Plasma concentrations of unconjugated and conjugated estrogens and gonadotrophins following application of various estrogen preparations after oophorectomy and in the menopause

Strecker, J. R.; Lauritzen, C; Goessens, L.

doi:10.1016/0378-5122(79)90007-0

Cited by 23 publications

(5 citation statements)

References 5 publications

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“…In control experiments, we first confirmed that at 24-h post-treatment, E2 (10 nM) induced an increase of ∼2.0-fold in BRCA-1 protein expression compared with the vehicle control ( Figure 1A, B ). This dose of E2 was used throughout this study and was similar to that used previously to investigate regulation of BRCA-1 in human breast cancer cells ( 16 ) and detected in women around the human menstrual phase and in patients receiving E2 replacement therapy ( 31 , 32 ). In contrast, as documented previously ( 19 , 20 ), an equimolar dose (10 nM) of TCDD did not change basal BRCA-1 concentrations ( Figure 1B ), but it reduced (∼50%) E2-induced BRCA-1 expression ( Figure 1C, D ).…”

Section: Resultsmentioning

confidence: 99%

Genistein Prevents BRCA1 CpG Methylation and Proliferation in Human Breast Cancer Cells with Activated Aromatic Hydrocarbon Receptor

Romagnolo

Donovan

Papoutsis

et al. 2017

Current Developments in Nutrition

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Background: Previous studies have suggested a causative role for agonists of the aromatic hydrocarbon receptor (AhR) in the etiology of breast cancer 1, early-onset (BRCA-1)–silenced breast tumors, for which prospects for treatment remain poor. Objectives: We investigated the regulation of BRCA1 by the soy isoflavone genistein (GEN) in human estrogen receptor α (ERα)–positive Michigan Cancer Foundation-7 (MCF-7) and ERα-negative sporadic University of Arizona Cell Culture-3199 (UACC-3199) breast cancer cells, respectively, with inducible and constitutively active AhR. Methods: In MCF-7 cells, we analyzed the dose- and time-dependent effects of GEN and (–)-epigallocatechin-3-gallate (EGCG) control, selected as prototype dietary DNA methyltransferase (DNMT) inhibitors, on BRCA-1 expression after AhR activation with 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) and in TCDD-washout experiments. We compared the effects of GEN and EGCG on BRCA1 cytosine-phosphate-guanine (CpG) methylation and cell proliferation. Controls for DNA methylation and proliferation were changes in expression of DNMT-1, cyclin D1, and p53, respectively. In UACC-3199 cells, we compared the effects of GEN and α-naphthoflavone (αNF; 7,8-benzoflavone), a synthetic flavone and AhR antagonist, on BRCA1 expression and CpG methylation, cyclin D1, and cell growth. Finally, we examined the effects of GEN and αNF on BRCA1, AhR-inducible cytochrome P450 (CYP)-1A1 (CYP1A1) and CYP1B1, and AhR mRNA expression. Results: In MCF-7 cells, GEN exerted dose- and time-dependent preventative effects against TCDD-dependent downregulation of BRCA-1. After TCDD washout, GEN rescued BRCA-1 protein expression while reducing DNMT-1 and cyclin D1. GEN and EGCG reduced BRCA1 CpG methylation and cell proliferation associated with increased p53. In UACC-3199 cells, GEN reduced BRCA1 and estrogen receptor-1 (ESR1) CpG methylation, cyclin D1, and cell growth while inducing BRCA-1 and CYP1A1. Conclusions: Results suggest preventative effects for GEN and EGCG against BRCA1 CpG methylation and downregulation in ERα-positive breast cancer cells with activated AhR. GEN and flavone antagonists of AhR may be useful for reactivation of BRCA1 and ERα via CpG demethylation in ERα-negative breast cancer cells harboring constitutively active AhR.

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Section: Resultsmentioning

confidence: 99%

Genistein Prevents BRCA1 CpG Methylation and Proliferation in Human Breast Cancer Cells with Activated Aromatic Hydrocarbon Receptor

Romagnolo

Donovan

Papoutsis

et al. 2017

Current Developments in Nutrition

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“…They did not find any significant change in the ratio of estradiol to estrone. Strecker et al (17) stated that serum estrogen levels showed a significant rise following oral medication of the commonly used estrogen preparations in the menopause. They also noted a positive correlation between rising estrogen levels and suppressed gonadotropins during replacement therapy.…”

Section: Discussionmentioning

confidence: 98%

Effect of Natural Estrogen on the Serum Level of Follicle‐stimulating Hormone (Fsh), Estradiol and Estrone in Post‐menopausal Women and Its Effect on Endometrium

Varma

Everard

Hole

1985

Acta Obstet Gynecol Scand

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Serum FSH, estradiol and estrone levels were assayed in 35 post-menopausal women who received the three commonly available estrogen preparations Premarin, Progynova and Harmogen. The results were compared with the levels during treatment with Dixarit. Hormone levels did not change when Dixarit was used. The levels of estrone and estradiol increased significantly (p less than 0.01) when estrogen preparations were used. There was no abnormality in the endometrium at the end of the treatment period.

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“…A microporous polymer film membrane was used to maintain the fluxes of oestradiol and ethanol in the vicinity of 0.1 and 400 μg·cm −2 ·h −1 respectively. The sustained plasma levels of oestradiol obtained with the device overcame the key peak and trough profile limitation of the then marketed oestradiol ointment (Strecker et al, 1979). In 1984, the first transdermal oestradiol system reached the US market.…”

Section: Transdermal Oestradiol For Female Hormone Replacement Therapymentioning

confidence: 99%

Transdermal patches: history, development and pharmacology

Pastore

Kalia

Horstmann³

et al. 2015

British J Pharmacology

435

279

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Transdermal patches are now widely used as cosmetic, topical and transdermal delivery systems. These patches represent a key outcome from the growth in skin science, technology and expertise developed through trial and error, clinical observation and evidence-based studies that date back to the first existing human records. This review begins with the earliest topical therapies and traces topical delivery to the present-day transdermal patches, describing along the way the initial trials, devices and drug delivery systems that underpin current transdermal patches and their actives. This is followed by consideration of the evolution in the various patch designs and their limitations as well as requirements for actives to be used for transdermal delivery. The properties of and issues associated with the use of currently marketed products, such as variability, safety and regulatory aspects, are then described. The review concludes by examining future prospects for transdermal patches and drug delivery systems, such as the combination of active delivery systems with patches, minimally invasive microneedle patches and cutaneous solutions, including metered-dose systems.

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Plasma concentrations of unconjugated and conjugated estrogens and gonadotrophins following application of various estrogen preparations after oophorectomy and in the menopause

Cited by 23 publications

References 5 publications

Genistein Prevents BRCA1 CpG Methylation and Proliferation in Human Breast Cancer Cells with Activated Aromatic Hydrocarbon Receptor

Genistein Prevents BRCA1 CpG Methylation and Proliferation in Human Breast Cancer Cells with Activated Aromatic Hydrocarbon Receptor

Effect of Natural Estrogen on the Serum Level of Follicle‐stimulating Hormone (Fsh), Estradiol and Estrone in Post‐menopausal Women and Its Effect on Endometrium

Transdermal patches: history, development and pharmacology

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