Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum

doi:10.1055/s-0032-1315121

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum
	Liu, Jiawei 1; Zhang, Qing2 ; Chen, Kaotang ; Liu, Jingli 2; Kuang, Shan 2; Chen, Weiwen ; Yu, Qiang2
刊名	PLANTA MEDICA
	2012-09
卷号	78 期号:14 页码:1568-1570
关键词	Polygonum cuspidatum Polygonaceae STAT3 signaling modulators 2-methoxystypandrone
ISSN号	0032-0943
DOI	10.1055/s-0032-1315121
文献子类	Article
英文摘要	Constitutively activated STAT3 plays a pivotal role in oncogenesis and metastasis in many human cancers, and STAT3 has been validated as a novel anticancer drug target. Thus, the identification of small molecules that modulate STAT3 activity could be of great therapeutic importance. The aim of this study was to isolate novel modulators of the STAT3 signaling pathway from the roots of Polygonum cuspidatum by bioassay-guided fractionation using a STAT3 reporter gene assay. 2-Methoxystypandrone (1), as well as three anthraquinones (2-4), were identified as major active components of P. cuspidatum. Compound 1 demonstrated a potent inhibitory effect on STAT3 activation and significantly inhibited cell proliferation of human breast cancer cells, especially those with constitutively activated STAT3 (IC50 = 2.7-3.1 mu M). The SAR analysis of quinone analogues suggested that the phenolic and carbonyl groups are the key structures contributing to their inhibitory activities against the STAT3 signaling.
资助项目	Guangzhou University of Chinese Medicine[00000000] ; Doctoral Fund of the Ministry of Education of China[20104425120006] ; China National Natural Science Foundation[91129701] ; China National Natural Science Foundation[81102848] ; China National Natural Science Foundation[31129004] ; China National Science and Technology 973 grant[2012CB910704]
WOS关键词	CONSTITUTIVE ACTIVATION ; CARCINOMA CELLS ; EMODIN ; TUMORS ; SRC
WOS研究方向	Plant Sciences ; Pharmacology & Pharmacy ; Integrative & Complementary Medicine
语种	英语
出版者	GEORG THIEME VERLAG KG
WOS记录号	WOS:000309521800009
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277951]
专题	药理学第一研究室
通讯作者	Liu, Jingli
作者单位	1.Guangzhou Univ Chinese Med, Res Ctr Med Plants Resource Sci & Engn, Key Lab Chinese Med Plants Resource Lingnan, Higher Educ Mega Ctr,Minist Educ, Guangzhou 510006, Guangdong, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Dept Pharmacol, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Liu, Jiawei,Zhang, Qing,Chen, Kaotang,et al. Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum[J]. PLANTA MEDICA,2012,78(14):1568-1570.
APA	Liu, Jiawei.,Zhang, Qing.,Chen, Kaotang.,Liu, Jingli.,Kuang, Shan.,...&Yu, Qiang.(2012).Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum.PLANTA MEDICA,78(14),1568-1570.
MLA	Liu, Jiawei,et al."Small-molecule STAT3 Signaling Pathway Modulators from Polygonum cuspidatum".PLANTA MEDICA 78.14(2012):1568-1570.