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Query: UMLS:C0338671 (Steroids)
 9,479 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The specific binding of 5 alpha-dihydroprogesterone (5 alpha-DHP), progesterone and R5020 to anterior pituitary nuclear extracts was studied using ovariectomized rats treated with estradiol benzoate and progesterone. The binding equilibrium association constant for 5 alpha-dihydroprogesterone with different preparations of nuclear extract ranged from 4.0 +/- 0.54 microM-1 to 59 +/- 10 microM-1. The association constants for progesterone and R5020 were 0.39 +/- 0.81 nM-1 and 1.5 +/- 0.15 nM-1, respectively. The binding of 5 alpha-DHP was specific in that it could be competed only by R5020, progesterone and 5 alpha-DHP and not by other progesterone metabolites and other hormonal steroids tested. With [3H]-progesterone and [3H]R5020 as ligands the most efficient competitors also were R5020, progesterone and 5 alpha-DHP. Estrogen priming of ovariectomized rats consistently and significantly increased the number of binding sites for all three progestins and subsequent progesterone treatment enabled their detection at higher levels in the nuclei.
Steroids
PMID:Binding of 5 alpha-dihydroprogesterone and other progestins to female rat anterior pituitary nuclear extracts. 356 86

The estrogenic properties of estrazinol hydrobromide (EZ), a water-soluble estrogen, were compared with those of Premarin (PR), another water-soluble estrogen preparation consisting of conjugated equine estrogens. Estradiol-17beta, estra-1,3,5(10)-triene-3,17beta-diol (E), and ethinyl estradiol, 17alpha-ethinyl-1,3,5 (10)-estratriene-3,17beta-diol (EE) were used as reference standards. Subcutaneous progesterone (400 mcg) given to rabbits primed with comparable subcutaneous doses of either E or EE produced full secretory changes of the endometrium, while such a transformation could not be elicited in orally primed animals regardless of the estrogen used. The biological profile or orally administered EZ was very similar to that of oral EE and different from oral PR. Howerver, the oral EZ-induced morphological changes of the rabbit endometrium appeared somewhat different from those produced by oral EE. The findings indicated that following oral administration, EZ-induced endometrial transformation is more "normal" and/or adequate than the changes produced by either EE or PR.
Steroids Lipids Res 1973
PMID:Estrogenic profile on a water-soluble estrogen, estrazinol hydrobromide. 436

The subcellular distribution of the enzymes involved in the metabolism of norethynodrel (17 alpha-ethynyl-17 beta-hydroxy-estr-5(10)-en-3-one) to the 3alpha and 3beta diols (17 alpha-ethynyl-3alpha (or 3beta-17 beta-dihydroxy-estr-5(10)-ene) and 17 alpha-ethinyl estradiol was studied. The purity of the male rat liver subcellular fractions was evaluated by the use of marker enzymes. Sample sections were viewed by electron microscopy. The data showed that the cytosol fraction contained the highest relative specific activity for the hydroxysteroid dehydrogenases required for the formation of the diols. The cytosol fraction also contained the highest total activity. The enzymes required for the formation of ethinyl estradiol were distributed equally among mitochondrial and microsomal fractions, however, the highest relative specific activity was associated with the heavy microsomal fraction (18,000 g).
Steroids 1970 Oct
PMID:Metabolism of norethynodre, a 19-nor progestin: subcellular localization of enzyme activity. 439 62

Data on the urinary excretion and subsequent fractionation of radioactivity derived from 6,7-tritiated-17alpha-ethinyl estradiol (tritiated EE) are presented. Tritiated EE was administered orally to 9 women. 17alpha-ethinyl estradiol 2-methoxy-17alpha-ethinyl estradiol, 2 -hydroxy-17alpha-ethinyl estradiol 3-methyl ether, and D-homoestradiol-1 7abeta were identified as urinary metabolites by reverse isotope dilution. The extent of D-homoannulation was much less than that reported previously with rabbits.
Steroids 1970 May
PMID:Metabolism of radioactive 17alpha-ethynylestradiol by women. 491 66

The preparation of 9alpha, 11xi-tritiated 17alpha-ethinyl estradiol, mestranol, estradiol-17beta, and norethindrone are described. Estrone-3-methyl ether was employed as starting material, and ethinylation with lithium acetylide-ethylene diamine resulted in 95% mestranol. Demethylation of mestranol with boron tribromide at 0 degrees resulted in 92% 17alpha-ethinyl estradiol. Dimethylsulfoxide was the choice of reagent for the condensation reaction which was complete at room temperature in about 4 hours. The usually less than 3% of unreacted 17-oxo product was removed by Girard separation. Demethylation of methyl ether with boran tribromide in methylene chloride resulted in an excellent yield of 17alpha-ethinyl estradiol-9alpha, 11xi-tritium. 3-methoxyestra-1,3,5-trien-17-one-9alpha, 11xi-tritium was reduced with sodium bis(2-methoxyethoxy) aluminum hydride to the 17beta-hydroxy compound and subsequent demethylation resulted in estradiol-9alpha, 11xi-tritium. The general method of Ringold et al was employed for the preparation of 17beta-hydroxy-17alpha-ethinylestr-4-en-3-one. Improvements for small scale radiosynthesis are also presented.
Steroids 1971 Aug
PMID:Preparation of 9-alpha,11-xi-tritiated 17-alpha-ethynylestradiol, mestranol, estradiol-alpha-17-beta, and norethindrone. 512 20

Estrogen secretion and estrogen synthetase (aromatase) activity are stimulated in human trophoblast cells (JAr line) after addition of 1 mM dibutyryl cyclic AMP plus 1 mM theophylline (dbT) to the growth medium. The data given here show that (a) the aromatase specific activity in homogenized cells increases linearly over a 96 hr incubation period after addition of dbT; (b) addition of inhibitors of macromolecular synthesis, cycloheximide or actinomycin D, to the culture medium at the time of addition of dbT abolishes the stimulation of aromatase activity; (c) mixing dbT-grown cells, containing increased aromatase activity, with control cells does not result in an aromatase specific activity higher than the expected average, suggesting that dbT-grown cells do not contain a factor present in excess which serves to stimulate aromatase in control cells; and (d) NADPH, included in vitro in the aromatase assay or incubated with the cells for 48 hr as well as being present in the aromatase assay, has no stimulatory effect on aromatase specific activity in homogenized cells.
Steroids 1981 Jan
PMID:Macromolecular synthesis is required for stimulation of estrogen synthetase activity by dibutyryl cyclic AMP plus theophylline in choriocarcinoma cell culture. 626 25

By using 20 meter wall-coated open tubular glass capillary columns of high stability, analysis of methyl ester, methyloxime trimethylsilyl ether derivatives of estrogen glucuronides had been achieved. Relative retention times of five glucuronide conjugates on OV-1 stationary phase are reported. Estrogen sulfates conjugated at the 3-position were shown to be quantitatively hydrolyzed and derivatized in a single trimethylsilylation step, and this method of direct derivatization was compared to two solvolysis methods. These analytical methods could be further developed to allow rapid and quantitative analysis of estrogens in biological fluids, and may prove particularly useful for analysis of labile compounds.
Steroids 1981 Nov
PMID:Derivatization of estrogen conjugates for analysis by capillary gas chromatography. 627 75

The production of progesterone, estrogen and androgen as well as the metabolism of radiolabelled progesterone by various cellular components of rat ovarian follicles were studied. Granulosa (G), theca (T), recombined granulosa plus theca (G+T) and intact follicular wall (FW) of ovaries from immature rats treated with pregnant mare serum gonadotropin (8 IU) were cultured for 24 h in the presence or absence of [4-14C]progesterone. The estrogen and androgen accumulation when calculated per follicle was several fold greater in FW than in G, T, or G+T preparations. The conversion of radiolabelled progesterone to its identified C21 catabolites (20 alpha-hydroxy-4-pregnen-3-one and 3 alpha-hydroxy-5 alpha-pregnan-20-one) was significantly lower in FW than in G+T incubations. Conversely, the metabolism of radiolabelled progesterone to androsterone was several fold greater in FW than in G+T incubations. Addition of hydroxyflutamide to FW incubations significantly decreased estrogen production and increased the conversion of radiolabelled progesterone to androsterone. Estrogen production by follicular wall may be enhanced by androgenic stimulation of aromatase activity as well as by a structure-dependent factor(s) of a yet unknown nature, both of which may decrease progesterone catabolism to biologically inactive progestins while promoting progesterone conversion to androgens and eventually to estrogens.
Steroids 1984 Oct
PMID:Steroidogenic capabilities of various compartments of rat ovarian follicles in culture. 654 71

We have investigated the action of high doses of androgens in Gobius niger L., a marine teleostean fish, by characterizing specific steroid receptors in liver and by assaying the plasma vitellogenin concentration under different hormonal treatments. Estrogen and androgen receptors were characterized in the liver nuclear extracts according to their binding specificity. The maximum binding capacity was 25 fmoles/mg protein for the estrogen and androgen receptors. In vivo, high doses of DHT()increased the concentration of plasmatic vitellogenin as assayed by immunodiffusion while low doses were inefficient. In spite of a similar number of estrogen and androgen nuclear receptor sites (25 fmoles/mg protein), DHT was at least 70 fold less active than E2 on yolk protein and vitellogenin induction both in male and female Gobius niger. In addition, the antiestrogen tamoxifen, which was inactive by itself, inhibited the E2 and the DHT induced accumulation of vitellogenin. Progesterone (2 mg/fish) was also totally inactive in inducing vitellogenin. We conclude that the induction of vitellogenin by DHT is mediated by the estrogen receptor rather than by the androgen receptor. In addition to the estradiol induced protein in rat uterus and to other estrogenic responses obtained by androgens in mammary cancer, fish vitellogenin is another estrogen regulated protein which can be induced by high doses of androgens.
Steroids 1980 Mar
PMID:Effect of androgen mediated by the estrogen receptor of fish liver: vitellogenin accumulation. 676 82

The effect of estrogens on hepatic beta-hydroxy-beta-methylglutaryl coenzyme A reductase activity and cholesterol in serum and liver of ovariectomized rats on normal diet 2% cholestyramine diet or 2% cholesterol diet was investigated. Estrogen administration to ovariectomized rats on normal diet resulted in increased reductase activity and was correlated with decreased serum cholesterol and increased liver cholesterol levels with mestranol (ME), ethinyl estradiol (EE) and estradiol benzoate (EB, 250 microgram) but increased serum and liver cholesterol levels with 25 microgram and 100 microgram EB administration. The increased stimulation of reductase activity by estrogen administration was abolished when rats were fed a 2% cholesterol diet. Cholestryramine feeding markedly increased reductase activity in livers of ovariectomized rats. These studies show that estrogens are not absolutely required for the stimulation of reductase activity and therefore is consistent with the model in which cholesterol functions as a feedback repressor of reductase activity.
Steroids 1981 Jun
PMID:Effect of estrogens on beta-hydroxy-beta-methylglutaryl coenzyme A reductase activity and cholesterol levels. 729 35


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