Egonol gentiobioside and egonol gentiotrioside from Styrax perkinsiae promote the biosynthesis of estrogen by aromatase
文献类型：期刊论文
| 作者 | Lu, Danfeng ; Yang, Lijuan ; Li, Qilin ; Gao, Xiaoping ; Wang, Fei ; Zhang, Guolin |
| 刊名 | EUROPEAN JOURNAL OF PHARMACOLOGY
 |
| 出版日期 | 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 |
| 产权排序 | 1 |
| 通讯作者 | Wang, F (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Chengdu 610041, Peoples R China ; Zhang, Guolin |
| 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 |
| 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. |
入库方式： OAI收割
来源：成都生物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。