Abstract
Three iridium(III) complexes ([Ir(Hppy)2(L)](PF6) (Hppy = 2-phenylpyridine, L = 5-nitrophenanthroline, NP), 1; 5-nitro-6-amino-phenanthroline (NAP), 2; and 5,6-diamino-phenanthroline (DAP) 3 were synthesized and characterized. The cytotoxicities of Ir(III) complexes 1–3 against cancer cell lines SGC-7901, A549, HeLa, Eca-109, HepG2, BEL-7402, and normal NIH 3T3 cells were investigated using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazoliumbromide (MTT) method. The results showed that the three iridium(III) complexes had moderate in vitro anti-tumor activity toward SGC-7901 cells with IC50 values of 3.6 ± 0.1 µM for 1, 14.1 ± 0.5 µM for 2, and 11.1 ± 1.3 µM for 3. Further studies showed that 1–3 induce cell apoptosis/death through DNA damage, cell cycle arrest at the S or G0/G1 phase, ROS elevation, increased levels of Ca2+, high mitochondrial membrane depolarization, and cellular ATP depletion. Transwell and Colony-Forming assays revealed that complexes 1–3 can also effectively inhibit the metastasis and proliferation of tumor cells. These results demonstrate that 1–3 induce apoptosis in SGC-7901 cells through ROS-mediated mitochondrial damage and DNA damage pathways, as well as by inhibiting cell invasion, thereby exerting anti-tumor cell proliferation activity in vitro.
Highlights
Cancer has long been a global problem
1,10-phenanthroline, palladium carbon and hydroxylamine hydrochloride were purchased from thehydrazine reagent, and hydroxylamine hydrochloride were purchased from the
The BEL-7402 and SGC-7901 cell lines were cultured in Roswell Park Memorial Institute Medium (RPMI-1640); and A549, Eca-109, HepG2, and NIH 3T3 cells were grown in Dulbecco’s Modified Eagle’s Medium (DMEM), including 10% fetal bovine serum (FBS), 100 units mL−1 penicillin/streptomycin mixture, and 2.0 g/L of NaHCO3
Summary
Cancer has long been a global problem. Cancer metastasis and drug resistance are two main causes of treatment failure, with the mortality rate approaching 90% [1]. –NO group was selected as a ligand for this modified for the purposes of drug development [14,15] Based on these studies and rare reports, study of iridium metal complexes. Cyclecancer arrestcells at the phase,cella exhibited potent cytotoxicity toward breast anduptake, colon Complexes in double-strand breaks, apoptosis induction, of ROS, and high mitochondrial with potent anti-tumor activity and to illuminate the pro-apoptotic mechanisms, we report the membrane depolarization [18]. SGC-7901 cells, subcellular localization of the complexes, activation of caspases, and mitochondrial apoptosis, and migration are evaluated.
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