Flavonoid glycosides isolated from Epimedium brevicornum and their estrogen biosynthesis-promoting effects
Li F1; Du BW1; Wang L1; Pu WC1; Liu CL5; Liu HW6; Wang MK*1,2; Wang F*1; Lu DF1,3,7; Wu WX1,7
刊名Scientific Reports
2017
卷号7期号:X页码:e7760
关键词Scientific Reports
英文摘要Epimedium brevicornum Maxim has a long history of use in the treatment of estrogen deficiency-related diseases. However, the chemical constituents and mechanism of action of this medicinal plant are not fully understood. In the present study, we isolated four new isoprenylated flavonoid glycosides, as well as 16 known flavonoids (13 isoprenylated flavonoids), from this plant. The chemical structures of the new flavonoid glycosides were elucidated by extensive spectroscopic analysis. The new compounds 1-4 were potent promoters of estrogen biosynthesis in human ovarian granulosa-like KGN cells. ZW1, an isoprenylated flavonoid analogue and a specific inhibitor of phosphodiesterase 5 (PDE5), was synthesized and used to explore the mechanism of the isoprenylated analogues on estrogen biosynthesis. ZW1 treatment increased estrogen production by upregulation of aromatase mRNA and protein expression. ZW1 increased the phosphorylation of cAMP response element-binding protein (CREB). Further study showed that the inhibition of PDE5 by ZW1 increased estrogen biosynthesis partly through suppression of phosphodiesterase 3 (PDE3). Our results suggested that the isoprenylated flavonoids from E. brevicornum may produce beneficial health effects through the promotion of estrogen biosynthesis. PDE5 warrants further investigation as a new therapeutic target for estrogen biosynthesis in the prevention and treatment of estrogen-deficiency related diseases.
语种英语
资助机构This work was supported by the National Natural Science Foundation of China (grants 21372214, 21561142003, 21550110193), Science & Technology Department of Sichuan Province (grants 2014JQ0028, 2016HH0073), CAS President’s International Fellowship Initiative (No. 2015PB061), Research Foundation of State General Administration of The People’s Republic of China for Quality Supervision and Inspection and Quarantine (No. 2015IK180), the West Light Foundation of Chinese Academy of Sciences, the Key Project of Education Department of Sichuan Province Natural Science Foundation (No. 14ZA0293), and Program of the Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province (No. SCTZ201304). ; This work was supported by the National Natural Science Foundation of China (grants 21372214, 21561142003, 21550110193), Science & Technology Department of Sichuan Province (grants 2014JQ0028, 2016HH0073), CAS President’s International Fellowship Initiative (No. 2015PB061), Research Foundation of State General Administration of The People’s Republic of China for Quality Supervision and Inspection and Quarantine (No. 2015IK180), the West Light Foundation of Chinese Academy of Sciences, the Key Project of Education Department of Sichuan Province Natural Science Foundation (No. 14ZA0293), and Program of the Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province (No. SCTZ201304). ; This work was supported by the National Natural Science Foundation of China (grants 21372214, 21561142003, 21550110193), Science & Technology Department of Sichuan Province (grants 2014JQ0028, 2016HH0073), CAS President’s International Fellowship Initiative (No. 2015PB061), Research Foundation of State General Administration of The People’s Republic of China for Quality Supervision and Inspection and Quarantine (No. 2015IK180), the West Light Foundation of Chinese Academy of Sciences, the Key Project of Education Department of Sichuan Province Natural Science Foundation (No. 14ZA0293), and Program of the Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province (No. SCTZ201304). ; This work was supported by the National Natural Science Foundation of China (grants 21372214, 21561142003, 21550110193), Science & Technology Department of Sichuan Province (grants 2014JQ0028, 2016HH0073), CAS President’s International Fellowship Initiative (No. 2015PB061), Research Foundation of State General Administration of The People’s Republic of China for Quality Supervision and Inspection and Quarantine (No. 2015IK180), the West Light Foundation of Chinese Academy of Sciences, the Key Project of Education Department of Sichuan Province Natural Science Foundation (No. 14ZA0293), and Program of the Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province (No. SCTZ201304).
内容类型期刊论文
源URL[http://159.226.149.26:8080/handle/152453/12021]  
专题昆明动物研究所_动物模型与人类重大疾病机理重点实验室
通讯作者wangmk@cib.ac.cn; wangfei@ cib.ac.cn
作者单位1.Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, P. R. China
2.Key Laboratory of Mountain Ecological Restoration and Bioresource Utilization and Ecological Restoration Biodiversity Conservation, Key Laboratory of Sichuan Province, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, 610041, P. R. China
3.3 Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, 650223, P. R. China
4.Department of Chemistry, Faculty of Science and Technology, Pibulsongkram Rajabhat University, Phitsanulok, 65000, Thailand.
5.Key Laboratory of Exploitation and Study of Distinctive Plants in Education Department of Sichuan Province, Sichuan University of Arts and Science, Dazhou, 635000, P. R. China
6.Ningbo Entry-Exit Inspection and Quarantine Bureau Technical Center, Ningbo, 315012, P. R. China
7.University of Chinese Academy of Sciences, Beijing, 100049, P. R. China
推荐引用方式
GB/T 7714
Li F,Du BW,Wang L,et al. Flavonoid glycosides isolated from Epimedium brevicornum and their estrogen biosynthesis-promoting effects[J]. Scientific Reports,2017,7(X):e7760.
APA Li F.,Du BW.,Wang L.,Pu WC.,Liu CL.,...&wangfei@ cib.ac.cn.(2017).Flavonoid glycosides isolated from Epimedium brevicornum and their estrogen biosynthesis-promoting effects.Scientific Reports,7(X),e7760.
MLA Li F,et al."Flavonoid glycosides isolated from Epimedium brevicornum and their estrogen biosynthesis-promoting effects".Scientific Reports 7.X(2017):e7760.
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