Abstract: 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
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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.
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(12):10556-10569.
Ma, Hu; Yao, Quan; Zhang, An-Mei; Lin, Sheng; Wang, Xin-Xin; Wu, Lei; Sun, Jian-Guo; Chen, Zheng-Tang. 2011. "The Effects of Artesunate on the Expression of EGFR and ABCG2 in A549 Human Lung Cancer Cells and a Xenograft Model." Molecules 16, no. 12: 10556-10569.