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

Woong Nam, Jungae Tak, Ju Kyoung Ryu, Mankil Jung, Jong In Yook, Hyung Jun Kim, In Ho Cha

Research output: Contribution to journalArticle

117 Citations (Scopus)

Abstract

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 (IC50 = 6.0 μM), even better than paclitaxel (IC50 = 13.1 μM), 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.

Original languageEnglish
Pages (from-to)335-340
Number of pages6
JournalHead and Neck
Volume29
Issue number4
DOIs
Publication statusPublished - 2007 Apr 1

Fingerprint

Mouth Neoplasms
dihydroartemisinin
Apoptosis
Growth
Paclitaxel
Fluorouracil
Inhibitory Concentration 50
Cell Line
Kidney Neoplasms
Benzoates
Antimalarials
Caspase 3
Pharmaceutical Preparations
Antineoplastic Agents
Cisplatin
deoxoartemisinin
artemisinine
Melanoma
Neoplasms
Prostatic Neoplasms

All Science Journal Classification (ASJC) codes

  • Otorhinolaryngology

Cite this

Nam, Woong ; Tak, Jungae ; Ryu, Ju Kyoung ; Jung, Mankil ; Yook, Jong In ; Kim, Hyung Jun ; Cha, In Ho. / Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells. In: Head and Neck. 2007 ; Vol. 29, No. 4. pp. 335-340.
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Effects of artemisinin and its derivatives on growth inhibition and apoptosis of oral cancer cells. / Nam, Woong; Tak, Jungae; Ryu, Ju Kyoung; Jung, Mankil; Yook, Jong In; Kim, Hyung Jun; Cha, In Ho.

In: Head and Neck, Vol. 29, No. 4, 01.04.2007, p. 335-340.

Research output: Contribution to journalArticle

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AU - Tak, Jungae

AU - Ryu, Ju Kyoung

AU - Jung, Mankil

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AU - Kim, Hyung Jun

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N2 - 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 (IC50 = 6.0 μM), even better than paclitaxel (IC50 = 13.1 μM), 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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