Recent advances on the action of estrogens and progestogens in normal and pathological human endometrium

Pasqualini, Jörge R.; Chétrite, G.

doi:10.1515/hmbci.2010.027

Cited by 2 publications

(2 citation statements)

References 202 publications

(195 reference statements)

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“…Other studies indicate that endometrial carcinoma is not, or only minimally, increased by 3 years of tibolone treatment in postmenopausal women [59] (for a review, see [60] ).…”

Section: Discussionmentioning

confidence: 99%

“…The cellular radioactivity uptake was determined in the ethanolic supernatant. After evaporation of the organic phase, the extracts were redissolved in 50 µ L ethanol, and the qualitative analysis and quantitative evaluation of E 1 and E 2 were carried out after isolation by thin-layer chromatography on silica gel 60 …”

Section: Isolation and Quantifi Cation Of [ 3 H]-e 1 From Normal Or Cmentioning

confidence: 99%

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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

Chétrite¹,

Cortés-Prieto

Pasqualini³

2011

Hormone Molecular Biology and Clinical Investigation

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“…Other studies indicate that endometrial carcinoma is not, or only minimally, increased by 3 years of tibolone treatment in postmenopausal women [59] (for a review, see [60] ).…”

Section: Discussionmentioning

confidence: 99%

Section: Isolation and Quantifi Cation Of [ 3 H]-e 1 From Normal Or Cmentioning

confidence: 99%

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

Chétrite¹,

Cortés-Prieto

Pasqualini³

2011

Hormone Molecular Biology and Clinical Investigation

Self Cite

View full text Add to dashboard Cite

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Biological responses of progestogen metabolites in normal and cancerous human breast

Pasqualini¹,

Chétrite

2010

Hormone Molecular Biology and Clinical Investigation

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At present, more than 200 progestogen molecules are available, but their biological response is a function of various factors: affinity to progesterone or other receptors, their structure, the target tissues considered, biological response, experimental conditions, dose, method of administration and metabolic transformations. Metabolic transformation is of huge importance because in various biological processes the metabolic product(s) not only control the activity of the maternal hormone but also have an important activity of its own. In this regard, it was observed that the 20-dihydro derivative of the progestogen dydrogesterone (Duphaston®) is significantly more active than the parent compound in inhibiting sulfatase and 17β-hydroxysteroid dehydrogenase in human breast cancer cells. Estrone sulfatase activity is also inhibited by norelgestromin, a norgestimate metabolite. Interesting information was obtained with a similar progestogen, tibolone, which is rapidly metabolized into the active 3α/3β-hydroxy and 4-ene metabolites. All these metabolites can inhibit sulfatase and 17β-hydroxysteroid dehydrogenase and stimulate sulfotransferase in human breast cancer cells. Another attractive aspect is the metabolic transformation of progesterone itself in human breast tissues. In the normal breast progesterone is mainly converted to 4-ene derivatives, whereas in the tumor tissue it is converted mostly to 5α-pregnane derivatives. 20α-Dihydroprogesterone is found mainly in normal breast tissue and possesses antiproliferative properties as well as the ability to act as an anti-aromatase agent. Consequently, this progesterone metabolite could be involved in the control of estradiol production in the normal breast and therefore implicated in one of the multifactorial mechanisms of the breast carcinogenesis process. In conclusion, a better understanding of both natural and synthetic hormone metabolic transformations and their control could potentially provide attractive new therapies for the treatment of hormone-dependent pathologies.

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Recent advances on the action of estrogens and progestogens in normal and pathological human endometrium

Cited by 2 publications

References 202 publications

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

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

Biological responses of progestogen metabolites in normal and cancerous human breast

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