Xia Yi, Shi Chuanjing, Lu Jingze, Zhu Zeyu, Li Mohan, Pan Yinan, Huang Xinyan, Zhang Lei, Liu Aifen
Institute of Interdisciplinary Integrative Medicine Research, School of Medicine, Nantong University, Nantong 226001, China.
Department of Pharmaceutical Botany, School of Pharmacy, Naval Medical University, Shanghai 200433, China.
Int J Mol Sci. 2025 Aug 29;26(17):8409. doi: 10.3390/ijms26178409.
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.
青蒿素及其衍生物因其卓越的抗疟功效而广受认可。最近，越来越多的证据表明其在疟疾之外具有治疗潜力。尽管有这些进展，但详细的机制和药理学局限性仍未完全明确。本综述总结了它们与肿瘤学、免疫调节和代谢紊乱相关的药理活性和分子机制。从机制上讲，这些化合物通过诱导氧化应激、阻滞细胞周期、触发细胞凋亡和抑制血管生成发挥强大的抗肿瘤作用。它们同样调节免疫反应，重新建立免疫稳态并增强免疫治疗策略的有效性。初步证据还表明其参与代谢调节，为治疗代谢紊乱指明了有前景的途径。鉴于青蒿素及其衍生物的其他作用机制，我们还讨论了抗肿瘤活性、免疫调节和代谢稳态之间的三位一体调节网络。我们预计未来的研究将填补这些知识空白，从而提高青蒿素及其衍生物的临床效用，并改善各种病症患者的治疗效果。
