Abstract
Dihydroartemisinin (DHA) is a derivative of artemisinin, which firstly showed higher
antimalarial activity. Over the years, DHA has also been discovered to exhibit higher anticancer
efficacy without adverse side effects. Although some shortcomings have been discovered during
biological evaluation (such as poor aqueous solubility, short half-life, and initial burst release effect),
several attempts have been developed to overcome these shortcomings. For example, appropriate
delivery techniques were used to improve its anticancer efficacy. In this minireview, we
focused on summarizing the anticancer mechanisms, anticancer efficacy of free DHA and in
combination therapies, hybrids, and nanoparticle formulations, which will provide adequate insights
for its clinical use as anticancer agents, and on the design and synthesis of DHA derivatives
for the development of anticancer agents.
Keywords:
Dihydroartemisinin, derivatives, anticancer mechanisms, shortcomings, hybrids, nanoparticles.
Graphical Abstract
[3]
Crespo-Ortiz, M.P.; Wei, M.Q. Antitumor Activity of Artemisinin and Its Derivatives: From a Well-Known Antimalarial Agent to a Potential Anticancer Drug. J. Biomed. Biotechnol., 2012, 2012, 1-18.
[19]
Li, T.; Yao, L. Basic and clinical researches on antitumor effects of antimalarial artemisinin and its derivatives. Zhongguo Xinyao yu Linchuang Zazhi, 2008, 27, 227-230.
[41]
Ontikatze, T.; Handrick, R.; Grimm, F.; Henke, G.; Daniel, P.T.; Belka, C.; Jendrossek, V. Dihydroartemisinin is a hypoxia active anticancer drug. EJC supplements, 2010, 8(5), 83-154.
[70]
Elhassanny, A.E.M.; Soliman, E.; Marie, M.; McGuire, P.; Gul, W.; ElSohly, M.A.; Van Dross, R. Heme-dependent ER stress apoptosis: A mechanism for the selective toxicity of the dihydroartemisinin, NSC735847, in colorectal cancer cells. Front. Oncol, 2020, 10, 965.1-16.
[82]
Que, Z.Y.; Wang, P.; Hu, Y.; Xue, Y.X.; Liu, X.B.; Qu, C.B.; Ma, J.; Liu, Y.H. Dihydroartemisin inhibits glioma invasiveness via a ROS to P53 to β-catenin signaling 2016, 119, 72-88.