Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: DrugBank:APRD00691 (EE2)
 7,802 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

In in vitro tests with lysosomes isolated from the liver and kidneys of castrated rats of both sexes the action of testosterone and beta-estradiol in concentrations of 3.76.10(-4)M on the activity of beta-glucosidase, beta-galactosidase and acid phosphatase was investigated. Testosterone is shown to reduce the total and free activity of the membrane-bound enzymes and to increase the release from the matrix lysosomes. Estradiol proved less active than is testosteron. The renal lysosomes in vitro are more sensitive to the action of sex hormones than are hepatic lysosomes. In the interaction of testosterone and estradiol with lysosomal membranes a sex specificity was revealed.
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PMID:[The effects of testosterone and estradiol on the activity of lysosomal enzymes in rat liver and kidneys]. 9 95

17beta-[6,7-3H]Estradiol (E2) was incubated with slices and homogenates of adult human renal tissue. The metabolites formed were identified by chromatography on DEAE-Sephadex, thin layer chromatography and crystallization with carrier steroids or steroid derivatives. The major metabolites formed by slices were estradiol-17-glucuronide (E217G), estrone sulfate and estradiol-3-sulfate. This is the first report of in vitro synthesis of estrogen sulfates by adult renal tissue. Minor quantities of the 3-glucuronides of estrone and estradiol were also found. An oxygen atmosphere appeared to stimulate the production of E217G. A time study with tissue slices showed similarities between the in vitro pattern of glucuronide synthesis and the excretion pattern of these compounds seen in earlier in vivo studies. Homogenates fortified with uridine diphosphoglucuronic acid formed the same pattern of glucuronide products but in lesser amounts. No sulfates were formed under these conditions. Testosterone did not act as a substrate in the experimental conditions used.
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PMID:In vitro synthesis of estrogen glucuronides and sulfates by human renal tissue. 16 18

Studies were conducted to further examine the mechanisms responsible for gonadal hormone effects on the rat adrenocortical 11beta-hydroxylase system. Despite higher concentrations of cytochrome P-450 and larger 11-deoxycorticosterone (DOC)-induced difference spectra in adrenal mitochondria from females than males, no sex difference in 11beta-hydroxylase activity was observed. The pregnenolone-induced difference spectrum, indicative of cholesterol binding to cytochrome P-450, also was similar in males and females. Testosterone administration to castrated males lowered both 11beta-hydroxylase activity and mitochondrial cytochrome P-450 content. Estradiol produced the opposite effects in castrated females. However, when given to ACTH-replaced hypophysectomized rats, neither testosterone nor estradiol affected cytochrome P-450 levels or the rate of 11beta-hydroxylation. These observations, taken with the known effects of estradiol and testosterone on ACTH secretion in rats and the effects of ACTH on 11beta-hydroxylation, indicate that gonadal hormone effects on the 11beta-hydroxylase system are mediated by ACTH.
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PMID:Relation of the pituitary gland to gonadal hormone effects on the adrenocortical 11beta-hydroxylase system in rats. 16 71

The effects of several steroid hormones on progesterone synthesis and cAMP accumulation in isolated bovine corpora luteal cells were investigated in an attempt to determine if any of the steroids would affect the basal level of these processes or their response to gonadotropin. Isolated bovine corpora luteal cells responded to LH with a significant (P less than 0.05) increase in progesterone synthesis and cAMP accumulation when incubated at 37 C for up to 1 h. Exogenous cAMP and analogs of cAMP also significantly stimulated steroidogenesis in these incubated cells. Stimulation of progesterone synthesis by 1 microgram/ml LH was significantly suppressed (P less than 0.05) in the presence of 5--10 microgram/ml estradiol. This inhibition appeared to be largely specific for 17beta-estradiol, in that other steroids such as estrone, estriol, 17alpha-estradiol, cortisol, and dihydrotestosterone were not inhibitory. Testosterone was found to be inhibitory, but it is uncertain if this effect was due to the androgen itself or to its conversion to estradiol. Estradiol did not affect the increase in endogenous cAMP caused by LH in these cells, but did inhibit the effect of exogenous dibutyryl cAMP on progesterone synthesis. The magnitude of this inhibition of the effect of dibutyryl cAMP was not, however, equal to the estradiol inhibition of the stimulation of progesterone synthesis by LH. These data indicate that estradiol, a possible physiological luteolytic agent, has a direct inhibitory action on the corpus luteum and produces its suppression by blocking the stimulatory effect of LH at a step after cAMP.
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PMID:Estradiol inhibition of luteinizing hormone-stimulated progesterone synthesis in isolated bovine luteal cells. 21 85

Nine ovarian Sertoli-Leydig tumors, showing varying degrees of differentiation, one pure ovarian Sertoli cell tumor, and one poorly differentiated stromal tumor of the testis, were examined for the presence of testosterone, estradiol and progesterone with an indirect immunoperoxidase method on formalin fixed paraffin embedded tissue. Clinically all nine patients with Sertoli-Leydig tumors had evidence of increased androgen production, manifested by either hirsutism or virilization; elevated serum testosterone was found in all four patients in whom it was measured. The patients with the pure ovarian Sertoli cell and testicular tumors were asymptomatic except for the presence of a mass. Testosterone was identified in Leydig cells in nine instances, in Sertoli cells in six, and in poorly differentiated spindle cells resembling the mesenchyme of the embryonic gonad in two. Cells with vacuolated cytoplasm, both Sertoli and Leydig cells, though positive for lipid were consistently negative for testosterone. Estradiol was present in Leydig cells in nine instances, in Sertoli cells in five, and in primitive gonadal stomal cells in two. The pattern of distribution was similar to that of testosterone but the intensity of the reaction for estradiol was generally less than that for testosterone. Progesterone was identified in Sertoli cells in one instance and was weakly positive in Leydig cells in three instances. The presence of testosterone and estradiol in both Sertoli and Leydig cells as well as in primitive spindle cells resembling those found in the embryonic gonad suggests that the latter cell is the precursor for both Sertoli and Leydig cells.
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PMID:An immunohistological study of steroid localization in Sertoli-Leydig tumors of the ovary and testis. 36 Dec 11

Eleven granulosa-theca tumors (seven pure granulosa and four with associated theca elements) were examined for the presence of estradiol, progesterone and testosterone using an indirect immunoperoxidase technique on formalin-fixed paraffin embedded tissue. In ten patients the endometrium was studied histologically and significant endometrial hyperplasia consistent with estrogen production by the tumors was found. Estradiol was localized in granulosa cells (nonluteinized) in all 11 cases and in luteinized theca cells in three of the four cases in which theca elements are present. In contrast, progesterone was always detected in luteinized theca cells and in granulosa cells in over one half the cases. Testosterone was also present in granulosa cells in just over half the cases but tended to be only weakly positive. The nonluteinized stromal cells were negative for all steroids. These results are compatible with the concept that in granulosa-theca tumors, both granulosa and theca cells can produce a wide range of steroid hormones but that the predominant steroid present in granulosa cells is estradiol, while progesterone is the predominant steroid in luteinized theca cells.
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PMID:Steroid localization in granulosa-theca tumors of the ovary. 37 57

Previous studies have demonstrated an important role for the pituitary gland in the regulation of hepatic drug and steroid metabolism. The present studies were carried out to determine the relationship between the pituitary gland and the actions of gonadal hormones on hepatic drug metabolism in rats. Testosterone administration to castrated male rats increased hepatic microsomal cytochrome P-450 concentrations and enhanced the rates of ethylmorphine demethylation and benzo(a)pyrene hydroxylation. Estradiol treatment, on the other hand, lowered cytochrome P-450 levels and decreased the rates of aniline, ethylmorphine and benzo(a)pyrene metabolism in orchiectomized rats. However, when given to hypophysectomized male rats, neither testosterone nor estradiol affected cytochrome P-450 levels or enzyme activities. Similarly, 5alpha-dihydrotestosterone administration increased hepatic drug metabolism only in the presence of the pituitary gland. The effects of both testosterone and estradiol were fully demonstrable in the absence of the thyroid or adrenal glands, excluding the need for either organ. The results indicate an absolute dependence on the pituitary gland for gonadal hormone (testosterone and estradiol) actions on hepatic mixed-function oxidases.
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PMID:Requirement of the pituitary gland for gonadal hormone effects on hepatic drug metabolism in rats. 75 12

After administration in situ of 3H-estradiol (8 X 10(-10) moles) to Guinea Pig fetuses (48-58 days of gestation) the presence of specific estradiol receptors in the cytosol and in the nuclear extracts of the fetal uterus has been demonstrated. The presence of these estradiol receptors was confirmed after incubation of the same fetal tissues with 3H-estradiol (8 X 10(-8) M). Estradiol has a significant competitive effect on the 3H-estradiol-complex; estrone and estriol also have an effect but less intense. Testosterone, cortisol, aldosterone have no effect. By ultracentrifugation in sucrose density gradient of the cytosol fraction a component with a sedimentation coefficient of 8.5-9 S is observed. The dissociation constant of the 3H-estradiol receptor has a high affinity (KD = 4 X 10(-10) M).
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PMID:[Cytosolic and nuclear estradiol receptors in the fetal guinea pig uterus]. 82 91

Protamine sulfate precipitation is used for the selective and quantitative assay of equilibrium binding constants. The association constant of dihydrotestosterone is 1 X 10(9)1/mole and the number of binding sites is 11.500/cell. The affinity of testosterone is slightly lower than that of dihydrotestosterone, whereas some synthetic androgens have a higher affinity in accordance with their biological activity. Estradiol, progesterone and antiandrogens can displace dihydrotestosterone from its receptor. The occupied cytosolic and nuclear binding sites can be measured by radioimmunoassay. After castration, the nuclear hormone-receptor complexes disappear with a half-life of 3 hours. The cytosol receptor decreases steadily between the first and the fourth day after castration, then increases spontaneously. Testosterone seems to inhibit the degradation and also to stimulate the synthesis of its own receptor. Radioautography shows that the receptor is present only in the epithelial cells.
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PMID:[Androgen binding proteins in the rat prostate: methodological problems and regulation (author's transl)]. 100 14

Dietary magnesium deficiency has been more damaging to the mast cells in females than in males. Estradiol at a dose of 1.5 mg per week for 4 weeks and testosterone at a dose of 3 mg per week in the males have resulted in lesser mast cell depletion in the magnesium-deficient animals. Large doses of testosterone have also improved in the condition of the skin, decreased the severity of other magnesium deprivation symptoms such as nephrocalcinosis, bone hyperplasia and nervous manifestations in the males. Testosterone has had no beneficial effect on mast cells of the females but the large dose has protected the kidney against nephrocalcinosis. Estrogen administration has aggrevated the production of kidney stones in the females.
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PMID:Protective action of sex hormones against mast cell depletion and other deleterious effects of magnesium deprivation. 122 26


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