Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization

Abstract Vascular restenosis is a serious clinical issue initiated and aggravated by macrophage inflammation, with no effective treatments available, in cardiovascular and autoimmune diseases. However, the untapped mechanisms and new targets that can regulate macrophage polarization and vascular res...

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Main Authors: Jinlin Miao, Yule Yong, Zhaohui Zheng, Kui Zhang, Wei Li, Jiayi Liu, Siyi Zhou, Juan‐juan Qin, Haoyang Sun, Yatao Wang, Xianghui Fu, Xing Luo, Siyu Chen, Zhi‐Gang She, Jingjing Cai, Ping Zhu
Format: Article
Language:English
Published: Wiley 2025-05-01
Series:Advanced Science
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Online Access:https://doi.org/10.1002/advs.202408992
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author Jinlin Miao
Yule Yong
Zhaohui Zheng
Kui Zhang
Wei Li
Jiayi Liu
Siyi Zhou
Juan‐juan Qin
Haoyang Sun
Yatao Wang
Xianghui Fu
Xing Luo
Siyu Chen
Zhi‐Gang She
Jingjing Cai
Ping Zhu
author_facet Jinlin Miao
Yule Yong
Zhaohui Zheng
Kui Zhang
Wei Li
Jiayi Liu
Siyi Zhou
Juan‐juan Qin
Haoyang Sun
Yatao Wang
Xianghui Fu
Xing Luo
Siyu Chen
Zhi‐Gang She
Jingjing Cai
Ping Zhu
author_sort Jinlin Miao
collection DOAJ
description Abstract Vascular restenosis is a serious clinical issue initiated and aggravated by macrophage inflammation, with no effective treatments available, in cardiovascular and autoimmune diseases. However, the untapped mechanisms and new targets that can regulate macrophage polarization and vascular restenosis remain elusive. The research identifies interferon regulatory factor 4 (IRF4) expression as crucial in macrophage polarization during arterial restenosis. Myeloid‐specific Irf4 deficiency and overexpression experiments showed that IRF4 promoted M2 macrophage polarization, inhibited M1 macrophage transitions, and disrupted the interaction between macrophages and vascular smooth muscle cells to reduce neointimal hyperplasia by directly upregulating krüppel like factor 4 (KLF4) expression. Artesunate, an FDA‐approved drug, is screened as a potent activator of IRF4 expression in M2 polarization, and its treatment attenuated arterial restenosis in rodents and non‐human primates. The findings reveal a significant protective role of IRF4 in the development of neointimal hyperplasia by regulating macrophage polarization, and artesunate may be proposed as a novel therapy for vascular restenosis.
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issn 2198-3844
language English
publishDate 2025-05-01
publisher Wiley
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spelling doaj-art-200fcee4f9f74260a08a38f006563f322025-08-20T03:13:30ZengWileyAdvanced Science2198-38442025-05-011219n/an/a10.1002/advs.202408992Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage PolarizationJinlin Miao0Yule Yong1Zhaohui Zheng2Kui Zhang3Wei Li4Jiayi Liu5Siyi Zhou6Juan‐juan Qin7Haoyang Sun8Yatao Wang9Xianghui Fu10Xing Luo11Siyu Chen12Zhi‐Gang She13Jingjing Cai14Ping Zhu15Department of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Cardiology Renmin Hospital Wuhan University Wuhan 430060 ChinaDepartment of Cardiology Renmin Hospital Wuhan University Wuhan 430060 ChinaInstitute of Model Animal Wuhan University Wuhan 430071 ChinaDepartment of Geriatrics Zhongnan Hospital Wuhan University Wuhan 430070 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaDepartment of Cardiology Renmin Hospital Wuhan University Wuhan 430060 ChinaDepartment of Cardiology The Third Xiangya Hospital Central South University Changsha 410013 ChinaDepartment of Clinical Immunology of Xijing Hospital and Department of Cell Biology of National Translational Science Center for Molecular Medicine Fourth Military Medical University Xi'an 710032 ChinaAbstract Vascular restenosis is a serious clinical issue initiated and aggravated by macrophage inflammation, with no effective treatments available, in cardiovascular and autoimmune diseases. However, the untapped mechanisms and new targets that can regulate macrophage polarization and vascular restenosis remain elusive. The research identifies interferon regulatory factor 4 (IRF4) expression as crucial in macrophage polarization during arterial restenosis. Myeloid‐specific Irf4 deficiency and overexpression experiments showed that IRF4 promoted M2 macrophage polarization, inhibited M1 macrophage transitions, and disrupted the interaction between macrophages and vascular smooth muscle cells to reduce neointimal hyperplasia by directly upregulating krüppel like factor 4 (KLF4) expression. Artesunate, an FDA‐approved drug, is screened as a potent activator of IRF4 expression in M2 polarization, and its treatment attenuated arterial restenosis in rodents and non‐human primates. The findings reveal a significant protective role of IRF4 in the development of neointimal hyperplasia by regulating macrophage polarization, and artesunate may be proposed as a novel therapy for vascular restenosis.https://doi.org/10.1002/advs.202408992artesunateIRF4macrophagesneointimal hyperplasiarestenosis
spellingShingle Jinlin Miao
Yule Yong
Zhaohui Zheng
Kui Zhang
Wei Li
Jiayi Liu
Siyi Zhou
Juan‐juan Qin
Haoyang Sun
Yatao Wang
Xianghui Fu
Xing Luo
Siyu Chen
Zhi‐Gang She
Jingjing Cai
Ping Zhu
Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
Advanced Science
artesunate
IRF4
macrophages
neointimal hyperplasia
restenosis
title Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
title_full Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
title_fullStr Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
title_full_unstemmed Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
title_short Artesunate Inhibits Neointimal Hyperplasia by Promoting IRF4 Associated Macrophage Polarization
title_sort artesunate inhibits neointimal hyperplasia by promoting irf4 associated macrophage polarization
topic artesunate
IRF4
macrophages
neointimal hyperplasia
restenosis
url https://doi.org/10.1002/advs.202408992
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