| Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells. | |
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MedLine Citation:
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PMID: 17163469 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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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Authors:
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Woong Nam; Jungae Tak; Ju-Kyoung Ryu; Mankil Jung; Jong-In Yook; Hyung-Jun Kim; In-Ho Cha |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Head & neck Volume: 29 ISSN: 1043-3074 ISO Abbreviation: Head Neck Publication Date: 2007 Apr |
Date Detail:
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Created Date: 2007-03-15 Completed Date: 2007-06-14 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8902541 Medline TA: Head Neck Country: United States |
Other Details:
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Languages: eng Pagination: 335-40 Citation Subset: IM |
Copyright Information:
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(c) 2006 Wiley Periodicals, Inc. |
Affiliation:
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Department of Oral and Maxillofacial Surgery, College of Dentistry, Yonsei University, Seoul, Korea. |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Antineoplastic Agents, Phytogenic
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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 |
| Chemical | |
Reg. No./Substance:
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0/Antineoplastic Agents, Phytogenic; 0/Artemisinins; 0/Sesquiterpenes; 63968-64-9/artemisinine |
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