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Chinese Academy of Sciences Institutional Repositories Grid
Stereospecific induction of nuclear factor-kappa b activation by isochamaejasmin

文献类型:期刊论文

作者Tian, QH; Li, J; Xie, X; Sun, ML; Sang, HR; Zhou, CH; An, TY; Hu, LH; Ye, RD; Wang, MW
刊名Molecular pharmacology
出版日期2005-12-01
卷号68期号:6页码:1534-1542
ISSN号0026-895X
DOI10.1124/mol.105.014720
通讯作者Wang, mw(center@mail.shcnc.ac.cn)
英文摘要The root of stellera chamaejasme l. is a traditional chinese herb termed rui xiang lang du and has been used to treat solid tumors, tuberculosis and psoriasis. exactly how s. chamaejasme l. regulates cellular responses remains unclear. we examined four biflavonoids isolated from s. chamaejasme l., including isochamaejasmin, two of its stereo-isomers and a methyl derivative, in functional assays originally designed to screen ligands for the g protein-coupled formyl peptide receptor-like 1 (fprl1). isochamaejasmin was found to induce the expression of a nuclear factor (nf)-kappa b-directed reporter gene in transfected hela cells with an ec(50) of 3.23 mu m, independently of fprl1. the isochamaejasmin-stimulated nf-kappa b reporter activity was accompanied by nuclear translocation of nf-kappa b proteins and was blocked by a dominant-negative construct of i kappa b alpha. isochamaejasmin also induced time-dependent phosphorylation of the mitogen-activated protein kinases extracellular signal-regulated kinase 1/2 and p38, and a novel protein kinase c (pkc delta). likewise, inhibition of these kinases with the respective pharmacological inhibitors significantly reduced the isochamaejasmin-stimulated nf-kappa b activation. it is noteworthy that the two stereoisomers and the methyl derivative did not induce detectable activation of nf-kappa b and were more cytotoxic than isochamaejasmin, which could partially rescue cycloheximide-induced apoptosis. inhibition of nf-kappa b activation reversed the anti-apoptotic effect of isochamaejasmin. these results provide the first evidence for a potential mechanism of action by s. chamaejasme l., and indicate that structurally similar compounds derived from s. chamaejasme l. may have different pharmacological properties.
WOS关键词STELLERA-CHAMAEJASME L ; FORMYL PEPTIDE RECEPTOR ; TUMOR PROMOTER ; 7-TRANSMEMBRANE ; INFLAMMATION ; GNIDIMACRIN ; MECHANISM ; LIGAND
WOS研究方向Pharmacology & Pharmacy
WOS类目Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000233340200004
出版者AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
URI标识http://www.irgrid.ac.cn/handle/1471x/2377639
专题中国科学院大学
通讯作者Wang, MW
作者单位1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China
2.Chinese Acad Sci, Grad Sch, Shanghai 201203, Peoples R China
3.Univ Illinois, Coll Med, Dept Pharmacol, Chicago, IL USA
推荐引用方式
GB/T 7714
Tian, QH,Li, J,Xie, X,et al. Stereospecific induction of nuclear factor-kappa b activation by isochamaejasmin[J]. Molecular pharmacology,2005,68(6):1534-1542.
APA Tian, QH.,Li, J.,Xie, X.,Sun, ML.,Sang, HR.,...&Wang, MW.(2005).Stereospecific induction of nuclear factor-kappa b activation by isochamaejasmin.Molecular pharmacology,68(6),1534-1542.
MLA Tian, QH,et al."Stereospecific induction of nuclear factor-kappa b activation by isochamaejasmin".Molecular pharmacology 68.6(2005):1534-1542.

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来源:中国科学院大学

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