Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1

Ulcerative colitis (UC) is characterized by increased cell death in intestinal epithelial cell (IEC), which compromises gut barrier function and activates inflammation. Aberrant mitochondrial dynamics have been implicated in various forms of cell death, but it is currently unclear if they play a rol...

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Main Authors: Zhiming Ye, Mingxia Deng, Yang Yang, Yuanming Song, Liangkun Weng, Wanchen Qi, Ping Ding, Yihang Huang, Can Yu, Yan Wang, Yixing Wu, Yan Zhang, Shaoying Yuan, Wenkai Nie, Luyong Zhang, Cheng Zeng
Format: Article
Language:English
Published: Elsevier 2024-12-01
Series:Pharmacological Research
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Online Access:http://www.sciencedirect.com/science/article/pii/S1043661824004833
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author Zhiming Ye
Mingxia Deng
Yang Yang
Yuanming Song
Liangkun Weng
Wanchen Qi
Ping Ding
Yihang Huang
Can Yu
Yan Wang
Yixing Wu
Yan Zhang
Shaoying Yuan
Wenkai Nie
Luyong Zhang
Cheng Zeng
author_facet Zhiming Ye
Mingxia Deng
Yang Yang
Yuanming Song
Liangkun Weng
Wanchen Qi
Ping Ding
Yihang Huang
Can Yu
Yan Wang
Yixing Wu
Yan Zhang
Shaoying Yuan
Wenkai Nie
Luyong Zhang
Cheng Zeng
author_sort Zhiming Ye
collection DOAJ
description Ulcerative colitis (UC) is characterized by increased cell death in intestinal epithelial cell (IEC), which compromises gut barrier function and activates inflammation. Aberrant mitochondrial dynamics have been implicated in various forms of cell death, but it is currently unclear if they play a role in IEC death and colitis pathogenesis. This study aims to investigate the contribution of aberrant mitochondrial dynamics to colitis progression using cellular models, animal models, and clinical samples. The results revealed that IEC in mice with Dextran sulfate sodium salt (DSS)-induced colitis exhibited dynamin-related protein 1 (Drp1)-mediated mitochondrial fission and Z-DNA binding protein 1 (ZBP1)-dependent PANoptosis, which is a combination of apoptosis, necroptosis, and pyroptosis. However, these processes and the pathogenesis of DSS-induced colitis were significantly attenuated in IEC-specific Drp1 heterozygous knockout mice. Importantly, ZBP1-PANoptosis and Drp1-mediated mitochondrial fission were observed in IEC of UC patients, exhibiting a positive correlation with disease severity. Mechanistically, hyperactivated mitochondrial fission induced mitochondrial reactive oxygen species production leading to PANoptosis through ZBP1 sulfenylation at Cys327 independently of its Zα domain. Saquinavir, an FDA-approved drug identified through in-silico screening alongside in vivo and in vitro experiments, inhibits mitochondrial fission thereby enhancing therapeutic efficacy in mice with colitis.
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spelling doaj-art-a86e01045dd64b42b96d8f1a4220b16d2025-08-20T01:57:55ZengElsevierPharmacological Research1096-11862024-12-0121010753810.1016/j.phrs.2024.107538Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1Zhiming Ye0Mingxia Deng1Yang Yang2Yuanming Song3Liangkun Weng4Wanchen Qi5Ping Ding6Yihang Huang7Can Yu8Yan Wang9Yixing Wu10Yan Zhang11Shaoying Yuan12Wenkai Nie13Luyong Zhang14Cheng Zeng15Center for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaThe Guangzhou Laboratory, Guangzhou 510000, ChinaDepartment of Pharmacy, Zhuhai People’s Hospital (Zhuhai hospital affiliated with Jinan University), Zhuhai 519000, China; School of Pharmacy, Faculty of Medicine, Macau University of Science and Technology, MacaoCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaDepartment of Pharmacy, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou 519000, ChinaCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Nursing, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Nursing, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Nursing, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCollege of Pharmacy, Guangdong Pharmaceutical University, Guangzhou 510006, ChinaCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, China; Jiangsu Key Laboratory of Drug Screening, China Pharmaceutical University, Nanjing 210009, ChinaCenter for Drug Research and Development, Guangdong Pharmaceutical University, Guangzhou 510006, China; Key specialty of Clinical Pharmacy, The first Affiliated Hospital of Guangdong Pharmaceutical University, Guangzhou 510699, China; Correspondence to: Center for Drug Research and Development, Guangdong Pharmaceutical University, 280 East Huan Road, Panyu District, Guangzhou City, Guangdong Province 510006, China.Ulcerative colitis (UC) is characterized by increased cell death in intestinal epithelial cell (IEC), which compromises gut barrier function and activates inflammation. Aberrant mitochondrial dynamics have been implicated in various forms of cell death, but it is currently unclear if they play a role in IEC death and colitis pathogenesis. This study aims to investigate the contribution of aberrant mitochondrial dynamics to colitis progression using cellular models, animal models, and clinical samples. The results revealed that IEC in mice with Dextran sulfate sodium salt (DSS)-induced colitis exhibited dynamin-related protein 1 (Drp1)-mediated mitochondrial fission and Z-DNA binding protein 1 (ZBP1)-dependent PANoptosis, which is a combination of apoptosis, necroptosis, and pyroptosis. However, these processes and the pathogenesis of DSS-induced colitis were significantly attenuated in IEC-specific Drp1 heterozygous knockout mice. Importantly, ZBP1-PANoptosis and Drp1-mediated mitochondrial fission were observed in IEC of UC patients, exhibiting a positive correlation with disease severity. Mechanistically, hyperactivated mitochondrial fission induced mitochondrial reactive oxygen species production leading to PANoptosis through ZBP1 sulfenylation at Cys327 independently of its Zα domain. Saquinavir, an FDA-approved drug identified through in-silico screening alongside in vivo and in vitro experiments, inhibits mitochondrial fission thereby enhancing therapeutic efficacy in mice with colitis.http://www.sciencedirect.com/science/article/pii/S1043661824004833Ulcerative colitisMitochondrial fissionDrp1PANoptosisZBP1Saquinavir
spellingShingle Zhiming Ye
Mingxia Deng
Yang Yang
Yuanming Song
Liangkun Weng
Wanchen Qi
Ping Ding
Yihang Huang
Can Yu
Yan Wang
Yixing Wu
Yan Zhang
Shaoying Yuan
Wenkai Nie
Luyong Zhang
Cheng Zeng
Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
Pharmacological Research
Ulcerative colitis
Mitochondrial fission
Drp1
PANoptosis
ZBP1
Saquinavir
title Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
title_full Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
title_fullStr Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
title_full_unstemmed Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
title_short Epithelial mitochondrial fission-mediated PANoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through Drp1
title_sort epithelial mitochondrial fission mediated panoptosis is crucial for ulcerative colitis and its inhibition by saquinavir through drp1
topic Ulcerative colitis
Mitochondrial fission
Drp1
PANoptosis
ZBP1
Saquinavir
url http://www.sciencedirect.com/science/article/pii/S1043661824004833
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