Competitive Studies with Dehydroepiandrosterone Sulfate and 16α-Hydroxydehydroepiandrosterone Sulfate in Cultured Human Choriocarcinoma JEG-3 Cells: Effect on Estrone, 17β-Estradiol,and Estriol Secretion*

Here, we report the effects of estrogen and the selective estrogen receptor modulator (SERM) levormeloxifene on adrenocortical measures in ovariectomized female cynomolgus monkeys ( Macaca fascicularis). Animals were randomized into one of five treatment groups, each containing 23 to 26 animals: (1) placebo, (2) 0.016 mg/kg 17β-estradiol (E2), (3) 0.5 mg/kg levormeloxifene (L1), (4) 1.0 mg/kg levormeloxifene (L2), and (5) 5.0 mg/kg levormeloxifene (L3). Treatments were administered orally each day for 18 mo. All doses of levormeloxifene resulted in adrenal weights at least 50% greater than placebo ( p < .0001 for all). The target dose of levormeloxifene (L2) resulted in higher serum concentrations of cortisol (+63%), dehydroepiandrosterone-sulfate (+73%), and androstenedione (+37%) compared with the placebo group ( p < .05 for all). In contrast, E2 resulted in no significant differences in adrenal weight or adrenocortical steroids. Oral E2 and all SERM doses resulted in similar reductions in serum gonadotropins and at least threefold greater uterine weight versus placebo ( p < .0001 for all). Results indicate that the SERM levormeloxifene, in contrast to E2, may have robust stimulatory effects on adrenocortical hormones in a postmenopausal model. These findings warrant further investigation into long-term SERM effects on adrenocortical function.

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Trichomonas vaginalis: Dehydroepiandrosterone sulfate and 17β-estradiol alter NTPDase activity and gene expression

Experimental Parasitology ◽

10.1016/j.exppara.2010.01.029 ◽

2010 ◽

Vol 125 (3) ◽

pp. 187-195 ◽

Cited By ~ 6

Author(s):

Caroline Rückert ◽

Cristiane dos Santos Stuepp ◽

Barbara Gottardi ◽

Jessica Rosa ◽

Julia Cisilotto ◽

...

Keyword(s):

Gene Expression ◽

Trichomonas Vaginalis ◽

Dehydroepiandrosterone Sulfate ◽

17Β Estradiol

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Metabolism of Dehydroepiandrosterone Sulfate and Estrone-Sulfate by Human Platelets

Physiological Research ◽

10.33549/physiolres.932323 ◽

2012 ◽

pp. 381-388 ◽

Cited By ~ 4

Author(s):

A. GARRIDO ◽

Y. MUÑOZ ◽

W. SIERRALTA ◽

L. VALLADARES

Keyword(s):

Organic Anion ◽

Dehydroepiandrosterone Sulfate ◽

Human Platelets ◽

Steroid Sulfatase ◽

Organic Anion Transporting Polypeptide ◽

Estrone Sulfate ◽

High Affinity ◽

Sulfatase Activity ◽

17Β Estradiol ◽

Estrone Sulphate

The aim of the present research was to study the uptake of DHEAS, and to establish the intracrine capacity of human platelets to produce sex steroid hormones. The DHEAS transport was evaluated through the uptake of [3H]-DHEAS in the presence or absence of different substrates through the organic anion transporting polypeptide (OATP) family. The activity of sulfatase enzyme was evaluated, and the metabolism of DHEAS was measured by the conversion of [3H]-DHEAS to [3H]-androstenedione, [3H]-testosterone, [3H]-estrone and [3H]-17β-estradiol. Results indicated the existence in the plasma membrane of an OATP with high affinity for DHEAS and estrone sulphate (E1S). The platelets showed the capacity to convert DHEAS to active DHEA by the steroid-sulfatase activity. The cells resulted to be a potential site for androgens production, since they have the capacity to produce androstenedione and testosterone; in addition, they reduced [3H]-estrone to [3H]-17β-estradiol. This is the first demonstration that human platelets are able to import DHEAS and E1S using the OATP family and to convert DHEAS to active DHEA, and to transform E1S to 17β-estradiol.

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Dehydroepiandrosterone Sulfate Is Neuroprotective when Administered Either before or after Injury in a Focal Cortical Cold Lesion Model

Endocrinology ◽

10.1210/en.2005-0693 ◽

2006 ◽

Vol 147 (2) ◽

pp. 683-686 ◽

Cited By ~ 28

Author(s):

Gabriella Juhász-Vedres ◽

Éva Rózsa ◽

Gabriella Rákos ◽

Márton B. Dobszay ◽

Zsolt Kis ◽

...

Keyword(s):

Primary Motor Cortex ◽

Vasogenic Edema ◽

Dehydroepiandrosterone Sulfate ◽

Therapeutic Benefit ◽

Neuroprotective Activity ◽

Triphenyltetrazolium Chloride ◽

Cold Lesion ◽

Focal Brain Injury ◽

The Central Nervous System ◽

17Β Estradiol

Dehydroepiandrosterone and its sulfate (DHEAS) are sex hormone precursors that exert marked neurotrophic and/or neuroprotective activity in the central nervous system. The present study evaluated the effects of DHEAS and 17β-estradiol (E2) in a focal cortical cold lesion model, in which DHEAS (50 mg/kg, sc) and E2 (35 mg/kg, sc) were administered either as pretreatment (two subsequent injections 1 d and 1 h before lesion induction) or posttreatment (immediately after lesion induction). The focal cortical cold lesion was induced in the primary motor cortex by means of a cooled copper cylinder placed directly onto the cortical surface. One hour later, the animals were killed, the brains cut into 0.4-mm-thick slices, and the sections stained with 1% triphenyltetrazolium chloride. The volume of the hemispheric lesion was calculated for each animal. The results demonstrated that the lesion area was significantly attenuated in both the DHEAS- and E2- pre- and posttreated groups and that in the presence of letrozole, a nonsteroidal aromatase inhibitor, no neuroprotection was observed, suggesting that the beneficial effect of DHEAS on the cold injury might depend on the conversion of DHEAS to E2 within the brain. It is concluded that even a single posttraumatic administration of DHEAS may be of substantial therapeutic benefit in the treatment of focal brain injury with vasogenic edema.

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