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

被引：34

作者：

Rao, Yerra Koteswara ^{[2
]}

Kao, Te-Yu ^{[3
]}

Ko, Jiunn-Liang ^{[1
,4
]}

Tzeng, Yew-Min ^{[2
]}

机构：

[1] Chung Shan Med Univ Hosp, Dept Med Oncol & Chest Med, Taichung, Taiwan

[2] Chaoyang Univ Technol, Inst Biochem Sci & Technol, Wufeng Township, Taiwan

[3] Chung Shan Med Univ, Inst Med & Mol Toxicol, Taichung, Taiwan

[4] Chung Shan Med Univ, Inst Med, Taichung, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 22期

关键词：

Chalcones; HTMC; Lung adenocarcinoma cells; Selective activity; p53-dependent pathway; In vivo tumor suppression; CANCER; DERIVATIVES; SERIES; P53;

D O I：

10.1016/j.bmcl.2010.09.056

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：6508 / 6512

页数：5

共 25 条

[1]

Amaral JD, 2010, DISCOV MED, V9, P145

[2] Transcriptional targets of p53 that regulate cellular proliferation [J].