Time dependency of uterine effects of naringenin type phytoestrogens in vivo

Abstract

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Activation of transgenic estrogen receptor-beta by selected phytoestrogens in a stably transduced rat serotonergic cell line

“…The strong estrogenic potency exhibited in RNDA cells is in accordance with the effects shown in other cell models and organs by our group and others [25,65,[73][74][75]. Hence, 8-PN seems to show strong affinity for both ER␣ and ER␤ [76], even though our data does not support ER selectivity in vivo.…”

“…These results are in contrast to Zierau et al, who reported a high measurable luciferase output in a dose-dependent manner in other cell models [25,65]. In addition, there are gene expression data indicating that 6-DMAN regulates the expression of several but not all ER target genes in the uterus of ovariectomized rats [25].…”

“…Those have been previously studied in our lab and with collaborators in an ER␣-dependent test systems in vitro and in animal experiments in vivo [25,28,33,[53][54][55][56].…”

“…Mechanistically, they have the ability to bind to different estrogen receptor subtypes. Functionally, they can show both estrogenic or anti-estrogenic properties depending on the circulating levels of endogenous estrogens and therefore may have a significant impact on human health [25].…”

“…The ability to chemically synthesize these compounds resulted in sufficient quantities to characterize them [32]. They also show low toxicity and weak cytostatic properties, allowing them to be utilized for in vitro and in vivo studies to evaluate their pharmacotherapeutic potential [25,33,35]. Nevertheless, conclusive data on their effects in the brain as well as on their transactivational activity on the ER␤ remain to be clarified.…”