Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells

Ferroptosis, a form of non-apoptotic cell death, is emerging as a promising strategy for cancer therapy. Artesunate (ART), an extract obtained from the traditional Chinese medicine Qinghaosu, has been shown to exhibit anti-cancer activity by inducing ferroptosis in cancer cells. While previous resea...

Full description

Saved in:
Bibliographic Details
Main Authors: Natsumi Ito, Ahmed Nabil, Koichiro Uto, Mitsuhiro Ebara
Format: Article
Language:English
Published: Taylor & Francis Group 2025-12-01
Series:Science and Technology of Advanced Materials
Subjects:
Online Access:https://www.tandfonline.com/doi/10.1080/14686996.2025.2482514
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850150465979809792
author Natsumi Ito
Ahmed Nabil
Koichiro Uto
Mitsuhiro Ebara
author_facet Natsumi Ito
Ahmed Nabil
Koichiro Uto
Mitsuhiro Ebara
author_sort Natsumi Ito
collection DOAJ
description Ferroptosis, a form of non-apoptotic cell death, is emerging as a promising strategy for cancer therapy. Artesunate (ART), an extract obtained from the traditional Chinese medicine Qinghaosu, has been shown to exhibit anti-cancer activity by inducing ferroptosis in cancer cells. While previous research has focused on incorporating ART monomer into drug delivery systems for enhanced cancer targeting, this study presents 2-methacryloyloxyethyl ART polymer (poly(ARTEMA)), a novel polymer synthesized from ART for the first time. Our goal was evaluation of poly(ARTEMA) anticancer potential on breast cancer cells. First, we synthesized ARTEMA using esterification followed by its polymerization using the reversible addition-fragmentation chain transfer (RAFT) polymerization method. We evaluated its mechanism of action, focusing on two key pathways: temperature-triggered singlet oxygen generation and ferrous ions (Fe2+) release, both of which contribute to ferroptosis. Our results demonstrate that poly(ARTEMA) selectively generates singlet oxygen and Fe2+ due to the endoperoxide crosslinks, leading to cell death in breast cancer cells. We also investigated the anti-cancer potential of poly(ARTEMA) on breast cancer cells with and without a ferroptosis inhibitor. The IC50 values were 125 µM for the MCF-7 cancer cell line and 300 µM for the normal MCF-10 cell line, indicating enhanced toxicity toward cancer cell lines. These findings suggested that poly(ARTEMA) induces ferroptosis in cancer cells and may serve as a promising candidate for cancer therapy with minimal cytotoxicity. To the best of our knowledge, this report may be the first that successfully synthesized poly(ARTEMA) using ART, with its anticancer potential evaluation.
format Article
id doaj-art-ccd45d46d90a484d965cd04d14b3c437
institution OA Journals
issn 1468-6996
1878-5514
language English
publishDate 2025-12-01
publisher Taylor & Francis Group
record_format Article
series Science and Technology of Advanced Materials
spelling doaj-art-ccd45d46d90a484d965cd04d14b3c4372025-08-20T02:26:33ZengTaylor & Francis GroupScience and Technology of Advanced Materials1468-69961878-55142025-12-0126110.1080/14686996.2025.2482514Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cellsNatsumi Ito0Ahmed Nabil1Koichiro Uto2Mitsuhiro Ebara3Research Center for Macromolecules and Biomaterials, National Institute for Materials Science (NIMS), Tsukuba, JapanResearch Center for Macromolecules and Biomaterials, National Institute for Materials Science (NIMS), Tsukuba, JapanResearch Center for Macromolecules and Biomaterials, National Institute for Materials Science (NIMS), Tsukuba, JapanResearch Center for Macromolecules and Biomaterials, National Institute for Materials Science (NIMS), Tsukuba, JapanFerroptosis, a form of non-apoptotic cell death, is emerging as a promising strategy for cancer therapy. Artesunate (ART), an extract obtained from the traditional Chinese medicine Qinghaosu, has been shown to exhibit anti-cancer activity by inducing ferroptosis in cancer cells. While previous research has focused on incorporating ART monomer into drug delivery systems for enhanced cancer targeting, this study presents 2-methacryloyloxyethyl ART polymer (poly(ARTEMA)), a novel polymer synthesized from ART for the first time. Our goal was evaluation of poly(ARTEMA) anticancer potential on breast cancer cells. First, we synthesized ARTEMA using esterification followed by its polymerization using the reversible addition-fragmentation chain transfer (RAFT) polymerization method. We evaluated its mechanism of action, focusing on two key pathways: temperature-triggered singlet oxygen generation and ferrous ions (Fe2+) release, both of which contribute to ferroptosis. Our results demonstrate that poly(ARTEMA) selectively generates singlet oxygen and Fe2+ due to the endoperoxide crosslinks, leading to cell death in breast cancer cells. We also investigated the anti-cancer potential of poly(ARTEMA) on breast cancer cells with and without a ferroptosis inhibitor. The IC50 values were 125 µM for the MCF-7 cancer cell line and 300 µM for the normal MCF-10 cell line, indicating enhanced toxicity toward cancer cell lines. These findings suggested that poly(ARTEMA) induces ferroptosis in cancer cells and may serve as a promising candidate for cancer therapy with minimal cytotoxicity. To the best of our knowledge, this report may be the first that successfully synthesized poly(ARTEMA) using ART, with its anticancer potential evaluation.https://www.tandfonline.com/doi/10.1080/14686996.2025.2482514Cancer therapyferroptosisartesunateendoperoxideferrous ironpoly(ARTEMA)
spellingShingle Natsumi Ito
Ahmed Nabil
Koichiro Uto
Mitsuhiro Ebara
Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
Science and Technology of Advanced Materials
Cancer therapy
ferroptosis
artesunate
endoperoxide
ferrous iron
poly(ARTEMA)
title Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
title_full Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
title_fullStr Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
title_full_unstemmed Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
title_short Poly(ARTEMA), a novel artesunate-based polymer induces ferroptosis in breast cancer cells
title_sort poly artema a novel artesunate based polymer induces ferroptosis in breast cancer cells
topic Cancer therapy
ferroptosis
artesunate
endoperoxide
ferrous iron
poly(ARTEMA)
url https://www.tandfonline.com/doi/10.1080/14686996.2025.2482514
work_keys_str_mv AT natsumiito polyartemaanovelartesunatebasedpolymerinducesferroptosisinbreastcancercells
AT ahmednabil polyartemaanovelartesunatebasedpolymerinducesferroptosisinbreastcancercells
AT koichirouto polyartemaanovelartesunatebasedpolymerinducesferroptosisinbreastcancercells
AT mitsuhiroebara polyartemaanovelartesunatebasedpolymerinducesferroptosisinbreastcancercells