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.

Graphic abstract

中文翻译：

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以胍为配体的线粒体靶向Re（I）配合物及其抗癌活性

摘要

线粒体作为细胞的“动力源”，保持能量稳态，通过氧化磷酸化合成ATP，生成ROS信号分子，并调节细胞凋亡。在此，已经合成并表征了三种带有胍鎓衍生物的Re（I）配合物。所有这些复合物在HepG2，HeLa，MCF-7和A549癌细胞中均显示中等的抗癌活性。机制研究表明，复合物3 [Re（CO）3（L）（Im）]（PF ₆）₂可以选择性地定位于线粒体中，并通过与线粒体相关的途径诱导癌细胞死亡。另外，复合物3可以有效地抑制细胞迁移，细胞侵袭和集落形成的能力。

图形摘要