Metabolic fate of intraperitoneally administered 5-androstene-3β,17β-DIOL, estradiol-17β and their combination in the immature female rat
| Autor: | L.G. Van Doorn, E. Valstar, J. Poortman |
|---|---|
| Rok vydání: | 1981 |
| Předmět: |
Androstenediol
medicine.medical_specialty Estrone medicine.drug_class Uterus Estrogen receptor Iodoacetates Biology Biochemistry Iodoacetamide Basal (phylogenetics) chemistry.chemical_compound Endocrinology Internal medicine Androstenediols medicine Animals Biotransformation Estradiol Rats Cytosol medicine.anatomical_structure chemistry Estrogen Female Nucleus Injections Intraperitoneal Subcellular Fractions Hormone |
| Zdroj: | Journal of Steroid Biochemistry. 14:657-661 |
| ISSN: | 0022-4731 |
| Popis: | Previous experiments in our laboratory have shown that the intraperitoneal administration to immature female rats of 1000 μg 5-androstene-3β,17β-diol (ADIOL) leads to effects, which are almost identical to those of 2.5 μg estradiol-17β (E 2 ) in several estrogen target organs. Moreover, the combination of these two hormones displayed strongly enhanced effects, which were shown to be related to a biphasic nuclear translocation of the estrogen receptor. The present investigation was undertaken to establish whether these effects of ADIOL could be due to its aromatization and to assess the contribution of the two steroids to the biphasic nuclear translocation of the estrogen receptor, which occurred with the combination of the two hormones. The distribution of E 2 and ADIOL over the plasma and the subcellular compartments of the uterus (cytosol and nucleus) was studied in experiments in which the steroids were administered in the same way as in our previous experiments. The conversion of ADIOL to E 2 in the plasma was found to be maximally 0.02%. No increase in the levels of E 2 in the cytosol and nuclear fraction was found. The addition of ADIOL to E 2 caused a protracted elevation of plasma and nuclear E 2 levels relative to those found with E 2 alone. Most probably this was caused by inhibition of the metabolic degradation of E 2 . This protracted elevation of E 2 levels, possibly together with the high levels of ADIOL, explain the occurrence of the second wave of nuclear translocation of the estrogen receptor observed in our earlier experiments. Unexpectedly we found that the immature female rat has a relatively high basal plasma level of estrone (E 1 ) as compared to the E 2 level. After injection of E 2 there was a large conversion of E 2 to E 1 . |
| Databáze: | OpenAIRE |
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