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

Fourteen esters (formate, acetate, propionate, butyrate, hexanoate, heptanoate, and benzoate) located at C-11 of 11 beta-hydroxyesterone and 11 beta-hydroxyestradiol-17 beta were synthesized and evaluated for uterotropic and gonadotropin release inhibition in rats, as well as their ability to displace (3H) estradiol-17 beta from the rat uterine cytosolic estrogen receptor. The most potent uterotropic agent was 11 beta-formoxyestrone which was 1,625 or 2,500 times as active as 11 beta-hydroxyesterone in the uterotropic or gonadotropin release inhibition assay, respectively. 11 beta-Formoxyestrone was 7.5 times as uterotropic as estradiol-17 beta and equal to estradiol-17 beta in inhibiting gonadotropin release. However, the most potent inhibitor of gonadotropin release was 11 beta-acetoxy-estradiol-17 beta which had 133% of the activity of estradiol-17 beta, although it had only 38% of the activity of estradiol-17 beta in the uterotropic assay. Esters larger than the acetoxy group showed sharply decreased activities in either assay. Despite the high estrogenic potency of the 11-formates or 11-acetates, they were rather weak (6% to 35% as active as estradiol-17 beta) in displacing (3H) estradiol-17 beta from the rat uterine cytosolic estrogen receptor.
Steroids 1984 Jan
PMID:Structure-activity relationships of estrogens: effects of esterification of the 11 beta-hydroxyl group. 652 30

Levels of magnal estrogen and progesterone receptors during egg formation in the hen were determined. Hens were sacrificed at various times after ovulation and magnal receptor levels were determined by tritiated hormone binding assays. A coincident increase in nuclear estrogen receptor and decrease in cytosol estrogen receptor 2 to 4 h postoviposition was suggestive of in vivo receptor translocation. At 12 to 16 h postoviposition cytosol progesterone receptor increased 2-fold and subsequently declined during the time of preovulatory progesterone surge (8 h to 6 h prior to expected ovulation). These data suggest that changes in circulating levels of estrogen and progesterone, associated with ovulation, are coordinated with oviductal function. This is reflected by fluxes of their respective oviductal receptors.
Steroids 1984 Mar
PMID:Magnal steroid hormone receptors during egg formation in the domestic hen. 652 43

The method of initiating dissociation of 3H-estradiol from the nuclear estrogen receptor of hen oviduct was found to have a profound effect on the dissociation rate. Likewise, prior exposure to charcoal or partial purification by ion-exchange chromatography had an effect on the dissociation rate. When the reaction was initiated by isotopic dilution with the addition of 1 microM unlabeled estradiol, dissociation of the complexes was rapid (t 1/2 approximately 3 min). When the reaction was initiated by the addition of charcoal to adsorb free steroid, the dissociation of the complexes proceeded slowly (t 1/2 approximately 30 min). Partial purification of the receptors by DEAE-Sephacel chromatography or 15 min exposure to charcoal at 0 degree C prior to initiation of the dissociation reaction by isotopic dilution produced a form of the receptor that exhibited an intermediate dissociation rate (t 1/2 approximately 10 min). The partially purified receptor that exhibited an intermediate dissociation rate was reconverted to the rapidly dissociating form in a reconstitution experiment. These data raise the possibility of a nuclear substance that regulates the rates of estrogen dissociation.
Steroids 1984 Oct
PMID:The effect of exposure to charcoal and ion-exchange chromatography on the dissociation rate of estrogen from the nuclear estrogen receptor of hen oviduct. 654 69

The mechanisms underlying the differences in uterotrophic potency between 2- and 4-hydroxyestrogens were explored. Doses of estradiol (E2)(10 micrograms/kg), 2-OHE2 (500 micrograms/kg) and 4-OHE2 (100 micrograms/kg) sufficient to induce near maximal cell nuclear estrogen receptor (ERn) binding were injected subcutaneously into 26 day old female rats. Uterine ERn concentrations declined more rapidly after 2-OHE2 than after E2 or 4-OHE2. E2 and 4-OHE2 both elicited a significant increase in uterine wet weight, measured at 24-36 hrs after injection. 2-OHE2 had no significant effect and neither synergized with nor antagonized the effects of simultaneously administered E2 or 4-OHE2. Under in vitro conditions at 25 degrees C, 2-hydroxyestrone (2-OHE1) and 2-OHE2 both dissociated from the receptors more rapidly than either their parent monophenolic estrogens or the corresponding 4-hydroxyestrogens. These results suggest that differences in estrogenic potency between 2- and 4-hydroxyestrogens may partly be a function of the dissociation kinetics of their estrogen receptor complexes.
Steroids 1983 May
PMID:Kinetics of catechol estrogen-estrogen receptor dissociation: a possible factor underlying differences in catechol estrogen biological activity. 665 96

Incubations of p-nitrophenyl fatty acyl esters and estradiol-17 beta fatty acyl 17-esters with porcine esterase, human mammary tumor cytosol and rat uterine cytosol leads to ester hydrolysis of compounds with short chain fatty acids. Esters with long chain fatty acids show no hydrolysis except in the presence of Tween 80. Short chain fatty acid esters have a higher binding potency to the estrogen receptor than long chain fatty acid esters. Extraction of the nuclear receptor peak sedimenting at 4.6S and identification of the steroid showed that about 90% of the radioactivity was associated with estradiol and only 10% with estradiol esters. These studies show that estradiol fatty acyl esters act as a storage form from which estradiol is released by enzymatic hydrolysis.
Steroids 1983 Oct
PMID:Significance of lipoidal estradiol in human mammary tumors. 667 46

Nuclear and cytoplasmic binding sites for estradiol (E2-17 beta) in granulosa cells of immature rats were characterized. These binding sites for estrogen were high affinity, low capacity with an affinity constant (Kd) of 1.9 X 10(-10)M (binding capacity, Ro = 80 pM) for nuclear sites and a Kd = 3.5 X 10(-10) M (Ro = 45 pM) for cytosol sites. Binding was specific for biologically active estrogens. The estrogen receptor in granulosa cells is a protein and heat-labile as treatment with protease or pre-incubation at 37 degrees C for 1 h significantly diminished binding. RNase and DNase had no effect on estrogen binding. Sedimentation coefficients for nuclear and cytosol binding components were 5S and 8S respectively, similar to values obtained with uteri. Finally, translocation was demonstrated after a s.c. injection of E2-17 beta. Forty-five minutes post-injection, cytosol binding sites for estradiol were depleted concomitant with accumulation of nuclear binding sites. We concluded that granulosa cells of immature rats have binding sites specific for estradiol which have characteristics similar to the classical estrogen receptor in uteri.
Steroids 1983 Oct
PMID:Identification of estrogen receptors in granulosa cells of immature rats. 667 47

The 9 beta isomers of estradiol-17 beta, estradiol-17 a estrone and 17-ethinylestradiol-17 beta were synthesized and compared with their 9a-counterparts in the rat uterine cytosol estrogen receptor, uterotropic, and gonadotropin release inhibition assays. Except for 17-ethinyl-9 beta-estradiol-17 beta which was as active as its 9a isomer in the uterotropic assay, none of the 9 beta estrogens exhibited any biological activity which was equal to or greater than their 9a counterparts. For examples, 9 beta-estradiol-17 beta was 1/10 as active as estradiol-17 beta, and 9 beta-estrone was 1/4 as active as estrone in the uterotropic assay.
Steroids 1983 Nov
PMID:Structure-activity relationships of 9 beta-estrogens. 668 Sep 29

Following a single intraperitoneal injection of 0.5 microgram estradiol-17 beta (E2) into immature female rats uterine ornithine decarboxylase (ODC) activity increased to a peak at 4 hours postinjection. It decreased to intermediate levels by 6 hours and remained elevated until returning to control levels by 18 hours. When either 0.5 microgram estriol (E3) or 0.05 microgram E2 was injected, activity increased to a 4 hour ODC peak then decreased to control levels by 10 hours. The decrease to intermediate levels of ODC activity after dosing with 0.5 microgram E2 occurred at the same time activity decreased to control levels following treatment with either 0.05 microgram E2 or 0.5 micrograms E3. S-Adenosyl methionine decarboxylase (SAMDC) activity had increased by 4 hours following an injection of 0.5 microgram E2 and remained elevated until 16 hours then decreased to control levels. An injection of 0.05 microgram E3 stimulated only a 4 hour peak after which time SAMDC decreased to control levels by 14 hours. After an injection of 5.0 microgram E2 SAMDC activity had increased by 4 hours and remained elevated for the remainder of the experiment (16 hours). Decreases in ODC activity following 4 and 10 hours may reflect a decrease in nuclear estrogen receptor levels. The ODC activity seen here following 0.5 microgram E2 injection is similar in timing to that seen in other proliferating systems and may be due to a common mechanism.
Steroids 1983 Dec
PMID:Polyamine biosynthetic decarboxylase activities following estradiol-17 beta or estriol stimulation of the immature rat uterus. 668 Sep 31

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

Total concentrations of estradiol-17 beta (E2) and progesterone (P) receptors (R) were measured in the endometrium of rhesus monkeys (Macaca mulatta) during the normal menstrual cycle. The endometrium was collected at abdominal fundal hysterotomy on days 8, 12, 15, 18 and 24 of the menstrual cycle. Visual inspection of the ovaries and measurement of E2, P, follicle stimulating hormone (FSH) and luteinizing hormone (LH) provided assuredness of normal ovarian function. Exchange procedures were used in order to measure the total concentrations of E2R and PR in nuclear and cytosol fractions. The pattern of estrogen receptor showed a slight increase in the cytosol and nuclear concentrations at the preovulatory interval. Later, the total E2R concentration was decreased when P increased during the luteal phase. Cytosol PR synthesis was parallel to the serum E2 increase during the late follicular phase. Secretion of P by the corpus luteum was accompanied by a rapid nuclear translocation and concomitant decrease in cytoplasmic PR. Thereafter the total PR concentration declined during the second half of the luteal phase. These findings in monkey endometrium are similar to those reported for human endometrium during the normal menstrual cycle and further establish the utility of these surrogate primates in investigations indicative of human endometrial function.
Steroids 1980 Apr
PMID:Patterns of estrogen and progesterone receptors in monkey endometrium during the normal menstrual cycle. 676 83


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