Effect of tibolone and its principal metabolites (3α- and 3β-hydroxy, 3α-sulfate, and 4-ene derivatives) on estrone sulfatase activity in normal and cancerous human breast tissue

Chétrite, G.; Cortés-Prieto, J; Pasqualini, Jörge R.

doi:10.1515/hmbci.2011.121

Cited by 2 publications

(1 citation statement)

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“…In breast tissue, tibolone and its metabolites suppress sulfatase and 17β-HSD. These enzymes convert estrone sulfate, a form of inactive estrogen, into estradiol in the breast [ 30 31 32 ]. Additionally, 3-OH metabolite increase the activity of sulfotransferase, which converts estrone back to estrone sulfate [ 33 ].…”

Section: Tibolone and Breast Tissuementioning

confidence: 99%

Tibolone and Breast Cancer

Lee,

Yun,

Kim

et al. 2023

J Menopausal Med

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Tibolone, a selective tissue estrogenic activity regulator, is a synthetic steroid with distinct pharmacological and clinical characteristics in contrast to conventional menopausal hormone therapy. Tibolone induces estrogenic activity in the brain, vagina, and bone but remains inactive in the endometrium and breast. In particular, several studies have investigated whether tibolone usage increases the risk of breast cancer. This study aims to determine the effects of tibolone on the breast by focusing on the relation between tibolone use and breast cancer. Our investigation emphasizes recent studies, particularly those based on Asian populations.

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Section: Tibolone and Breast Tissuementioning

confidence: 99%

Tibolone and Breast Cancer

Lee,

Yun,

Kim

et al. 2023

J Menopausal Med

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The formation and transformation of hormones in maternal, placental and fetal compartments: biological implications

Pasqualini¹,

Chétrite

2016

Hormone Molecular Biology and Clinical Investigation

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The fetal endocrine system constitutes the earliest system developing in fetal life and operates during all the steps of gestation. Its regulation is in part dependent on the secretion of placental and/or maternal precursors emanating across the feto-maternal interface. Human fetal and placental compartments possess all the enzymatic systems necessary to produce steroid hormones. However, their activities are different and complementary: the fetus is very active in converting acetate into cholesterol, in transforming pregnanes to androstanes, various hydroxylases, sulfotransferases, while all these transformations are absent or very limited in the placenta. This compartment can transform cholesterol to C21-steroids, convert 5-ene to 4-ene steroids, and has a high capacity to aromatize C19 precursors and to hydrolyze sulfates. Steroid hormone receptors are present at an early stage of gestation and are functional for important physiological activities. The production rate of some steroids greatly increases with fetal evolution (e.g. estriol increases 500-1000 times in relation to non-pregnant women). Other hormones, such as glucocorticoids, in particular the stress hormone cortisol, adipokines (e.g. leptin, adiponectin), insulin-like growth factors, are also a key factor for regulating reproduction, metabolism, appetite and may be significant in programming the fetus and its growth. We can hypothesize that the fetal and placental factors controlling hormonal levels in the fetal compartment can be of capital importance in the normal development of extra-uterine life.

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Effect of tibolone and its principal metabolites (3α- and 3β-hydroxy, 3α-sulfate, and 4-ene derivatives) on estrone sulfatase activity in normal and cancerous human breast tissue

Abstract: This very significant inhibitory effect of tibolone and its principal metabolites on the enzyme involved in E2biosynthesis in the human breast provides interesting perspectives to study the biological responses of these compounds in trials with breast cancer patients.

Cited by 2 publications

References 59 publications

Tibolone and Breast Cancer

Tibolone and Breast Cancer

The formation and transformation of hormones in maternal, placental and fetal compartments: biological implications

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