Zhongshan School of Medicine, Sun Yat-sen University.
Department of Haematology, The Third Affiliated Hospital of Sun Yat-sen University, Sun Yat-sen Institute of Hematology, Guangzhou, Guangdong, China.
Anticancer Drugs. 2019 Jan;30(1):1-18. doi: 10.1097/CAD.0000000000000697.
Artemisinin (ART) and its derivatives are one of the most important classes of antimalarial agents, originally derived from a Chinese medicinal plant called Artemisia annua L. Beyond their outstanding antimalarial and antischistosomal activities, ART and its derivatives also possess both in-vitro and in-vivo activities against various types of cancer. Their anticancer effects range from initiation of apoptotic cell death to inhibition of cancer proliferation, metastasis and angiogenesis, and even modulation of the cell signal transduction pathway. This review provides a comprehensive update on ART and its derivatives, their mechanisms of action, and their synergistic effects with other chemicals in targeting leukemia cells. Combined with limited evidence of drug resistance and low toxicity profile, we conclude that ART and its derivatives, including dimers, trimers, and hybrids, might be a potential therapeutic alternative to current chemotherapies in combating leukemia, although more studies are necessary before they can be applied clinically.
青蒿素（ART）及其衍生物是最重要的抗疟药物之一，最初来源于一种名为黄花蒿（Artemisia annua L.）的中草药。除了出色的抗疟和抗血吸虫活性外，ART 及其衍生物还具有体外和体内对抗各种类型癌症的活性。它们的抗癌作用范围从诱导细胞凋亡到抑制癌细胞增殖、转移和血管生成，甚至调节细胞信号转导途径。本综述全面介绍了 ART 及其衍生物的作用机制及其与其他化学物质在靶向白血病细胞方面的协同作用。结合耐药性证据有限且毒性特征较低的情况，我们得出结论，ART 及其衍生物（包括二聚体、三聚体和杂合体）可能是对抗白血病的一种有前途的治疗选择，尽管在临床应用之前还需要进行更多的研究。
