Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma

Summary: Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, and it is associated with a poor prognosis due to the lack of effective targeted therapies. Artemisinin (ARS), a widely used antimalarial drug, has demonstrated anti-tumor effects in several types of cancer, in...

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Main Authors: Minyue Xie, Xiang Gu, Zheng Zhao, Yu Hua, Qianru Wu, Yizhen Tang, Ai Zhuang, Shengfang Ge, Renbing Jia, Jie Yu, Jing Ruan, Xianqun Fan
Format: Article
Language:English
Published: Elsevier 2025-08-01
Series:iScience
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Online Access:http://www.sciencedirect.com/science/article/pii/S2589004225012337
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author Minyue Xie
Xiang Gu
Zheng Zhao
Yu Hua
Qianru Wu
Yizhen Tang
Ai Zhuang
Shengfang Ge
Renbing Jia
Jie Yu
Jing Ruan
Xianqun Fan
author_facet Minyue Xie
Xiang Gu
Zheng Zhao
Yu Hua
Qianru Wu
Yizhen Tang
Ai Zhuang
Shengfang Ge
Renbing Jia
Jie Yu
Jing Ruan
Xianqun Fan
author_sort Minyue Xie
collection DOAJ
description Summary: Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, and it is associated with a poor prognosis due to the lack of effective targeted therapies. Artemisinin (ARS), a widely used antimalarial drug, has demonstrated anti-tumor effects in several types of cancer, including UM. However, these effects are primarily observed at high concentrations, which restricts its broader use. Our study reveals mitochondrial uncoupler agents as synergistic partners with DHA in treating UM, both in vitro and in vivo. Specifically, the combination of DHA and CCCP, a representative mitochondrial uncoupler, induced endoplasmic reticulum (ER) stress by enhancing the binding of ATF4 and CHOP to the SESN2 promoter region. This ER stress subsequently activated autophagic cell death, augmenting UM cell eradication. Our findings suggest that combining DHA with mitochondrial protonophore uncouplers inhibits UM proliferation, underscoring the therapeutic promise of this approach for UM treatment.
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institution Kabale University
issn 2589-0042
language English
publishDate 2025-08-01
publisher Elsevier
record_format Article
series iScience
spelling doaj-art-6975c7ed628a41299610dddb9b7c5a412025-08-20T03:29:10ZengElsevieriScience2589-00422025-08-0128811297210.1016/j.isci.2025.112972Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanomaMinyue Xie0Xiang Gu1Zheng Zhao2Yu Hua3Qianru Wu4Yizhen Tang5Ai Zhuang6Shengfang Ge7Renbing Jia8Jie Yu9Jing Ruan10Xianqun Fan11Beijing Tongren Eye Center, Beijing Tongren Hospital, Capital Medical University, Beijing, China; Department of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaRenmin University of China, Beijing, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaBeijing Tongren Eye Center, Beijing Tongren Hospital, Capital Medical University, Beijing, ChinaBeijing Tongren Eye Center, Beijing Tongren Hospital, Capital Medical University, Beijing, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, ChinaDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, China; Corresponding authorDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, China; Corresponding authorDepartment of Ophthalmology, Ninth People’s Hospital, Shanghai JiaoTong University School of Medicine, Shanghai, China; Shanghai Key Laboratory of Orbital Diseases and Ocular Oncology, Shanghai, China; Corresponding authorSummary: Uveal melanoma (UM) is the most common primary intraocular malignancy in adults, and it is associated with a poor prognosis due to the lack of effective targeted therapies. Artemisinin (ARS), a widely used antimalarial drug, has demonstrated anti-tumor effects in several types of cancer, including UM. However, these effects are primarily observed at high concentrations, which restricts its broader use. Our study reveals mitochondrial uncoupler agents as synergistic partners with DHA in treating UM, both in vitro and in vivo. Specifically, the combination of DHA and CCCP, a representative mitochondrial uncoupler, induced endoplasmic reticulum (ER) stress by enhancing the binding of ATF4 and CHOP to the SESN2 promoter region. This ER stress subsequently activated autophagic cell death, augmenting UM cell eradication. Our findings suggest that combining DHA with mitochondrial protonophore uncouplers inhibits UM proliferation, underscoring the therapeutic promise of this approach for UM treatment.http://www.sciencedirect.com/science/article/pii/S2589004225012337BiochemistryCell biology
spellingShingle Minyue Xie
Xiang Gu
Zheng Zhao
Yu Hua
Qianru Wu
Yizhen Tang
Ai Zhuang
Shengfang Ge
Renbing Jia
Jie Yu
Jing Ruan
Xianqun Fan
Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
iScience
Biochemistry
Cell biology
title Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
title_full Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
title_fullStr Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
title_full_unstemmed Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
title_short Artemisinin synergizes with CCCP in autophagic cell death induction via ER stress in uveal melanoma
title_sort artemisinin synergizes with cccp in autophagic cell death induction via er stress in uveal melanoma
topic Biochemistry
Cell biology
url http://www.sciencedirect.com/science/article/pii/S2589004225012337
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