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Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells
Author(s) -
Nam Woong,
Tak Jungae,
Ryu JuKyoung,
Jung Mankil,
Yook JongIn,
Kim HyungJun,
Cha InHo
Publication year - 2007
Publication title -
head and neck
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.012
H-Index - 127
eISSN - 1097-0347
pISSN - 1043-3074
DOI - 10.1002/hed.20524
Subject(s) - artemisinin , dihydroartemisinin , cisplatin , paclitaxel , artesunate , pharmacology , apoptosis , chemistry , carboplatin , trimer , cytostasis , cancer research , in vitro , cytotoxicity , cancer , medicine , chemotherapy , biochemistry , plasmodium falciparum , immunology , dimer , organic chemistry , malaria
Background. 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 μ M ), even better than paclitaxel (IC 50 = 13.1 μ M ), 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. © 2006 Wiley Periodicals, Inc. Head Neck, 2007.