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Molecules 2011, 16(12), 10556-10569; doi:10.3390/molecules161210556

The Effects of Artesunate on the Expression of EGFR and ABCG2 in A549 Human Lung Cancer Cells and a Xenograft Model

1,2, 1, 1, 1, 1, 1, 1,*  and 1,*
1 Cancer Institute of PLA, Xinqiao Hospital, Third Military Medical University, Xinqiao Street No. 2, Chongqing 400037, China 2 Department of Oncology, Affiliated Hospital of Zunyi Medical College, Zunyi 563000, China
* Authors to whom correspondence should be addressed.
Received: 31 October 2011 / Revised: 25 November 2011 / Accepted: 5 December 2011 / Published: 19 December 2011
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Non-small cell lung cancer (NSCLC) is the leading cause of cancer death worldwide. Clinical and laboratory studies have suggested that multi-targeting approaches against neoplastic cells could help to increase patient survival and might reduce the emergence of cells that are resistant to single-target inhibitors. Artesunate (ART) is one of the most potent and rapidly acting antimalarial agents known, and it also exerts a profound cytotoxic activity toward cancer cells and reverses multi-drug resistance. In the present study, we found that artesunate inhibited NSCLC A549 cell growth and proliferation, induced apoptosis and suppressed tumor growth in a dose-dependent manner in A549 cells and a mouse xenograft model. Furthermore, artesunate down-regulated the expression of epidermal growth factor receptor (EGFR), Akt and ATP-binding cassette subfamily G member 2 (ABCG2) at the mRNA and protein levels in vitro and in vivo. In conclusion, artesunate is an effective anti-cancer drug that may enhance the effectiveness of other anticancer drugs and may reverse multi-drug resistance by suppressing the transcription of ABCG2, which inhibits drug efflux.
Keywords: EGFR; ABCG2; Akt; artesunate; NSCLC; multi-drug resistance EGFR; ABCG2; Akt; artesunate; NSCLC; multi-drug resistance
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Ma, H.; Yao, Q.; Zhang, A.-M.; Lin, S.; Wang, X.-X.; Wu, L.; Sun, J.-G.; Chen, Z.-T. The Effects of Artesunate on the Expression of EGFR and ABCG2 in A549 Human Lung Cancer Cells and a Xenograft Model. Molecules 2011, 16, 10556-10569.

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