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.
aZhongshan School of Medicine, Sun Yat-sen University
bDepartment of Haematology, The Third Affiliated Hospital of Sun Yat-sen University, Sun Yat-sen Institute of Hematology, Guangzhou, Guangdong, China
cDepartment of Pathology
dDepartment of Pharmacy
eDepartment of Haematology, Monash Medical Centre
fDepartment of Medicine, Monash University, Clayton, Victoria
gThe Canberra Hospital, Woden Valley, Canberra, Australia
*Nelson Siukei Lam and Xinxin Long contributed equally to the writing of this article.
Correspondence to James C.G. Doery, MD, FRCPA, Department of Pathology, Monash Medical Centre, 246 Clayton Road, Clayton, Victoria 3168, Australia Tel: +61 39 594 4522; fax: +61 39 594 6619; e-mail: firstname.lastname@example.org
Received March 9, 2018
Accepted September 3, 2018