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

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 (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.

• Authors: Woong Nam, Jungae Tak, Ju-Kyoung Ryu, Mankil Jung, Jong-In Yook, Hyung-Jun Kim, In-Ho Cha
• Journal: Head & neck (Head Neck) Vol. 29 Issue 4 Pg. 335-40 (Apr 2007) ISSN: 1043-3074 [Print] United States
• PMID: 17163469 (Publication Type: Journal Article)
• Copyright: (c) 2006 Wiley Periodicals, Inc.

Chemical References

• Antineoplastic Agents, Phytogenic
• Artemisinins
• Sesquiterpenes
• artemisinin

Topics

• 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