Abstract
Abstract Introduction: Artesunate is a semi-synthetic derivative of artemisinin, a natural compound from the herb sweet wormwood (Artemisia annua L). Artemisinin has been used for centuries in traditional Chinese medicine while artesunate has recently been used as an anti-malarial drug. Artesunate is also cytotoxic to human cancer cells. Since the use of artesunate as an anti-malarial agent is associated with few adverse effects, artesunate may represent a less toxic alternative to conventional chemotherapy. This study investigates the effects of artesunate on ovarian cancer cell lines and the mechanism(s) underlying its activity. Methods and Results: Artesunate had a time- and dose-dependent growth inhibitory effect on all ovarian carcinoma cell lines examined (SKOV3, OVCAR3, IG-OV-1, HEY) using an MTT assay. Further examination of artesunate-treated SKOV3 and HEY cells using Oregon Green-488 and Annexin-V-FLUOS/propidium iodide staining indicated that artesunate had a strong anti-proliferative effect but was not cytotoxic towards the ovarian cancer cells. Cell cycle arrest occurred in the G1 and G2 phases of the cell cycle, and western blot analysis showed artesunate-induced changes in the expression and phosphorylation of a range of cell cycle proteins including the retinoblastoma protein, p21, and cyclin B1. Pretreatment with holotransferrin increased artesunate's anti-proliferative activity. Conclusions: These data show that artesunate possess a strong anti-proliferative activity in ovarian cancer cell cultures and therefore warrants further investigation as a possible treatment for ovarian cancer. Research supported by NSERC. Citation Format: {Authors}. {Abstract title} [abstract]. In: Proceedings of the 103rd Annual Meeting of the American Association for Cancer Research; 2012 Mar 31-Apr 4; Chicago, IL. Philadelphia (PA): AACR; Cancer Res 2012;72(8 Suppl):Abstract nr 1979. doi:1538-7445.AM2012-1979
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