Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults

Abstract The rapid deterioration and progression of hepatocellular carcinoma (HCC) is intimately associated with copper ion overload, and integrating the cuproptosis mechanism for the treatment of HCC presents a promising prospect. Nevertheless, cell death complexity renders efficient removal of all...

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Main Authors: Yingjie Zeng, Yuening Cao, Senmiao Ren, Chaozheng Zhang, Jianan Liu, Ke Liu, Yan Wang, Hongyu Chen, Fengjiao Zhou, Xiuli Yang, Xian Ge, Tingting Zhang, Tianbao Wang, Yao He, Defang Li, Chuantao Zhang, Jun Lu
Format: Article
Language:English
Published: Wiley 2025-08-01
Series:Advanced Science
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Online Access:https://doi.org/10.1002/advs.202501420
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author Yingjie Zeng
Yuening Cao
Senmiao Ren
Chaozheng Zhang
Jianan Liu
Ke Liu
Yan Wang
Hongyu Chen
Fengjiao Zhou
Xiuli Yang
Xian Ge
Tingting Zhang
Tianbao Wang
Yao He
Defang Li
Chuantao Zhang
Jun Lu
author_facet Yingjie Zeng
Yuening Cao
Senmiao Ren
Chaozheng Zhang
Jianan Liu
Ke Liu
Yan Wang
Hongyu Chen
Fengjiao Zhou
Xiuli Yang
Xian Ge
Tingting Zhang
Tianbao Wang
Yao He
Defang Li
Chuantao Zhang
Jun Lu
author_sort Yingjie Zeng
collection DOAJ
description Abstract The rapid deterioration and progression of hepatocellular carcinoma (HCC) is intimately associated with copper ion overload, and integrating the cuproptosis mechanism for the treatment of HCC presents a promising prospect. Nevertheless, cell death complexity renders efficient removal of all HCC cells insufficient solely relying on the cuproptosis pathway. Herein, the GSH‐responsive prodrug hybridization nanoassembly CA‐4S2@ES‐Cu is exploited, which targets the delivery of copper ions to mitochondria via Elesclomol, contributing to mitochondrial dysfunction and evoking cuproptosis. Simultaneously, CA‐4S2 depletes GSH to release CA‐4, disrupting microtubule function and suppressing HCC cell proliferation and angiogenesis, to realize a dual attack against copper ion‐mediated deterioration and metastasis of HCC. Furthermore, both in the HCC mouse model synergistically elicit oxidative stress to amplify the cuproptosis effect and release activated immunogenetic cell death to initiate a vigorous antitumor immune response in cascade assault modality. Conclusively, the multilevel synergistic assault penetrates the limitations of single therapy and implements a multidimensional targeted treatment for HCC.
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publisher Wiley
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series Advanced Science
spelling doaj-art-1dad7de46b2c42bb91333cb0dbd77cdb2025-08-20T04:01:15ZengWileyAdvanced Science2198-38442025-08-011229n/an/a10.1002/advs.202501420Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade AssaultsYingjie Zeng0Yuening Cao1Senmiao Ren2Chaozheng Zhang3Jianan Liu4Ke Liu5Yan Wang6Hongyu Chen7Fengjiao Zhou8Xiuli Yang9Xian Ge10Tingting Zhang11Tianbao Wang12Yao He13Defang Li14Chuantao Zhang15Jun Lu16State Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaDepartment of Respiratory Medicine Hospital of Chengdu University of Traditional Chinese Medicine Chengdu 610075 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaDepartment of Respiratory Medicine Hospital of Chengdu University of Traditional Chinese Medicine Chengdu 610075 ChinaDepartment of Respiratory Medicine Hospital of Chengdu University of Traditional Chinese Medicine Chengdu 610075 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaSichuan Clinical Research Center for Cancer Sichuan Cancer Hospital & Institute Sichuan Cancer Center Affiliated Cancer Hospital of University of Electronic Science and Technology of China Chengdu 610041 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaCollege of Pharmacy Hebei University of Chinese Medicine Shijiazhuang 050200 ChinaDepartment of Respiratory Medicine Hospital of Chengdu University of Traditional Chinese Medicine Chengdu 610075 ChinaState Key Laboratory of Southwestern Chinese Medicine Resources School of Pharmacy Chengdu University of Traditional Chinese Medicine Chengdu 611137 ChinaAbstract The rapid deterioration and progression of hepatocellular carcinoma (HCC) is intimately associated with copper ion overload, and integrating the cuproptosis mechanism for the treatment of HCC presents a promising prospect. Nevertheless, cell death complexity renders efficient removal of all HCC cells insufficient solely relying on the cuproptosis pathway. Herein, the GSH‐responsive prodrug hybridization nanoassembly CA‐4S2@ES‐Cu is exploited, which targets the delivery of copper ions to mitochondria via Elesclomol, contributing to mitochondrial dysfunction and evoking cuproptosis. Simultaneously, CA‐4S2 depletes GSH to release CA‐4, disrupting microtubule function and suppressing HCC cell proliferation and angiogenesis, to realize a dual attack against copper ion‐mediated deterioration and metastasis of HCC. Furthermore, both in the HCC mouse model synergistically elicit oxidative stress to amplify the cuproptosis effect and release activated immunogenetic cell death to initiate a vigorous antitumor immune response in cascade assault modality. Conclusively, the multilevel synergistic assault penetrates the limitations of single therapy and implements a multidimensional targeted treatment for HCC.https://doi.org/10.1002/advs.202501420cascade assaultscuproptosishepatocellular carcinomaoxidative stressprodrug hybridization nanoassembly
spellingShingle Yingjie Zeng
Yuening Cao
Senmiao Ren
Chaozheng Zhang
Jianan Liu
Ke Liu
Yan Wang
Hongyu Chen
Fengjiao Zhou
Xiuli Yang
Xian Ge
Tingting Zhang
Tianbao Wang
Yao He
Defang Li
Chuantao Zhang
Jun Lu
Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
Advanced Science
cascade assaults
cuproptosis
hepatocellular carcinoma
oxidative stress
prodrug hybridization nanoassembly
title Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
title_full Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
title_fullStr Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
title_full_unstemmed Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
title_short Responsive ROS‐Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults
title_sort responsive ros augmented prodrug hybridization nanoassemblies for multidimensionally synergitic treatment of hepatocellular carcinoma in cascade assaults
topic cascade assaults
cuproptosis
hepatocellular carcinoma
oxidative stress
prodrug hybridization nanoassembly
url https://doi.org/10.1002/advs.202501420
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