A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis

Modulating mitochondrial activity to regulate cancer cell homeostatic recycling presents a promising approach to overcome tumor resistance. Consequently, there is an urgent need for novel mitochondria-targeting agents and innovative strategies. We have developed [((η5-Cp∗)Ir(rhod)]2+2PF6− (Ir-rhod),...

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Main Authors: Juanjuan Li, Guibin Gao, Wenrui Ouyang, Jinkun Huang, Hongxing Liu, Jin Li
Format: Article
Language:English
Published: Elsevier 2025-04-01
Series:Redox Biology
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Online Access:http://www.sciencedirect.com/science/article/pii/S2213231725000497
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author Juanjuan Li
Guibin Gao
Wenrui Ouyang
Jinkun Huang
Hongxing Liu
Jin Li
author_facet Juanjuan Li
Guibin Gao
Wenrui Ouyang
Jinkun Huang
Hongxing Liu
Jin Li
author_sort Juanjuan Li
collection DOAJ
description Modulating mitochondrial activity to regulate cancer cell homeostatic recycling presents a promising approach to overcome tumor resistance. Consequently, there is an urgent need for novel mitochondria-targeting agents and innovative strategies. We have developed [((η5-Cp∗)Ir(rhod)]2+2PF6− (Ir-rhod), a new mitochondria-targeted iridium complex that exhibits greater cytotoxicity towards A549R (cisplatin-resistant human lung cancer) cells compared to the ligand rhod. Ir-rhod's mitochondrial targeting ability stems from both rhodamine's inherent mitochondrial affinity and the complex's positive bivalent nature. The positively charged Ir-rhod enters cells and is drawn to mitochondria due to the high transmembrane potential in tumor cells. Notably, rhodamine enables real-time observation of Ir-rhod's dynamic distribution in vivo. Ir-rhod influences mitochondrial function, triggering tumor cell ferroptosis and apoptosis by modulating ACSL4 and GPX4. The targeting effect of Ir-rhod reduces its systemic toxicity in vivo, enhancing its biosafety profile. To our knowledge, Ir-rhod is an effective mitochondria-targeted Ir complex capable of inducing tumor cell death by disrupting mitochondrial function, offering a potent strategy to suppress cisplatin resistance in non-small cell lung cancer.
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issn 2213-2317
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publishDate 2025-04-01
publisher Elsevier
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series Redox Biology
spelling doaj-art-a394c3d6f6d2420ba652aba929df06072025-08-20T03:02:56ZengElsevierRedox Biology2213-23172025-04-018110353610.1016/j.redox.2025.103536A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosisJuanjuan Li0Guibin Gao1Wenrui Ouyang2Jinkun Huang3Hongxing Liu4Jin Li5Department of Urology, Guangzhou Institute of Urology, Guangdong Key Laboratory of Urology, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong, 510230, ChinaGuangdong Provincial Key Laboratory of Allergy & Immunology the Second Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong, 510230, ChinaDepartment of Urology, Guangzhou Institute of Urology, Guangdong Key Laboratory of Urology, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong, 510230, ChinaDepartment of Urology, Guangzhou Institute of Urology, Guangdong Key Laboratory of Urology, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong, 510230, ChinaDepartment of Urology, Guangzhou Institute of Urology, Guangdong Key Laboratory of Urology, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou Medical University, Guangzhou, Guangdong, 510230, China; Corresponding author.Department of Oncology, The Key Laboratory of Advanced Interdisciplinary Studies, The State Key Laboratory of Respiratory Disease, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, Guangdong, 510163, China; Corresponding author.Modulating mitochondrial activity to regulate cancer cell homeostatic recycling presents a promising approach to overcome tumor resistance. Consequently, there is an urgent need for novel mitochondria-targeting agents and innovative strategies. We have developed [((η5-Cp∗)Ir(rhod)]2+2PF6− (Ir-rhod), a new mitochondria-targeted iridium complex that exhibits greater cytotoxicity towards A549R (cisplatin-resistant human lung cancer) cells compared to the ligand rhod. Ir-rhod's mitochondrial targeting ability stems from both rhodamine's inherent mitochondrial affinity and the complex's positive bivalent nature. The positively charged Ir-rhod enters cells and is drawn to mitochondria due to the high transmembrane potential in tumor cells. Notably, rhodamine enables real-time observation of Ir-rhod's dynamic distribution in vivo. Ir-rhod influences mitochondrial function, triggering tumor cell ferroptosis and apoptosis by modulating ACSL4 and GPX4. The targeting effect of Ir-rhod reduces its systemic toxicity in vivo, enhancing its biosafety profile. To our knowledge, Ir-rhod is an effective mitochondria-targeted Ir complex capable of inducing tumor cell death by disrupting mitochondrial function, offering a potent strategy to suppress cisplatin resistance in non-small cell lung cancer.http://www.sciencedirect.com/science/article/pii/S2213231725000497Mitochondria-targetedIridium complexFerroptosisMitochondrial functionCisplatin-resistant non-small cell lung cancer
spellingShingle Juanjuan Li
Guibin Gao
Wenrui Ouyang
Jinkun Huang
Hongxing Liu
Jin Li
A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
Redox Biology
Mitochondria-targeted
Iridium complex
Ferroptosis
Mitochondrial function
Cisplatin-resistant non-small cell lung cancer
title A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
title_full A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
title_fullStr A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
title_full_unstemmed A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
title_short A rhodamine-coordinated iridium complex to overcome cisplatin-resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
title_sort rhodamine coordinated iridium complex to overcome cisplatin resistant cancer via regulating mitochondrial function triggered apoptosis and ferroptosis
topic Mitochondria-targeted
Iridium complex
Ferroptosis
Mitochondrial function
Cisplatin-resistant non-small cell lung cancer
url http://www.sciencedirect.com/science/article/pii/S2213231725000497
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