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Volume 26
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10.3390/ijms26178409
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This is an early access version, the complete PDF, HTML, and XML versions will be available soon.
Review

Artemisinin and Its Derivatives from Molecular Mechanisms to Clinical Applications: New Horizons Beyond Antimalarials

by
Yi Xia
1,
Chuanjing Shi
1,
Jingze Lu
1,
Zeyu Zhu
1,
Mohan Li
1,
Yinan Pan
1,
Xinyan Huang
1,
Lei Zhang
1,2,* and
Aifen Liu
1,*
1
Institute of Interdisciplinary Integrative Medicine Research, School of Medicine, Nantong University, Nantong 226001, China
2
Department of Pharmaceutical Botany, School of Pharmacy, Naval Medical University, Shanghai 200433, China
*
Authors to whom correspondence should be addressed.
Int. J. Mol. Sci. 2025, 26(17), 8409; https://doi.org/10.3390/ijms26178409
Submission received: 21 July 2025 / Revised: 23 August 2025 / Accepted: 28 August 2025 / Published: 29 August 2025
(This article belongs to the Section Molecular Biology)
Versions Notes

Abstract

Artemisinin and its derivatives are widely recognized for their exceptional antimalarial efficacy. Recently, accumulating evidence indicates therapeutic potential beyond malaria. Despite these advances, detailed mechanisms and pharmacological limitations remain incompletely defined. This review summarizes their pharmacological activities and molecular mechanisms associated with oncology, immunoregulation, and metabolic disorders. Mechanistically, these compounds exert potent antitumor effects by inducing oxidative stress, arresting the cell cycle, triggering apoptosis, and inhibiting angiogenesis. They likewise modulate immune responses, re-establishing immune homeostasis and enhancing the effectiveness of immunotherapeutic strategies. Preliminary evidence also suggests involvement in metabolic regulation, pointing to promising avenues for treating metabolic disorders. Given alternative mechanisms of artemisinin and its derivatives, we also discuss the trinity modulation network among antitumor activity, immunoregulation, and metabolic homeostasis. We anticipate that future research will address these knowledge gaps, thereby enhancing the clinical utility of artemisinin and its derivatives and improving patient outcomes across diverse pathologies.
Keywords: artemisinin; derivatives; antitumor; immunoregulation; metabolic regulation artemisinin; derivatives; antitumor; immunoregulation; metabolic regulation

Share and Cite

MDPI and ACS Style

Xia, Y.; Shi, C.; Lu, J.; Zhu, Z.; Li, M.; Pan, Y.; Huang, X.; Zhang, L.; Liu, A. Artemisinin and Its Derivatives from Molecular Mechanisms to Clinical Applications: New Horizons Beyond Antimalarials. Int. J. Mol. Sci. 2025, 26, 8409. https://doi.org/10.3390/ijms26178409

AMA Style

Xia Y, Shi C, Lu J, Zhu Z, Li M, Pan Y, Huang X, Zhang L, Liu A. Artemisinin and Its Derivatives from Molecular Mechanisms to Clinical Applications: New Horizons Beyond Antimalarials. International Journal of Molecular Sciences. 2025; 26(17):8409. https://doi.org/10.3390/ijms26178409

Chicago/Turabian Style

Xia, Yi, Chuanjing Shi, Jingze Lu, Zeyu Zhu, Mohan Li, Yinan Pan, Xinyan Huang, Lei Zhang, and Aifen Liu. 2025. "Artemisinin and Its Derivatives from Molecular Mechanisms to Clinical Applications: New Horizons Beyond Antimalarials" International Journal of Molecular Sciences 26, no. 17: 8409. https://doi.org/10.3390/ijms26178409

APA Style

Xia, Y., Shi, C., Lu, J., Zhu, Z., Li, M., Pan, Y., Huang, X., Zhang, L., & Liu, A. (2025). Artemisinin and Its Derivatives from Molecular Mechanisms to Clinical Applications: New Horizons Beyond Antimalarials. International Journal of Molecular Sciences, 26(17), 8409. https://doi.org/10.3390/ijms26178409

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