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Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells

 Woong Nam  ;  Jungae Tak  ;  In-Ho Cha  ;  Hyung-Jun Kim  ;  Jong-In Yook  ;  Mankil Jung  ;  Ju-Kyoung Ryu 
 Head & Neck, Vol.29(4) : 335-340, 2007 
Journal Title
 Head & Neck 
Issue Date
Antineoplastic Agents, Phytogenic/pharmacology* ; Apoptosis/drug effects* ; Artemisia ; Artemisinins/pharmacology* ; Carcinoma, Squamous Cell/pathology* ; Cell Line, Tumor ; Cell Proliferation/drug effects* ; DNA Fragmentation/drug effects ; Drug Screening Assays, Antitumor* ; Humans ; Mouth Neoplasms/pathology* ; Sesquiterpenes/pharmacology* ; Tumor Cells, Cultured
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 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.
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2. College of Dentistry (치과대학) > Dept. of Oral Pathology (구강병리학교실) > 1. Journal Papers
2. College of Dentistry (치과대학) > Dept. of Oral and Maxillofacial Surgery (구강악안면외과학교실) > 1. Journal Papers
Yonsei Authors
Kim, Hyung Jun(김형준) ORCID logo https://orcid.org/0000-0001-8247-4004
Nam, Woong(남웅) ORCID logo https://orcid.org/0000-0003-0146-3624
Ryu, Ju Kyoung(유주경)
Yook, Jong In(육종인) ORCID logo https://orcid.org/0000-0002-7318-6112
Cha, In Ho(차인호) ORCID logo https://orcid.org/0000-0001-8259-2190
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