosensitizers can readily cause mitochondrial membrane potential (MMP) loss, [29] change in MMP was assessed by JC‐1 staining. A549 cells treated with Ir4 demonstrated significant MMP reduction in comparison with the controls, while Ir1 – 3 showed no obvious change (Figure S30–S33).…”

Organometallic anti-tumor agents: targeting from biomolecules to dynamic bioprocesses

“…26(b)). 182 This non-luminescent complex can be oxidised by two equivalents of cellular labile Fe 3+ to form a Schiff base which is unstable in lysosomes and simultaneously releases Fe 2+ to perturb iron homeostasis. After acidic stimulation, the Schiff base was hydrolysed to form an aminobipyridyl complex and 2-hydroxybenzoquinone with obvious phosphorescence recovery, which endowed 3-27 with the ability to monitor cellular labile iron.…”

A Neutral Pyridine-Pyrazole-Based N^N*N^N Ligand as a Tetradentate Chromophore for Diverse Transition Metal Cations

“…Mono-and bis-cyclometalated transition metal complexes have been extensively studied in the past few decades. In particular, compounds with heavy transition metals, such as Pt(II) [1,2], Ir(III) [3,4] and Os(II) [5,6], are widely used in optoelectronics [7][8][9], bioimaging [10,11] and in anticancer therapy [12][13][14] due to their outstanding physical and chemical properties. However, lighter metal ions, such as Zn 2+ , Cu 2+ and Fe 2+ , cannot be complexed via cyclometalation, or only under difficult conditions.…”