Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase

	Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase
	Lu, Danfeng ; Yang, Lijuan ; Li, Qilin ; Gao, Xiaoping ; Wang, Fei ; Zhang, Guolin
刊名	EUROPEAN JOURNAL OF PHARMACOLOGY
	2012
卷号	691 期号:1-3 页码:275-282
关键词	Egonol Estrogen Aromatase Styrax perkinsiae KGN cellline
ISSN号	0014-2999
通讯作者	Wang, F (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China ; Zhang, Guolin
产权排序	1
英文摘要	Estrogen deficiency is associated with a variety of diseases, including osteoporosis, atherosclerosis, and Alzheimer's disease. Aromatase cytochrome P450 is the only enzyme in vertebrates known to catalyze the biosynthesis of estrogens from androgens. Inhibitors of aromatase have been developed for the treatment of estrogen-dependent breast cancer. However, small molecular agonists of aromatase, which would be useful to locally promote estrogen biosynthesis for the prevention of estrogen deficiency-induced diseases, are rarely reported. In this study, we established a nonradioactive assay for measuring aromatase activity by using human ovarian granulosa KGN cells and identified two estrogen biosynthesis-promoting compounds, egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae. The compounds also promoted estrogen biosynthesis in 3T3-L1 preadipocyte cells. Further study showed that neither compound affected the transcriptional and translational expression of aromatase in KGN cells, but that both significantly promoted the in vitro enzyme activity of recombinant expressed aromatase. Egonol gentiotrioside was also found to increase the serum estrogen level in ovariectomized rats. These results suggest that these two compounds may promote estrogen biosynthesis through the allosterical regulation of aromatase activity. Egonol gentiobioside and egonol gentiotrioside are, therefore, valuable targets for structural modification and warrant further investigation for their potential as novel pharmaceutical tools for the prevention of estrogen deficiency-induced diseases. (c) 2012 Elsevier B.V. All rights reserved.
学科主题	Pharmacology & Pharmacy
收录类别	SCI
资助信息	National Natural Science Foundation of China [20932007, 30572221, 30900769]; West Light Foundation of Chinese Academy of Sciences; National New Drug Innovation Major Project of China [2011ZX09307-002-02]
语种	英语
WOS记录号	WOS:000307815800034
公开日期	2013-07-03
内容类型	期刊论文
源URL	[http://210.75.237.14/handle/351003/23881]
专题	成都生物研究所_天然产物研究
推荐引用方式 GB/T 7714	Lu, Danfeng,Yang, Lijuan,Li, Qilin,et al. Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase[J]. EUROPEAN JOURNAL OF PHARMACOLOGY,2012,691(1-3):275-282.
APA	Lu, Danfeng,Yang, Lijuan,Li, Qilin,Gao, Xiaoping,Wang, Fei,&Zhang, Guolin.(2012).Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase.EUROPEAN JOURNAL OF PHARMACOLOGY,691(1-3),275-282.
MLA	Lu, Danfeng,et al."Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase".EUROPEAN JOURNAL OF PHARMACOLOGY 691.1-3(2012):275-282.