Icariin from Epimedium brevicornum Maxim promotes the biosynthesis of estrogen by aromatase (CYP19)
Icariin from Epimedium brevicornum Maxim promotes the biosynthesis of estrogen by aromatase (CYP19)
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淫羊藿中的淫羊藿苷通过芳香酶 (CYP19) 促进雌激素的生物合成
DOI：
10.1016/j.jep.2012.11.031
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发表时间：
2013-02-13
影响因子：
5.4
通讯作者：
Wang, Fei
中科院分区：
文献类型：
--
作者：
Yang, Lijuan;Lu, Danfeng;Wang, Fei
民族药理学相关性：在中国和其他亚洲国家，淫羊藿长期用于治疗骨质疏松症。然而，这种药用植物的抗真菌活性背后的机制尚未完全了解。研究目的：本研究旨在研究五种广泛使用的抗骨质疏松药用植物的作用（淫羊藿、菟丝子、骨碎补、何首乌、女贞子）对雌激素产生的影响，并鉴定负责雌激素生物合成促进作用的生物活性化合物。人卵巢颗粒样KGN细胞用于评价雌激素生物合成，并通过基于磁性颗粒的酶联免疫吸附测定（ELISA）试剂盒定量17 β-雌二醇的产生。通过实时定量逆转录聚合酶链反应（qRT-PCR）测定芳香化酶的mRNA表达，并通过蛋白质印迹法检测芳香化酶的蛋白表达。结果：在5种抗雌激素药物中，淫羊藿提取物对KGN细胞的雌激素合成有明显的促进作用。淫羊藿苷是淫羊藿中的主要成分，被鉴定为具有促进雌激素生物合成作用的活性成分。淫羊藿苷以浓度和时间依赖性方式促进KGN细胞中雌激素的生物合成，并增强芳香化酶的mRNA和蛋白质表达，芳香化酶是脊椎动物中雄激素转化为雌激素的唯一酶。结论：淫羊藿苷具有促进成骨细胞UMR-106雌激素合成和碱性磷酸酶活性的作用，提示淫羊藿苷可用于防治骨质疏松症。(C)2012爱思唯尔爱尔兰有限公司保留所有权利。
Ethnopharmacological relevance: Epimedium brevicornum Maxim has long been used for the treatment of osteoporosis in China and other Asian countries. However, the mechanism behind the antiosteoporotic activity of this medicinal plant is not fully understood.Aim of the study: The present study was designed to investigate the effects of five widely used antiosteoporotic medicinal plants (Epimedium brevicornum, Cuscuta chinensis, Rhizoma drynariae, Polygonum multiflorum, and Ligustrum lucidum) on the production of estrogen, and identify the bioactive compounds responsible for the estrogen biosynthesis-promoting effect.Materials and methods: Human ovarian granulosa-like KGN cells were used to evaluate estrogen biosynthesis, and the production of 17 beta-estradiol was quantified by a magnetic particle-based enzyme-linked immunosorbent assay (ELISA) kit. Further, the mRNA expression of aromatase was determined by a quantitative real-time reverse-transcription polymerase chain reaction (qRT-PCR), and the protein expression of aromatase was detected by western blotting. The activity of alkaline phosphatase (ALP) in rat osteoblastic UMR-106 cells was measured using p-nitrophenyl sodium phosphate assay.Results: Among the 5 antiosteoporotic medicinal plants, the extract of Epimedium brevicornum was found to significantly promote estrogen biosynthesis in KGN cells. Icariin, the major compound in Epimedium brevicornum, was identified to be the active compound for the estrogen biosynthesis-promoting effect. Icariin promoted estrogen biosynthesis in KGN cells in a concentration- and time-dependant manner and enhanced the mRNA and protein expressions of aromatase, which is the only enzyme for the conversion of androgens to estrogens in vertebrates. Further study showed that icariin also promoted estrogen biosynthesis and ALP activity in osteoblastic UMR-106 cells.Conclusions: These results show that the promotion of estrogen biosynthesis is a novel effect of Epimedium brevicornum, and icariin could be utilized for the prevention and treatment of osteoporosis. (C) 2012 Elsevier Ireland Ltd. All rights reserved.