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查尔酮 HTMC 引起体外选择性细胞毒性，通过 p53 依赖性途径在人肺腺癌细胞 A549 中引起细胞周期 G1 期阻滞，并在体内抑制肿瘤生长。

Chalcone HTMC causes in vitro selective cytotoxicity, cell-cycle G1 phase arrest through p53-dependent pathway in human lung adenocarcinoma A549 cells, and in vivo tumor growth suppression.

机构信息

Institute of Biochemical Sciences and Technology, Chaoyang University of Technology, Wufeng, Taiwan, ROC.

出版信息

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6508-12. doi: 10.1016/j.bmcl.2010.09.056. Epub 2010 Sep 17.

DOI:10.1016/j.bmcl.2010.09.056
PMID:20926293
Abstract

The present Letter identified 2'-hydroxy-2,3,4',6'-tetramethoxychalcone (HTMC) as a potent in vitro cytotoxic agent with selective activity against cell lines derived from human lung cancer. In A549 lung adenocarcinoma cells, HTMC caused G1 phase cell-cycle arrest. HTMC treatment also led to an inhibition of cell-cycle regulatory proteins phosphorylation of cdc2 (Tyr(15) and Tyr(161)) and Rb (Ser(795) and Ser(807/811)), which was accompanied by the accumulation of tumor suppressor genes p53 and p21. In addition, in vivo data demonstrated that HTMC act as a tumor growth suppressing agent.

摘要

这封信件指出 2'-羟基-2,3,4',6'-四甲氧基查耳酮（HTMC）是一种有效的体外细胞毒性剂，对源自人类肺癌的细胞系具有选择性活性。在 A549 肺腺癌细胞中，HTMC 导致 G1 期细胞周期停滞。HTMC 处理还导致细胞周期调节蛋白 cdc2（Tyr(15) 和 Tyr(161)) 和 Rb (Ser(795) 和 Ser(807/811))的磷酸化抑制，这伴随着肿瘤抑制基因 p53 和 p21 的积累。此外，体内数据表明 HTMC 作为肿瘤生长抑制剂发挥作用。

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