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	The design, synthesis, and anti-tumor mechanism study of N-phosphoryl amino acid modified resveratrol analogues
	Liu, Huachen ; Dong, Aijun ; Gao, Chunmei ; Tan, Chunyan ; Liu, Hongxia ; Zu, Xuyu ; Jiang, Yuyang
	2010-05-11 ; 2010-05-11
关键词	Resveratrol N-Phosphoryl amino acid Apoptosis Mitochondrial pathway APOPTOSIS-INDUCING AGENTS BIOLOGICAL EVALUATION CELL-DEATH K562 CELLS PTEROSTILBENE DERIVATIVES PATHWAY PROBES KIND Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic
中文摘要	A novel series of trans-N-phosphoryl amino acid modified resveratrol analogues were synthesized and evaluated in vitro for their cytotoxic effects against CNE-1 and CNE-2 cell lines. These analogues showed good anti-proliferative activity, among which 8d, 8e, 8j, and 9d displayed much stronger inhibition effect than resveratrol and 8d showed the most potent activity with IC50 value at 3.45 +/- 0.82 mu M. The antitumor effects of 8d, 8e, 8j, and 9d were due to the induction of apoptosis, confirmed by the DNA fragmentation and flow cytometry analysis using PI (propidium iodide) staining and Annexin-V-FITC/PI staining assay. The PI staining assay also showed that 8d, 8e, 8j, and 9d caused cell cycles arrest at G(0)-G(1) phase which finally led to cell apoptosis. Further mechanism study on compound 8d against CNE-2 cells has shown the PARP cleavage, which is a hallmark of caspase-3 activation, as well as the activation of caspase-9, and the intracellular ROS generation. These results all suggest that 8d induced a mitochondrial-dependent apoptosis pathway. (c) 2008 Elsevier Ltd. All rights reserved.
语种	英语 ; 英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD ; OXFORD ; THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND
内容类型	期刊论文
源URL	[http://hdl.handle.net/123456789/26413]
专题	清华大学
推荐引用方式 GB/T 7714	Liu, Huachen,Dong, Aijun,Gao, Chunmei,et al. The design, synthesis, and anti-tumor mechanism study of N-phosphoryl amino acid modified resveratrol analogues[J],2010, 2010.
APA	Liu, Huachen.,Dong, Aijun.,Gao, Chunmei.,Tan, Chunyan.,Liu, Hongxia.,...&Jiang, Yuyang.(2010).The design, synthesis, and anti-tumor mechanism study of N-phosphoryl amino acid modified resveratrol analogues..
MLA	Liu, Huachen,et al."The design, synthesis, and anti-tumor mechanism study of N-phosphoryl amino acid modified resveratrol analogues".(2010).

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