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)

Uteroglobin was obtained from 5 day pregnant rabbits and purified to homogeneity by Sephadex G 75 and DEAE-cellulose chromatographies. Progesterone binding to uteroglobin was decreased by lyophilization and enhanced by SH-reducing agents. Dithiothreitol was more effective than dithioerythritol, and beta-mercaptoethanol was only active at 25 to 100 mM concentrations. SH-blocking agents (iodoacetate, iodoacetamide, phydroxymercuribenzoate and, dithiobisnitrobenzoic acid) inhibited binding. In the absence of SH-reducing agents only one in every 500 uteroglobin molecules bound the hormone, whereas under optimal conditions (20 mM dithiothreitol) one in every two molecules bound progesterone. There was no significant difference in equilibrium dissociation constants under these two conditions. Uteroglobin had a relatively high affinity for progesterone (KD=4.1 X 10(-7)M) but a threefold higher affinity for 5alpha-pregnane-3,20-dione (KD=1.3 X 10(-7)M). Estradiol was bound but non-specifically with a very low affinity, and its binding was not enhanced by SH-reducing agents. Hormonal specificity of binding to uteroglobin was different from that of binding to rabbit uterine progesterone receptor. Various synthetic progestagens (chlormadinone acetate, norethisterone, R5020) were bound to the latter but not to the former protein. Diethylstilbestrol had some affinity (15% of that of progesterone) for uteroglobin and no affinity for the progesterone receptor. Uteroglobin incubated in the presence or absence of cofactors (NADH and NADPH) with or without dithiothreitol did not metabolize progesterone.
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PMID:Interaction of uteroglobin with progesterone, 5alphapregnane-3,20-dione and estrogens. 1 Oct 93

Gonadotropin secretion in cryptorchid and castrate rams and the acutve been determined. Rams made cryptorchid at 6 weeks of age had increased serum levels of luteinizing hormone (LH) and follicle stimulating hormone (FSH) when determined at 9 months of age. These levels approached those of the castrate animal; and yet serum levels of testosterone (T) were unchanged. Even though mean serum LH concentrations were elevated sixfold to eightfold over those of intact ram levels, a temporal relationship between this hormone and T was observed similar to that reported in the intact ram. Intramuscular injections of dihydrotestosterone had no effect on circulating levels of LH or FSH in either cryptorchid or castrate rams, whereas T effectively reduced these gonadotropins in castrate but not in cryptorchid rams. Only estradiol-17beta (E2) was effective in both cryptorchid and castrate rams. Estradiol was a potent inhibitor of LH secretion; however, its effect on FSH levels was less dramatic. This suggests that testicular products other than E2 may be important in the regulation of FSH production and/or release. Importantly, the inhibition of LH secretion lasted less than 12 h; whereas, the negative effects of E2 on FSH secretion lasted 72 to 144 h. In conclusion, results from this study show that T is not the single factor responsible for regulation of LH and FSH secretion in male sheep. Estradiol may be an important regulator of gonadotropin secretion, but 5alpha-reduction plays no apparent role in this process.
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PMID:Gonadotropin secretion in cryptorchid and castrate rams and the acute effects of exogenous steroid treatment. 1 31

Serial plasma unconjugated estradiol-17 beta was measured by a radioimmunoassay method in 26 cases of hypertensive disorder of pregnancy, 13 cases of poor obstetric history and 4 cases of intra-uterine growth retardation. There was considerable overlap of hormonal values between pregnancies, resulting in delivery of normal fetuses and those with dysmature fetuses. Serial estimation of estradiol-17 beta were not found to be useful in the prediction of intra-uterine death, although low values were obtained after fetal death has occurred. Estradiol-17 beta estimation appeared to be an unreliable index of fetoplacental function.
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PMID:Plasma estradiol-17 beta as an index of fetoplacental function. 1 13

Simultaneous pituitary and ovarian responses to acute stimulation (100 mcg iv injection) with luteinizing hormone-releasing hormone (LH-RH) in normal women at different times of the menstrual cycle were determined and the results were compared with those obtained in women with anuvulation from different causes. There were 12 normal women, 2 women who had had surgical oophorectomy, 2 who were taking combined hormonal contraceptives, 1 with amenorrhea following pelvic irradiation, 1 with gonadal dysgenesis, and 2 with anorexia nervosa. There were also 12 patients with secondary amenorrhea without detectable pathology. All patients received an iv injection of 100 mcg of synthetic LH-RH. In the normal patients basal LH levels were significantly (p .05) higher on Days 13-14 of the cycle than on Days 4-5. In all 3 phases of the cycle, LH reached peak poststimulation levels within 60 minutes after LH-RH injection. Castrate women showed basal LH levels and LH response profiles similar to normals. There were no estadiol or progesterone responses in this group. Women using hormonal contraception showed low basal levels of both gonadotropins with poststimulation LH response but no follicle stimulating hormone response. Estradiol response in this group was slightly lower and more sustained than in normal women. In patients with ovarian amenorrhea, responses were similar to those in castrated women. In patients with anorexia nervosa findings were normal.
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PMID:Pituitary and ovarian response to acute stimulation with LH-RH in normal and anovulatory women. 1 16

This study has characterized two new enzymatic hydroxylase activities specific for 5 alpha-androstane-3 beta, 17 beta-diol (3 beta-diol) in the rat ventral prostate: 5 alpha-androstane-3 beta, 17 beta-diol 6 alpha-hydroxylase (6 alpha-hydroxylase) and 5 alpha-androstane-3 beta, 17 beta-diol 7 alpha-hydroxylase (7 alpha-hydroxylase). Both of these irreversible hydroxylase activities require NADPH and are localized in the microsomal fraction of the prostate. The apparent Km for 3 beta-diol is 2.5 microM for both the 6 alpha- and 7 alpha-hydroxylase activities. The apparent Km for NADPH is 7.6 microM for the 6 alpha-hydroxylase and 7.0 microM for the 7 alpha-hydroxylase. The pH optimum for both activities is 7.4. Several steroid inhibitors of these hydroxylase activities in vitro were identified including cholesterol, progesterone, and estradiol. Estradiol was found in vitro to be a noncompetitive inhibitor (Ki = 5 microM). Injection of estradiol into intact male rats, simultaneously receiving exogenous testosterone, also produced a significant lowering of the 6 alpha-plus 7 alpha-hydroxylase activities. Both the 6 alpha- and 7 alpha-hydroxylase were found to be androgen sensitive. Following castration there is a rapid decrease in both activities.
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PMID:Characterization of two new enzymatic activities of the rat ventral prostate: 5 alpha-androstane-3 beta, 17 beta-diol 6 alpha-hydroxylase and 5 alpha-androstane-3 beta, 17 beta-diol 7 alpha-hydroxylase. 3 13

Estradiol and testosterone both lowered endogenous liver glycogen and at 20-fold higher doses impaired triamcinolone acetonide mediated glyconeogenesis in adult adrenalectomized male rats. Neither steroid influenced liver tyrosine transaminase although tryptophan pyrrolase activity was depressed by testosterone. Progesterone increased liver tryptophan pyrrolase but did not influence other parameters. Cortexolone did not alter either of these processes whereas cortisol induced both enzymes and, at much higher dose levels, gluconeogenesis. Binding of 3H-triamcinolone acetonide to its cytoplasmic receptor in vitro was left unaffected in presence of 20-fold greater concentration of either sex steroid but almost totally abolished by cold, homologous molecules. Similar results were obtained by 3H-cortisol except that estradiol partially competed for 3H-cortisol binding sites even at 20-fold greater concentrations of cold estradiol. Separation on DEAE-cellulose-52 and Ultrogel 44 columns revealed binding of all steroids to macromolecules of comparable physicochemical properties although the ratios of binding to the various subpopulations of the receptor were a function of the steroid in question. These results are discussed in terms of sex steroid binding to different moieties of a complex, heterogeneous, polymorphic protein rather than inhibition of binding to the active configuration acquired in presence of an inducer.
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PMID:Search for antiglucocorticoid activity in rat liver in vivo. 4 49

1. Male flounders receiving 100 micrograms estradiol each second day were fully induced to vitellogenin synthesis within 11 days, while fishes given 5 micrograms doses continued to accumulate vitellogenin in the serum at a progressive rate through 17 days. 2. Liver DNA per unit fish remained constant, while RNA per unit fish in flounders given 100 and 5 micrograms doses attained values 80 and 25% respectively, above the values found in control animals. 3. Liver RNA per unit DNA increased at maximal rate within 6 days in fishes receiving 100 micrograms doses. RNA synthesis continued at a progressive rate through 17 days in fishes given 5 micrograms doses of estradiol. 4. Liver protein per unit DNA elevated at a plateau 60% above control within 6 days with 100 micrograms doses. Doses of 5 micrograms had only little effect on liver protein. 5. Estradiol had a lipogenic effect on the liver. Cellular lipid rose 120 and 60% above control after treatment with 100 and 5 micrograms respectively. 6. Liver dry weight per unit DNA increased 60 and 55% above control with 100 and 5 micrograms doses respectively. Cellular hypertrophy in fishes receiving the smaller dose was primarily associated with an increase in lipid concentration, while protein and lipid contributed almost equally to cellular growth in fishes receiving the high dose.
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PMID:Dose response kinetics of serum vitellogenin, liver DNA, RNA, protein and lipid after induction by estradiol-17 beta in male flounders (Platichthys flesus L.). 9 87

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

Estrogens have been examined in the plasma of diploid and triploid newts Pleurodeles waltlii. Estradiol-17 beta (E2) and estrone (E1) were determined by radioimmunoassay, before and after enzymatic hydrolysis of the conjugates. Total (t) and unconjugated (u) E2 levels were positively correlated (E2u = 0.478 35 E2t + 0.579 98; r = 0.883), but no correlation was detected between E1 levels. No statistical difference was found for the estrogen levels between the different experimental lots of diploid newts (E2t = 7.5 +/- 0.37 ng/ml, E2u = 4.3 +/- 0.20 ng/ml, E1t = 2.19 +/- 0.08 ng/ml, E1t = 0.41 +/- 0.02 ng/ml) but every estrogen level was lower in the triploid group (E2t = 1.8 +/- 0.60, E2u = 1.0 +/- 0.18, E1t = 1.4 +/- 0.13, E1u = 0.3 +/- 0.04 ng/ml). This difference is discussed in relation to lower fertility of the triploid females.
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PMID:[Plasma estrogens in Pleurodeles waltlii. Comparison between diploid and triploid females]. 11 5

Consumption of vitamin A and cytochrome P 450 by pregnant Rat is more important than in non pregnant and ovariectomised Rat. Estradiol implant in ovariectomised female has some, but slighter, influence only on retinol. These physiological situations have no action on the hepatic levels of tocopherols (total and alpha). These results are discussed.
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PMID:[Vitamin A consumption in pregnant and non pregnant rats, and in castrated rats receiving or not receiving estradiol or pregnenolone; relation to tocopherol and cytochrome P-450]. 11 10


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