Preventive effect of oral estetrol in a menopausal hot flush model

Holinka, Christian F.; Brincat, Mark; Bennink, Herjan J.T. Coelingh

doi:10.1080/13697130701822807

Cited by 45 publications

(29 citation statements)

References 31 publications

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“…To understand the contribution of estrogenic activity in reducing TST by S-equol, it is necessary to determine the correlation between the estrogenicity and the effect on TST using estradiol as a positive control. 36 If the TST-reducing effect by S-equol is greater than expected based on its estrogenicity, it is possible that the anti-inflammatory properties of equol 37 may also play a role. Administration of the cytokines interleukin (IL)-6 and IL-1A directly into the cerebral ventricle induces hyperthermia, 32 and serum IL-6 and IL-8 levels are increased in women with moderate and severe hot flush.…”

Section: Discussionmentioning

confidence: 98%

S-equol and the fermented soy product SE5-OH containing S-equol similarly decrease ovariectomy-induced increase in rat tail skin temperature in an animal model of hot flushes

Yoneda

Ueno²,

Uchiyama³

2011

Menopause

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Section: Discussionmentioning

confidence: 98%

S-equol and the fermented soy product SE5-OH containing S-equol similarly decrease ovariectomy-induced increase in rat tail skin temperature in an animal model of hot flushes

Yoneda

Ueno²,

Uchiyama³

2011

Menopause

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“…In well validated and predictive rat models E 4 behaves as an estrogen agonist in all tissues investigated, i. e. bone [16], vagina [21], myometrium [21], endometrium [21] and brain (hot flush [20] and ovulation inhibition [20 ,21]), except for breast tumor tissue where this steroid acts as an estrogen antagonist in the presence of E 2 [24].…”

Section: Discussionmentioning

confidence: 99%

“…The efficacy of E 4 in alleviating hot flushes was studied in an experimental rat model considered representative for menopausal vasomotor symptoms [20].…”

Section: Vasomotor Symptomsmentioning

confidence: 99%

Clinical applications for estetrol

Visser

Bennink

2009

The Journal of Steroid Biochemistry and Molecular Biology

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In this paper the potential clinical applications for the human fetal estrogen estetrol (E 4 ) are presented based on recently obtained data in preclinical and clinical studies. In the past E 4 has been classified as a weak estrogen due to its rather low estrogen receptor affinity. However, recent research has demonstrated that due to its favorable pharmacokinetic properties, especially the slow elimination and long half-life, E 4 is an effective orally bioavailable estrogen agonist with estrogen antagonistic effects on the breast in the presence of estradiol. Based on the pharmacokinetic properties, the pharmacological profile and the safety and efficacy results in human studies, E 4 seems potentially suitable as a drug for human use in applications such as hormone replacement therapy (vaginal atrophy and vasomotor

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“…Sin embargo, la dosis máxima de E4 utilizada en el estudio (3 mg/kg/día), tiene un efecto similar al control con etinilestradiol (EE), pero con una dosis 10 veces menor (0,3 mg/kg/día) sugiriendo una menor potencia al aplicar E4 en este modelo (11). Estos datos apoyan la supuesta efectividad que pudiera presentar el E4 en el manejo de la sintomatología vasomotora en la mujer posmenopáusica.…”

Section: Síntomas Vasomotoresunclassified

Estetrol: Desde Un Estrógeno Fetal Hasta El Tratamiento De La Menopausia

2009

Rev. chil. obstet. ginecol.

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RESUMENEstetrol es un esteroide estrogénico sintetizado exclusivamente por el hígado fetal, que traspasa a la circulación materna por la placenta. Descrito por primera vez por Diczfalusy en 1965. Desde esa fecha se han realizado diversas investigaciones preclínicas. En los últimos años, el interés por el estetrol ha aumentado, dado el logro de su síntesis en el laboratorio y la demostración de su buena biodisponibilidad y larga vida media al administrarlo por vía oral a mujeres. Se presenta una revisión de su síntesis, metabolismo y de la información científica existente de sus diferentes efectos en los tejidos estrógeno sensibles en distintos modelos animales.PALABRAS CLAVE: Estetrol, efecto estrogénico, menopausia, terapia hormonal de reemplazo SUMMARYEstetrol is an estrogenic steroid synthesized exclusively by the fetal liver. It crosses over from the placenta to the maternal circulation. It was first described in 1965 by Diczfalusy and from this date onwards, several preclinical investigations have been carried out. In recent years, the interest for estetrol has been growing due to its laboratory synthesis and the demonstration of its good bioavailability together with its long half life, when administered orally to women. A review of its synthesis, metabolism and existing scientific information on its different effects on estrogen sensitive tissues, in a variety of animal models, is here presented. KEY WORDS: Estetrol, estrogenic effect, menopause, hormonal replacement therapy INTRODUCCIÓNEl esteroide estrogénico estetrol (E4) fue descrito en 1965 por Diczfalusy y cols (1). En los años siguientes diversos investigadores demostraron que esta molécula con 4 grupos hidroxilo (C18H24O4) era sintetizada en forma exclusiva por el hígado fetal durante el embarazo humano (2-3) y traspasada a la circulación materna por la placenta (Figura 1).El E4 puede ser detectado ya a las 9 semanas de embarazo en la orina materna alcanzando altas concentraciones en el plasma materno en el segundo trimestre con un aumento sostenido hasta el momento del parto (4). Los niveles de E4 no conjugado en el plasma fetal en el momento del parto son 12 a 19 veces mayores que en la madre. La concentración en el líquido amniótico corresponde a un tercio de la fetal, pero 5 -6 veces mayor que la del plasma materno (5). Casi no sufre cambios metabólicos, siendo eliminado por la orina como monoglucuronido, no participando de la circulación entero-hepática. REV CHIL OBSTET GINECOL 2009; 74(2): 123 -126

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Preventive effect of oral estetrol in a menopausal hot flush model

Abstract: Estetrol is effective in alleviating hot flushes in an experimental animal model considered representative for studying menopausal hot flushes (vasomotor symptoms). In this model, the potency of estetrol is 10-fold lower compared to ethinylestradiol.

Cited by 45 publications

References 31 publications

S-equol and the fermented soy product SE5-OH containing S-equol similarly decrease ovariectomy-induced increase in rat tail skin temperature in an animal model of hot flushes

S-equol and the fermented soy product SE5-OH containing S-equol similarly decrease ovariectomy-induced increase in rat tail skin temperature in an animal model of hot flushes

Clinical applications for estetrol

Estetrol: Desde Un Estrógeno Fetal Hasta El Tratamiento De La Menopausia

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