Department of Pharmacognosy and Natural Products Chemistry, Faculty of Pharmacy, National and Kapodistrian University of Athens, Panepistimiopoli Zografou, 15771 Athens, Greece.
Institute of Chemical Biology, National Hellenic Research Foundation, 48, Vassileos Constantinou Avenue, 11635 Athens, Greece.
Molecules. 2020 Nov 24;25(23):5507. doi: 10.3390/molecules25235507.
As part of our ongoing research on phytoestrogens, we investigated the phytochemical profile and estrogen-like activities of eight extracts from the aerial parts of four species of Greek flora using estrogen-responsive cell lines. Ethyl acetate and methanolic extracts of , and were obtained with accelerated solvent extraction and their phytochemical profiles were compared using ultra-high-performance liquid chromatography-high-resolution mass spectrometry (uHPLC-HRMS). Fourteen isoflavonoids, previously isolated from , were used as reference standards for their identification in the extracts. Thirteen isoflavonoids were detected in both extracts of and , while fewer and far fewer were detected in and respectively. The ethyl acetate extracts of and displayed 2.45- and 1.79-fold higher, respectively, estrogen-like agonist activity in Ishikawa cells compared to MCF-7 cells at pharmacologically relevant concentrations. Both these extracts, but not that of , contained mono- and di-β-d-glucosides of genistein as well as the aglycone, all three of which are known to display full estrogen-like activity at lower-than-micromolar concentrations. The possibility of using preparations rich in and/or extracts as a potentially safer substitute for low-dose vaginal estrogen for menopausal symptoms is discussed.
作为我们正在进行的植物雌激素研究的一部分，我们使用雌激素反应细胞系研究了来自希腊植物群的四个物种的空中部分的八种提取物的植物化学特征和类似雌激素的活性。使用加速溶剂提取法获得了 的乙酸乙酯和甲醇提取物，并使用超高效液相色谱-高分辨率质谱（uHPLC-HRMS）比较了它们的植物化学特征。从 中分离出的 14 种异黄酮被用作提取物中鉴定的参考标准。在 和 的两种提取物中均检测到 13 种异黄酮，而在 和 中则检测到较少和更少的异黄酮。与 MCF-7 细胞相比，在药理学相关浓度下， 和 的乙酸乙酯提取物在 Ishikawa 细胞中表现出 2.45 倍和 1.79 倍更高的类似雌激素激动剂活性。这两种提取物都含有金雀异黄素的单-β-d-葡萄糖苷和双-β-d-葡萄糖苷以及苷元，所有这三种物质在低于微摩尔浓度时均显示出完全的类似雌激素活性。讨论了使用富含 和/或 提取物的制剂作为绝经症状的低剂量阴道雌激素的潜在更安全替代品的可能性。
