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

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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.

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Acknowledgments

This work was supported by the National Natural Science Foundation of China (21101034), the Science and Technology Plan of Guangdong Province (2016A020217020), the Scientific Research Project of Guangdong Provincial Bureau of Traditional Chinese Medicine (20182070), and “Group-type” special support project for Education Talents in University (4SG19045G, 4SG19053G and 4SG19057G).

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Correspondence to Jia-Xi Chen or Jing Sun.

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He, SF., Pan, NL., Chen, BB. et al. Mitochondria-targeted Re(I) complexes bearing guanidinium as ligands and their anticancer activity. J Biol Inorg Chem 25, 1107–1116 (2020). https://doi.org/10.1007/s00775-020-01827-7

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  • DOI: https://doi.org/10.1007/s00775-020-01827-7

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