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	11,11'-dideoxy-verticillin: a natural compound possessing growth factor receptor tyrosine kinase-inhibitory effect with anti-tumor activity
	Zhang, YX; Chen, Y; Guo, XN; Zhang, XW; Zhao, WM; Zhong, L; Zhou, J; Xi, Y; Lin, LP; Ding, J
刊名	Anti-cancer drugs
	2005-06-01
卷号	16期号:5页码:515-524
关键词	11,11'-dideoxy-verticillin Epidermal growth factor receptor Vascular endothelial growth factor receptor-1 Erk1/2 Anti-tumor
ISSN号	0959-4973
通讯作者	Ding, j()
英文摘要	11,11'-dideoxy-verticillin, a compound of the novel epidithiodioxopiprazine structural class, is isolated from the traditional chinese medicinal herb shiraia bambusicola. the present study demonstrated for the first time that 11,11'-dideoxy-verticillin has potent tyrosine kinase-inhibitory and anti-tumor activities. in the cell-free elisa tyrosine kinase assay, 11,11'-dideoxy-verticillin significantly inhibited the activities of epidermal growth factor receptor (egfr), vascular endothelial growth factor receptor-1/fms-like tyrosine kinase-1 (vegfr-1/flt-1) and human epidermal growth factor receptor-2 (her2/erbb-2), with relative specificity on egfr and vegfr-1 with ic(50)s of 0.136 +/- 0.109 and 1.645 +/- 0.885 nm, respectively. exposure of 11,11'-dideoxy-verticillin for 1 h to egfr-overexpressed mda-mb-468 human breast carcinoma cells and her2-overexpressed sk-ov-3 human ovarian adenocarcinoma cells resulted in obvious inhibition of egf-induced phosphorylation of egfr and her2. in addition, 11,11'-dideoxy-verticillin also inhibited the egf-induced phosphorylation of erk1/2, but had no effect on the phosphorylation of akt in both tumor cell lines. moreover, 11,11'-dideoxy-verticillin has potent anti-tumor activity. in vitro cytotoxicity assay showed that 11,11'-dideoxy-verticillin potently inhibited the proliferation of four human breast tumor cell lines with an average ic50 value of 0.2 mu m. in vivo, 11,11'-dideoxy-verticillin exhibited remarkable efficacy against mice sarcoma 180 and hepatoma 22 after daily i.p. administration of 0.5 or 0.75 mg/kg with inhibition rates ranging from 45.0 to 72.4%. treated with 11,11'-dideoxy-verticillin at 0.5-2.0 mu m for 36h, mb-mb-468 cells exhibited significant apoptotic morphological changes. at low concentrations (0.0625-0.5 mu m) for 24 h, 11,11'-dideoxy-verticillin induced a dose-dependent accumulation of mda-mb-468 cells in the g(2)/m phase of the cell cycle. these results indicate that 11,11'-dideoxy-verticillin is a naturally derived growth factor receptor tyrosine kinase inhibitor with potent anti-tumor activity. anti-cancer drugs 16:515-524 (c) 2005 lippincott williams & wilkins.
WOS关键词	CELL LUNG-CANCER ; PHASE-II TRIAL ; GEFITINIB ; THERAPY ; PATHWAY ; DRUGS
WOS研究方向	Oncology ; Pharmacology & Pharmacy
WOS类目	Oncology ; Pharmacology & Pharmacy
语种	英语
出版者	LIPPINCOTT WILLIAMS & WILKINS
WOS记录号	WOS:000229224300007
内容类型	期刊论文
URI标识	http://www.corc.org.cn/handle/1471x/2378081
专题	中国科学院大学
通讯作者	Ding, J
作者单位	1.Chinese Acad Sci, Div Anti Tumor Pharmacol, State Key Lab Drug Res, Shanghai Inst Mat Med,Inst Biol Sci,Dept Phytoche, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, Div Anti Tumor Pharmacol, State Key Lab Drug Res, Shanghai, Peoples R China 3.Chinese Acad Sci, Grad Sch, Shanghai, Peoples R China
推荐引用方式 GB/T 7714	Zhang, YX,Chen, Y,Guo, XN,et al. 11,11'-dideoxy-verticillin: a natural compound possessing growth factor receptor tyrosine kinase-inhibitory effect with anti-tumor activity[J]. Anti-cancer drugs,2005,16(5):515-524.
APA	Zhang, YX.,Chen, Y.,Guo, XN.,Zhang, XW.,Zhao, WM.,...&Ding, J.(2005).11,11'-dideoxy-verticillin: a natural compound possessing growth factor receptor tyrosine kinase-inhibitory effect with anti-tumor activity.Anti-cancer drugs,16(5),515-524.
MLA	Zhang, YX,et al."11,11'-dideoxy-verticillin: a natural compound possessing growth factor receptor tyrosine kinase-inhibitory effect with anti-tumor activity".Anti-cancer drugs 16.5(2005):515-524.

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