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铁角蕨提取物及分离化合物的体外雌激素活性

In vitro estrogenic activity of Asplenium trichomanes L. extracts and isolated compounds.

作者信息

Dall'Acqua Stefano, Tomè Franca, Vitalini Sara, Agradi Elisabetta, Innocenti Gabbriella

机构信息

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Padova, Padova, Italy.

出版信息

J Ethnopharmacol. 2009 Apr 21;122(3):424-9. doi: 10.1016/j.jep.2009.02.012. Epub 2009 Feb 14.

DOI:10.1016/j.jep.2009.02.012
PMID:19429306
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Asplenium trichomanes was used as an expectorant, anti-cough remedy, laxative, emmenagogue, abortifacient and for irregular menses.

AIM OF THE STUDY

To investigate the in vitro estrogenic activity of Asplenium trichomanes extracts and isolated compounds and their ability to activate ERalpha and ERbeta.

MATERIALS AND METHODS

Leaves infusion (IF), decoction (DC) and methanol extract (ME) were prepared. MCF7/EREluc cell line which expresses endogenous ERalpha, and SK-NBE cells transiently transfected with the estrogen receptors (ERalpha and ERbeta) were used for the estrogenic activity assays. Phytochemical investigations were performed (CC, HPLC, etc.) and structure of isolated compounds were achieved on the basis of 1D and 2D NMR techniques and HR-MS spectrometry.

RESULTS

IF and ME were active in our MCF7 model; selectivity for the ERbeta receptor was observed in the SK-NBE test. Two new phenol derivatives, 4-vinyl-phenol-1-O-[alpha-L-rhamno(1-->6)-beta-d-glucopyranosyde] (1) and kaempferol-3-O-alpha-[2'acetyl]-arabinofuranosyl-7-O-alpha-L-rhamnopyranoside (2) were isolated with six known compounds (3-8). Compounds 2-4, 7 and 8 showed selectivity for the activation of the ERbeta receptor although with a moderate activity compared with 17-beta-estradiol.

CONCLUSION

Further investigations about the estrogenic effects of this plant are needed but our data can, at least in part, explain some of its traditional use as emmeagogue.

摘要

民族药理学相关性

铁角蕨被用作祛痰剂、止咳药、泻药、通经药、堕胎药以及用于治疗月经不调。

研究目的

研究铁角蕨提取物和分离化合物的体外雌激素活性及其激活雌激素受体α(ERα)和雌激素受体β(ERβ)的能力。

材料与方法

制备了叶浸剂(IF)、煎剂(DC)和甲醇提取物(ME)。使用表达内源性ERα的MCF7/EREluc细胞系以及瞬时转染了雌激素受体(ERα和ERβ)的SK-NBE细胞进行雌激素活性测定。进行了植物化学研究(柱色谱、高效液相色谱等),并基于一维和二维核磁共振技术以及高分辨质谱法确定了分离化合物的结构。

结果

IF和ME在我们的MCF7模型中具有活性;在SK-NBE试验中观察到对ERβ受体的选择性。分离出两种新的酚类衍生物,4-乙烯基苯酚-1-O-[α-L-鼠李糖(1→6)-β-D-吡喃葡萄糖苷](1)和山奈酚-3-O-α-[2'-乙酰基]-阿拉伯呋喃糖基-7-O-α-L-鼠李糖苷(2)以及六种已知化合物(3 - 8)。化合物2 - 4、7和8显示出对ERβ受体激活的选择性,尽管与17-β-雌二醇相比活性适中。

结论

需要对这种植物的雌激素作用进行进一步研究,但我们的数据至少可以部分解释其作为通经药的一些传统用途。

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