Isolation of linoleic acid as an estrogenic compound from the fruits of Vitex agnus-castus L. (chaste-berry).

Autor: J. Liu, J. E. Burdette, Y. Sun, S. Deng, S. M. Schlecht, W. Zheng, D. Nikolic, G. Mahady, R. B. van Breemen, H. H. S. Fong, J. M. Pezzuto, J. L. Bolton, N. R. Farnsworth
Zdroj: Phytomedicine; Feb2004, Vol. 11 Issue 1, p18-23, 6p
Abstrakt: A methanol extract of chaste-tree berry (Vitex agnus-castus L.) was tested for its ability to displace radiolabeled estradiol from the binding site of estrogen receptors alpha (ERα) and beta (ERβ). The extract at 46 ± 3 μg/ml displaced 50% of estradiol from ERα and 64 ± 4 μg/ml from ERβ. Treatment of the ER+ hormone-dependent T47D:A18 breast cancer cell line with the extract induced up-regulation of ERβ mRNA. Progesterone receptor (PR) mRNA was upregulated in the Ishikawa endometrial cancer cell line. However,chaste-tree berry extract did not induce estrogendependent alkaline phosphatase (AP) activity in Ishikawa cells. Bioassay-guided isolation, utilizing ER binding as a monitor,resulted in the isolation of linoleic acid as one possible estrogenic component of the extract. The use of pulsed ultrafiltration liquid chromatography-mass spectrometry, which is an affinity-based screening technique, also identified linoleic acid as an ER ligand based on its selective affinity, molecular weight, and retention time. Linoleic acid also stimulated mRNA ERβ expression in T47D:A18 cells, PR expression in Ishikawa cells, but notAPactivity in Ishikawa cells. These data suggest that linoleic acid from the fruits of Vitex agnus-castus can bind to estrogen receptors and induce certain estrogen inducible genes. [ABSTRACT FROM AUTHOR]
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