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Anti-metastasis and anti-proliferation effect of mitochondria-accumulating ruthenium(II) complexes via redox homeostasis disturbance and energy depletion by Lina Xie; Lili Wang; Ruilin Guan; Liangnian Ji; Hui Chao is a Chemistry article available to read on EtoBox.

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The antiproliferative activity of three cyclometalated Ru(II) complexes with the formula [Ru(bpy)L]PF, where bpy = 2,2'-bipyridine, Ru1: L1 = phenanthro[4,5-fgh]quinoxaline; Ru2: L2 = benzo[f]naphtho[2,1-h]quinoxaline; and Ru3: L3 = phenanthro[9,10-b]pyrazine, have been synthesized and characterized. The lipophilicity of the three Ru(II) complexes was modulated by the alteration of the planarity in the ligands of the complexes. With appropriate lipophilicity, Ru1-Ru3 exhibited mitochondrial accumulating property and cytotoxic activity against a spectrum of cancer cell lines. The underlying mechanism study indicated that these Ru(II) complexes can selectively accumulate in mitochondria and disrupt physiological processes, including the redox balance and energy generation in cancer cells. Elevation of iron content in triple-negative breast cancer (MDA-MB-231 cells) was observed after treatment with Ru(II) complexes, which may contribute to the production of reactive oxygen species (ROS) via Fenton reaction chemistry. Besides, the Ru(II) complexes decreased the intracellular glutathione (GSH) in cancer cells, leading to the failure in the cells to combat oxidative damage. Both of the

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Author

Lina Xie; Lili Wang; Ruilin Guan; Liangnian Ji; Hui Chao

Publisher

Elsevier BV

Published

2021

Language

EN

Field

Chemistry (Physical Sciences)