Cancer Institute of PLA, Xinqiao Hospital, Third Military Medical University, Xinqiao Street No. 2, Chongqing 400037, China.
Molecules. 2011 Dec 19;16(12):10556-69. doi: 10.3390/molecules161210556.
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.
非小细胞肺癌（NSCLC）是全球癌症死亡的主要原因。临床和实验室研究表明，针对肿瘤细胞的多靶点方法可能有助于提高患者的生存率，并可能减少对单靶点抑制剂产生耐药性的细胞的出现。青蒿琥酯（ART）是已知最有效和作用最快的抗疟药物之一，它对癌细胞也具有很强的细胞毒性作用，并能逆转多药耐药性。在本研究中，我们发现青蒿琥酯能抑制 NSCLC A549 细胞的生长和增殖，在 A549 细胞和小鼠异种移植模型中，以剂量依赖的方式诱导细胞凋亡和抑制肿瘤生长。此外，青蒿琥酯在体外和体内均能下调表皮生长因子受体（EGFR）、Akt 和三磷酸腺苷结合盒亚家族 G 成员 2（ABCG2）的 mRNA 和蛋白表达。总之，青蒿琥酯是一种有效的抗癌药物，它可能通过抑制 ABCG2 的转录来增强其他抗癌药物的疗效，并逆转多药耐药性，从而抑制药物外排。
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