Differential estrogen receptor binding of estrogenic substances: a species comparison

Matthews, Jason; Celius, Trine; Halgren, Robert G.; Zacharewski, Tim

doi:10.1016/s0960-0760(00)00126-6

Cited by 271 publications

(173 citation statements)

References 45 publications

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“…These results are in conflict with our earlier studies in which estradiol benzoate was administered to rats during the neonatal period of life between days 5 th and 11 th , showing that the numbers of undifferentiated and differentiating type A spermatogonia were increased at day 15 th [44]. One of the possible explanations for these discrepancies can be the use of an estradiol compound (estradiol benzoate) in our previous study instead of pure E, which binding affinity to the human and murine ERα seems to be 6-10-fold reduced in comparison with E [45]. As the ERα is the main ER expressed in the rat pituitary gland [46] the differences in the effects exerted by both substances could be attributed to their different action on gonadotropins secretion, suggesting inhibition of FSH by E. The selective suppression of FSH action in immature rats by passive immunisation caused a significant reduction in Sertoli cells and spermatogonia numbers, but spermatocytes were more resistant to this conditions [47].…”

Section: Discussionmentioning

confidence: 78%

Xenoestrogens diethylstilbestrol and zearalenone negatively influence pubertal rat's testis.

Filipiak

Walczak-Jędrzejowska²,

Oszukowska³

et al. 2010

Folia Histochem Cytobiol.

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Abstract:The aim of this study was to assess the impact of xenoestrogens: diethylstilbestrol (DES) and zearalenone (ZEA) on rat's pubertal testis and to compare it with the effect of natural estrogen -17β-estradiol (E). Male Wistar rats were daily, subcutaneously injected at 5 th -15 th postnatal days (p.d.) with E (1.25 or 12.5 μg) or DES (1.25 or 12.5 μg) or ZEA (4 or 40 μg) or vehicle. At 16 th p.d. testes were dissected, weighted, and paraffin embedded. Following parameters were assessed: diameter and length of seminiferous tubule, numbers of spermatogonia A+intermediate+B (A/In/B), preleptotene spermatocytes (PL), leptotene+zygotene+pachytene spermatocytes (L/Z/PA) and Sertoli cells per testis. Testes weight, seminiferous tubule diameter and length were decreased by both doses of E, DES and ZEA. DES effect was the strongest, but its influence on testis weight and seminiferous tubule length, on the contrary to E and ZEA, was not dose-dependent. Similarly, DES in both doses had the most severe negative impact on the number of germ and Sertoli cells. The negative influence of E on germ cells was less pronounced. The negative effect of ZEA was seen only after administration of the higher dose on spermatogonia number, while DES and E decreased A/In/B number more evidently. Sertoli cell number were decreased after both doses of E. ZEA40 decreased Sertoli cell number while ZEA4 had no effect. Conclusion: exposure of prepubertal male rat to DES has the strongest detrimental effect on the developing testis in comparison to E and ZEA. Both, E and DES, decreased number of germ and Sertoli cells, diminished seminiferous tubule diameter, length and testis weight. ZEA had much more weaker effect than the potent estrogens.

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Section: Discussionmentioning

confidence: 78%

Xenoestrogens diethylstilbestrol and zearalenone negatively influence pubertal rat's testis.

Filipiak

Walczak-Jędrzejowska²,

Oszukowska³

et al. 2010

Folia Histochem Cytobiol.

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“…The lack of effect of 17β-estradiol on arachidonic acid release observed in this report is in line with previous reported findings [69] and suggests that the estrogen receptors are not involved in PCB-induced arachidonic acid release. Also, the estrogen-like activities of CB47, CB52, CB118 and CB153 [70,71] does not correlate with their ability to induce eicosanoid synthesis and arachidonic acid release in platelets. Thus, the effects observed for anti-estrogens on CB52-induced eicosanoid formation suggest that PCBs might activate cPLA 2 -α by binding to a binding site distinct from the estrogen receptors.…”

Section: Discussionmentioning

confidence: 89%

Polychlorinated biphenyls induce arachidonic acid release in human platelets in a tamoxifen sensitive manner via activation of group IVA cytosolic phospholipase A2-α

Forsell

Olsson

Andersson

et al. 2005

Biochemical Pharmacology

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Polychlorinated biphenyls (PCBs) are stable compounds commonly found in nature as environmental pollutants. PCBs can affect the endocrine function of hormones such as steroid-hormones. Also, PCBs are known to be inducers of arachidonic acid release in various cells. We report, here, the effects of PCBs on eicosanoid formation, arachidonic acid release and cytosolic phospholipase A 2 -α(cPLA 2 -α) activation in human platelets. Ortho-substituted PCBs induced a time and dosedependent release of arachidonic acid and the concomitant formation of 12(S)-hydroxy-5,8-cis-10-trans-14-cis-eicosatetraenoic acid (12-HETE) and 12(S)-hydroxy-5-cis-8,10-transheptadecatrienoic acid (12-HHT) in human platelets. The release of arachidonic acid and the formation of 12-HETE was completely blocked by the cPLA 2 -α inhibitors AACOCF 3 or pyrrolidine-1. PCB-treatment of platelets demonstrated that the cPLA 2 -α protein as well as PLA 2 activity translocated to the membrane fraction, independent of a rise in intracellular Ca 2+ . Furthermore, electrophoretic gel mobility shift analysis of cPLA 2 -α on SDS-PAGE demonstrated a PCB-dependent phosphorylation of cPLA 2 -α. The effects of 17β-estradiol and two structurally unrelated anti-estrogens, nafoxidin and tamoxifen on PCB-induced arachidonic acid release in platelets were also investigated. Both nafoxidin and tamoxifen inhibited PCB-induced arachidonic acid release as well as 12-HETE and 12-HHT formation. Interestingly, platelets incubated with PCBs did not aggregate despite the fact that robust release of arachidonic acid was observed. In summary, these results demonstrate that certain PCBs induce activation of cPLA 2 -α independent of a rise in intracellular calcium and a robust release of arachidonic acid release with resulting eicosanoid formation in human platelets.

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“…It should be noted that the cell lines used in the present study contained human oestrogen receptors and a slight difference of the extracts to activate murine oestrogen receptors cannot be ruled out. However, studies by Matthews et al (2000) showed that human and mouse ER react in a very similar manner to steroidal and anti-oestrogenic compounds. We therefore expect that differences between activation of human versus murine oestrogen receptors by the steroid hormones tested will be quantitative rather than qualitative.…”

Section: Discussionmentioning

confidence: 99%

Detection of oestrogenic activity of steroids present during mammalian gestation using oestrogen receptor alpha- and oestrogen receptor beta-specific in vitro assays

Lemmen¹,

Brink²,

Legler³

et al. 2002

Journal of Endocrinology

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Numerous steroid hormones are present in the foetus but their potential to activate oestrogen receptor (ER) and/or is largely unknown. In this study, in vitro assays were developed to rapidly and specifically detect ER or ER activation by these steroid hormones. Our results showed that several oestrogen precursors and androgens are able to activate both ER and ER . Of special interest is that some of these precursors are able to activate ER and ER at concentrations that are present during human gestation. Moreover, some precursors (dehydroepiandrosterone (DHEA) and 17-hydroxylated pregnenolone sulphate) and androgens (5-androsten-3 ,16 ,17 -triol and testosterone) showed a more than 100-fold relative preference for ER transactivation over ER transactivation when compared with 17 -oestradiol. Due to their relatively high levels, the precursor steroids DHEA and pregnenolone may be of particular importance in the regulation of ER activity in vivo. To obtain information about the oestrogenic activity of the total pool of steroid hormones present during mammalian gestation, steroids were extracted from mouse embryos at different prenatal stages and assayed for oestrogenic activity in the established in vitro assays. Oestrogenic activity was detected in steroid extracts from all stages tested. This study has demonstrated that oestrogen receptor agonists are present in the murine embryo and that oestrogen precursors may contribute to the total pool of agonists during foetal life.

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Differential estrogen receptor binding of estrogenic substances: a species comparison

Cited by 271 publications

References 45 publications

Xenoestrogens diethylstilbestrol and zearalenone negatively influence pubertal rat's testis.

Xenoestrogens diethylstilbestrol and zearalenone negatively influence pubertal rat's testis.

Polychlorinated biphenyls induce arachidonic acid release in human platelets in a tamoxifen sensitive manner via activation of group IVA cytosolic phospholipase A2-α

Detection of oestrogenic activity of steroids present during mammalian gestation using oestrogen receptor alpha- and oestrogen receptor beta-specific in vitro assays

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