- Head Neck. 2007 Apr;29(4):335-40.
Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells.
Nam W, Tak J, Ryu JK, Jung M, Yook JI, Kim HJ, Cha IH.
Department of Oral and Maxillofacial Surgery, College of Dentistry, Yonsei University, Seoul, Korea.
Artemisinin is of special biological interest because of its
outstanding antimalarial activity. Recently, it was reported that
artemisinin has antitumor activity. Its derivatives, artesunate,
arteether, and artemeter, also have antitumor activity against
melanoma, breast, ovarian, prostate, CNS, and renal cancer cell lines.
Recently, monomer, dimer, and trimer derivatives were synthesized from
deoxoartemisinin, and the dimers and the trimers were found to have
much more potent antitumor activity than the monomers. METHODS: We
evaluated the antitumor activity of artemisinin and its various
derivatives (dihydroartemisinin, dihydroartemisinin 12-benzoate,
12-(2'-hydroxyethyl) deoxoartemisinin, 12-(2'-ethylthio)
deoxoartemisinin dimer, deoxoartemisinin trimer) in comparison with
paclitaxel (Taxol), 5-fluorouracil (5-FU), cisplatin in vitro. RESULTS:
In this study, the deoxoartemisinin trimer had the most potent
antitumor effect (IC(50) = 6.0 microM), even better than paclitaxel
(IC(50) = 13.1 microM), on oral cancer cell line (YD-10B). In addition,
it induced apoptosis through a caspase-3-dependent mechanism.
CONCLUSION: The deoxoartemisinin trimer was found to have greater
antitumor effect on tumor cells than other commonly used
chemotherapeutic drugs, such as 5-FU, cisplatin, and paclitaxel.
Furthermore, the ability of artemisinin and its derivatives to induce
apoptosis highlights their potential as chemotherapeutic agents, for
many anticancer drugs achieve their antitumor effects by inducing
apoptosis in tumor cells. (c) 2006 Wiley Periodicals, Inc.