期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 22, 页码 6508-6512出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.056
关键词
Chalcones; HTMC; Lung adenocarcinoma cells; Selective activity; p53-dependent pathway; In vivo tumor suppression
资金
- National Science Council of Taiwan [NSC 96-2113-M-324-002-MY3, NSC 99-2811-M-324-003]
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 suppresser genes p53 and p21. In addition, in vivo data demonstrated that HTMC act as a tumor growth suppressing agent. (C) 2010 Elsevier Ltd. All rights reserved.
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