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Title: Estrogenic activities of sesame lignans and their metabolites on human breast cancer cells
Authors: Prisna Pianjing
Apinya Thiantanawat
Nuchanart Rangkadilok
Piyajit Watcharasit
Chulabhorn Mahidol
Jutamaad Satayavivad
Chulabhorn Research Institute
Asian Institute of Technology Thailand
Mahidol University
Chulabhorn Graduate Institute
Keywords: Agricultural and Biological Sciences;Chemistry
Issue Date: 12-Jan-2011
Citation: Journal of Agricultural and Food Chemistry. Vol.59, No.1 (2011), 212-221
Abstract: Sesame lignans (sesamin, sesamolin) and their metabolites (enterodiol, ED; enterolactone, EL; and sesamol) have been evaluated for their estrogenic activities. ED and EL have been indicated to have estrogenic/antiestrogenic properties on human breast cancer cells; however the estrogenic activities of sesamin, sesamolin and sesamol have not been reported. In the present study, estrogenic potencies of sesame lignans and their metabolites were determined by estrogen responsive element (ERE) luciferase reporter assay in T47D cells stably transfected with ERE-luc (T47D-KBluc cells) and quantifying pS2 and progesterone receptor gene expression in T47D cells. All tested compounds except ED possessed ability of ERE activation with a very low potency compared to estradiol (E2). These effects were abolished by coincubating tested compounds with 1 μM ICI 182 780, suggesting that estrogen receptors were directly involved in their ERE activations. Among tested compounds, sesamol showed the highest ability in ERE induction. The coincubation of increasing concentration of E2 (10 -12 -10 -6 M) with 10 μM of tested compounds resulted in a downward shift of E2-ERE dose-response curves. In contrast, at the low concentration of E2 (10 -12 M), sesamin and sesamol significantly exhibited additive effects on the E2 responses. The inhibitory effect in a dose-dependent manner was also observed when 1-100 μM sesamol was coincubated with 1 nM E2. Sesamin, sesamol and EL significantly induced pS2 gene expression whereas only sesamol could significantly induce progesterone receptor gene. The data obtained in this study suggested that sesame lignans and their metabolites possess weak estrogenic/antiestrogenic activity. © 2010 American Chemical Society.
ISSN: 15205118
Appears in Collections:Scopus 2011-2015

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