Photocytotoxicity and G‐quadruplex DNA interaction of water‐soluble gallium(III) tris(N‐methyl‐4‐pyridyl)corrole complex

Abstract

A water-soluble cationic gallium corrole, 5,10,15-tris(N-methyl-4-pyridyl)corrolatogallium(III) (3), was prepared and characterized. The photocytotoxicity of 3 was investigated using Hep G2 cancer cell line. Upon treatment with corrole 3 and irradiation, fragmentation of tumor cell nuclei was observed, which led to apoptosis. Flow cytometric analysis clearly showed the efficient induction of apoptotic cell death, and corrole 3 exhibited high photocytotoxicity towards Hep G2 cancer cells (IC 50 = 60 nM). Furthermore, the binding behavior of corrole 3 with c-MYC G-quadruplex DNA, a potent target for antitumor drugs, was investigated using spectroscopic methods and molecular docking simulation.

Water-soluble Manganese and Iron Mesotetrakis(carboxyl)porphyrin: DNA Binding, Oxidative Cleavage, and Cytotoxic Activities

“…Interestingly, the cytotoxicity of 2-Mn to Hep G2 cell lines was sharply increased under light irradiation. These observations suggest the cytotoxicity of metal meso -tetrakis (carboxyl) porphyrins depend largely not only on the central metals, but also the type of tumor cell lines [ 58 ]. The phototoxicity of m THPC was also obtained under the same experimental conditions, as a positive control.…”

“…Cells receiving either treatment alone showed no such phenotype. This indicates that light at specific wavelength scan promote 2-Mn cytotoxicity to cancer cells [ 58 ]. Such morphological changes are often observed in apoptotic and necrosis cells, and thus 2-Mn may induce cell death in Hep G2 cells through an apoptotic/necrosis pathway.…”

“…This suggests the cells were resistant to 2-Mn treatment without irradiation. After receiving 2-Mn and light, however, not only did massive bright spots appear (a typical apoptotic feature) and the density of the cells be reduced, but also morphological changes of the nucleus were also observed [ 58 ], such as condensed chromatin and fragmented nuclei (red arrow). Cells receiving either treatment alone showed no such phenotype.…”

Underlying mechanism of the photodynamic activity of hematoporphyrin‑induced apoptosis in U87 glioma cells

“…The inhibition of cell growth by drugs is generally caused by induction of apoptosis or cell cycle arrest (23). The photodynamic activity of hematoporphyrin was found to inhibit cell growth via induction of cell apoptosis at the later stage.…”

Methyl Benzoate Gallium(III) corrole complexes: DNA‐binding, Photocleavage Activity, Cytotoxicity on Tumor Cells

“…Recently, carboxylated gallium corrole was identified as effective cell‐permeable chemotherapeutic agent and can be used for tumor imaging . While cationic gallium pyridylcorrole is a potential photosensitizer of photodynamic therapy and a potent G‐quadruplex DNA stabilizers …”