Abstract
The sourcing of pharmaceutical agents from natural products remains a cornerstone of drug discovery. For millennia, herbal remedies have served as foundational therapeutic interventions, yet their mechanisms of action often remain elusive. Artemisinin (ART, or "Qinghaosu") and its derivatives, collectively known as ARTs, exemplify this paradigm. Originating from traditional Chinese medicine, these well-established antimalarial compounds exhibit potent cytotoxicity, positioning them as promising anti-cancer agents. ARTs operate through multiple cancer cell-intrinsic mechanisms and demonstrate synergistic effects with conventional therapies, even against chemoresistant malignancies. Beyond oncology, the therapeutic portfolio of ART-based drugs is rapidly expanding. This review synthesizes recent advancements in the application of ARTs for treating various cancers, Alzheimer's disease, and reproductive disorders. Furthermore, we explore the frontier of ART drug development, focusing on the rational design of ART-derived molecular hybrids and the engineering of nano-enabled delivery systems. These innovative strategies are pivotal for enhancing anti-cancer efficacy and achieving cancer-specific targeting. Ultimately, this work aims to guide the innovation of ART-based precision medicine, revitalizing the exploration and development of natural products in modern pharmacotherapy.