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. 2020 Dec;25(8):1107-1116.
doi: 10.1007/s00775-020-01827-7. Epub 2020 Oct 20.

Mitochondria-targeted Re(I) complexes bearing guanidinium as ligands and their anticancer activity

Shu-Fen He #  1   2 , Nan-Lian Pan #  1 , Bing-Bing Chen  1 , Jia-Xin Liao  1 , Min-Ying Huang  1 , Hai-Jun Qiu  1 , Dong-Chun Jiang  1 , Jun-Jie Wang  1 , Jia-Xi Chen  3 , Jing Sun  4
Affiliations

Mitochondria-targeted Re(I) complexes bearing guanidinium as ligands and their anticancer activity

Shu-Fen He et al. J Biol Inorg Chem. 2020 Dec.

Abstract

As the "powerhouse" of a cell, mitochondria maintain energy homeostasis, synthesize ATP via oxidative phosphorylation, generate ROS signaling molecules, and modulate cell apoptosis. Herein, three Re(I) complexes bearing guanidinium derivatives have been synthesized and characterized. All of these complexes exhibit moderate anticancer activity in HepG2, HeLa, MCF-7, and A549 cancer cells. Mechanism studies indicate that complex 3, [Re(CO)3(L)(Im)](PF6)2, can selectively localize in the mitochondria and induce cancer cell death through mitochondria-associated pathways. In addition, complex 3 can effectively depress the ability of cell migration, cell invasion, and colony formation.

Keywords: Apoptosis; Cytotoxicity; Mitochondria; Re(I) complex.

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