Issue 33, 2020

Dinuclear phosphorescent rhenium(i) complexes as potential anticancer and photodynamic therapy agents

Abstract

Chemotherapeutic agents that affect lysosomal functions represent a promising strategy for selective tumor therapy and overcoming drug resistance. In this work, two dinuclear phosphorescent rhenium(I) tricarbonyl complexes (DRe1 and DRe2) containing carboline derivatives have been synthesized, characterized and explored as potential chemotherapeutic and photodynamic therapy agents. The two dinuclear rhenium(I) complexes have good intrinsic phosphorescence properties and can label the lysosomes in cancer cells. Both dinuclear rhenium(I) complexes show potent anticancer activities toward several tested cancer cells. Moreover, they also have marked inhibitory activities against cisplatin-resistant human lung carcinoma cells (A549R), with complex DRe2 displaying 16-fold higher activity than cisplatin. Mechanism studies reveal that complex DRe2 can induce cancer cells to overproduce reactive oxygen species (ROS), including superoxide anion radicals, which leads to lysosomal membrane permeabilization (LMP) and subsequent cell apoptosis. Additionally, both DRe1 and DRe2 display significant phototoxicity under light (425 nm) irradiation in A549 cells, with phototoxicity index values of 60.8 and 41.8, respectively. Therefore, these two dinuclear organometallic rhenium(I) tricarbonyl complexes are potential anticancer agents for combined chemo-photodynamic therapy.

Graphical abstract: Dinuclear phosphorescent rhenium(i) complexes as potential anticancer and photodynamic therapy agents

Supplementary files

Article information

Article type
Paper
Submitted
09 Jul 2020
Accepted
04 Aug 2020
First published
05 Aug 2020

Dalton Trans., 2020,49, 11583-11590

Dinuclear phosphorescent rhenium(I) complexes as potential anticancer and photodynamic therapy agents

Z. Pan, D. Cai and L. He, Dalton Trans., 2020, 49, 11583 DOI: 10.1039/D0DT02424D

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