Luteinizing hormone secretion and female lordosis behavior in male pigs.
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Aging↗
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Results for “ESTRADIOL, THERAPEUTIC”
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[EXPERIENCE WITH EXTERNAL USE OF SYNESTROL IN THE TREATMENT OF ALOPECIA AREATA IN WOMEN].
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Alopecia↗
ENDOCRINE TREATMENT OF METASTASING BREAST CANCER.
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Androgens↗
[Prognostic values of oestradiol/oocyte rate in ICSI patients].
OBJECTIVES: To analyze the pregnancy rate in women who underwent Intracytoplasmic Sperm Injection (ICSI) program depending of the oestradiol/oocyte index. STUDY DESIGN: Retrospective, comparative. MATERIAL AND METHODS: 332 patients were included. There were divided in three groups depending on the oestradiol/oocyte index: Group A:(100 pg/mL, group B: 101-250 pg/mL and group C: > 250 pg/mL). Therapeutic protocol. Down regulation with leuprolide acetate in late luteal phase protocol, COH with rec-FSH and / or HMG, ultrasonographic and estradiol blood levels were monitored; hCG application when > 3 follicles > 18 mm, oocyte retrieval performed 34 hours later. We analyzed: patient age, male age, number of follicles, estradiol serum levels at the day of hCG application, number of mature oocytes, oestradiol/oocyte index, fertilization rate, transferred embryos, transfer quality, catheter type and luteal support. Statistical analysis (SPSS 11) with chi square, ANOVA and Kruskall-Wallis was used. RESULTS: On having analyzed the number of metaphase II oocytes retrieval, oocytes fertilized and number of transferred embryos among three groups, the best results were obtained in group B. The differences among these variables were significant. (P = 0.014, p = 0.005 and p = 0.003, respectively). When the oestradiol/oocyte index was analyzed and the PR among groups (21.83, 36.62 and 17.80 %) we observed a significant difference (p = 0.003). CONCLUSION: It is convenient to monitor the oestradiol blood levels to offer schemes of COH less aggressive to improve the oocyte quality. The oestradiol/oocyte index is a parameter adapted as a predictive value of pregnancy.
Adult↗
[Effects of combined therapy of salpingostomy and Bushen Huoxue drugs on fallopian tube obstructive infertility].
OBJECTIVE: To compare the effect of treatment of fallopian tube obstructive infertility by salpingostomy alone and in combination with TCM drugs for Bushen Huoxue (invigorating Shen and promoting blood circulation). METHODS: To all the patients, salpingostomy was performed 3 to 7 days after menstruation and hydrotubation with Xiangdan Injection (XI) was applied once in the next menstrual cycle. Bushen Huoxue Decoction (BHD) was administrated additionally to patients in the treated group, 1 dose every day starting from the 5th day of menstrual cycle for 14 days. Three months' treatment was taken as one therapeutic course and the observation lasted for 4 courses. RESULTS: The condition of follicular development, thickness of endometrium and level of serum estradiol in the preovulatory phase after treatment were all significantly increased in the two groups (P < 0.05 and P < 0.01); but the improvement in the treated group was significantly superior to that in the control group, showing significant difference. Moreover, the pregnancy rate was also higher in the former than in the latter (P < 0.05). CONCLUSION: The combined therapy of salpingostomy and TCM drugs for invigorating Shen and promoting blood circulation is an effective therapy for fallopian tube obstructive infertility, it has the effect of enhancing follicular development and increasing thickness of endometrium, and could elevate the pregnancy rate in patients.
Adult↗
Estrogenic activity of RU 486 (mifepristone) in rat uterus and cultured uterine myocytes.
OBJECTIVE: Our purpose was to determine whether RU 486 (mifepristone) has direct estrogenic activity in uterine myocytes. STUDY DESIGN: Ovariectomized adult rats were treated with RU 486, and its effect on uterine oxytocin receptor concentration, as a marker of estrogenic activity, was measured. Results were compared with the induction by RU 486 of an estrogen-responsive reporter gene in a cultured Syrian hamster uterine myocyte cell line. RESULTS: Baseline oxytocin receptor concentration was 58.8 +/- 7.2 fmol/mg protein (mean +/- SEM) and increased to 227 +/- 49 fmol/mg with 17 beta-estradiol (2.5 micrograms/kg) and to 145 +/- 18 fmol/mg after RU 486 (5 mg/kg) treatment, an effect that was inhibited by the antiestrogen ICI 182,780 (1.5 mg/kg). In the cultured Syrian hamster uterine myocyte cell line cells RU 486 (10(-6) mol/L) caused a 2.17 +/- 0.17-fold increase in the expression of the reporter gene versus 113.0 +/- 7.4-fold with 17 beta-estradiol (10(-8) mol/L). The estrogenic activity of RU 486 was dependent on the presence of both estrogen receptor and the promoter's estrogen response element. CONCLUSION: RU 486 has a weak estrogen-like activity in uterine myocytes. This activity may partly explain the therapeutic effects of RU 486 on this target organ.
Animals↗
Contraceptive and therapeutic effectiveness of two low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsute patients.
OBJECTIVE: To compare the effectiveness of two very low-dose ethinylestradiol and cyproterone acetate regimens in the treatment of hirsutism. PATIENTS: Eighteen hirsute women were randomized into two different regimens of cyproterone acetate and ethinylestradiol in a reverse sequential pattern: group 1 (0.28 mg ethinylestradiol monthly), group 2 (0.32 mg ethinylestradiol monthly). Both groups received 12.5 mg/day cyproterone acetate for the first 10 days of treatment each month. MAIN OUTCOME MEASURES: Hirsutism scores were measured according to the Ferriman and Gallwey scoring system and side-effects and complications were recorded during the 6 months of therapy. Ovulation was monitored by radioimmunoassay of estradiol, follicle stimulating hormone (FSH), luteinizing hormone (LH) and progesterone levels. The pituitary response was studied using a gonadotropin releasing hormone test. RESULTS: Hirsutism scores decreased significantly in both groups at the end of the 6 months (-30%). All patients were anovulatory, as documented by the reduction of the LH, FSH, estradiol and progesterone levels. Pretreatment basal LH and FSH levels were higher than LH and FSH levels during the treatment. Side-effects were observed only occasionally with some differences between the two therapeutic regiments. CONCLUSION: Both treatments greatly improve hirsutism, reduce clinical problems and side-effects, guarantee both anovulation and contraceptive effectiveness and afford an optimal control of the menstrual cycle.
Adult↗
Intramuscular administration of estrogen may promote angiogenesis and perfusion in a rabbit model of chronic limb ischemia.
OBJECTIVE: Promoting angiogenesis may be an effective treatment for patients with diffuse peripheral vascular disease. This study investigated whether estrogen can promote angiogenesis and perfusion in a rabbit model of chronic limb ischemia. METHODS AND RESULTS: Ischemia was induced in one hindlimb of 24 oophorectomized New Zealand White rabbits. Ten days later (day 0), they were randomized into 4 groups for intramuscular treatment in the ischemic limb: controls receiving saline at day 0; Estrogen-1 group receiving estradiol valerate, modified release (EVMR), 1 mg/kg at day 0; Estrogen-2 group receiving EVMR 1 mg/kg at days 0 and 15; and Estrogen-3 group receiving EVMR 2 mg/kg at day 0. Revascularization was evaluated by clinical indexes, such as ischemic/normal limb systolic blood pressure (BPR), and capillary density/muscle fiber in the abductor muscle of the ischemic limb at the time of death (day 30). At day 30 the BPR was increased in all groups (0.39+/-0.08 in the controls, 0.52+/-0.11 in the Estrogen-1 group, 0.65+/-0.13 in the Estrogen-2 group and 0.61+/-0.16 in the Estrogen-3 group, F=2.39, P=0.04). The capillary/muscle fiber at day 30 was 0.87+/-0.09, 1.08+/-0.15, 1.01+/-0.14 and 1.10+/-0.9 (F=5.01, P=0.01), respectively, in the 4 groups. The capillary/muscle fiber was related to BPR (r=0.48, P<0.02) and to 17-beta estradiol plasma levels of day 15 (r=0.58, P=0.003) and of day 30 (r=0.46, P<0.02). CONCLUSION: Administration of estrogen promotes angiogenesis and perfusion in ischemic rabbit hindlimbs. Thus, estrogen may represent a new therapeutic modality in the management of arterial insufficiency.
Animals↗
The effects of a promoter of cell differentiation and selected hormones on human cytomegalovirus infection using an in vitro cell system.
The influence of factors that can regulate cellular developmental or metabolic processes in host tissue on cytomegalovirus (CMV) replication in vitro was determined. Hydrocortisone treatment of cells before viral infection resulted in a 12- to 13-fold increase in the expression of immediate early proteins at 4 h after virus inoculation. The addition of a phorbol diester 1.5 h after CMV infection resulted in an 8- to 13-fold increase in production of viral progeny. In contrast, beta-human chorionic gonadotropin treatment generally resulted in a 25%-72% suppression of both CMV-specific proteins and progeny. Effects on CMV infection with either progesterone or estradiol were minor and generally suppressive. The stimulating or suppressive effects of these factors on CMV replication in vitro may be important to CMV reactivation in humans. Further study of regulatory factors may lead to the development of therapeutic approaches to the prevention of CMV reactivation in patients at risk for severe disease.
Cell Differentiation↗
Estrogen receptor-mediated vascular responsiveness to nebivolol: a novel endothelium-related mechanism of therapeutic vasorelaxation.
Nebivolol is a highly selective and lipophilic beta1-adrenergic receptor antagonist with vasodilating characteristics attributed mainly to endothelial generation of nitric oxide (NO). Coincidently, rapid vascular vasodilating effects of estradiol are also widely reported and membrane-initiated signaling by estrogen receptor (ER), leading to generation of NO, parallels the vasodilating effects observed for nebivolol. Thus, we hypothesized that the NO-dependent vasodilating effect attributed to nebivolol may be partially mediated through its interaction with the membrane-associated form of ER. The objective of this study was to examine the ER-mediated/endothelium-dependent vascular responses to nebivolol and the specific binding properties of nebivolol to ER. In isolated rat aortic rings, the endothelium-dependent vasodilating effect of nebivolol was significantly blocked by the use of the potent ER antagonist, ICI 182,780. In contrast, in the absence of intact endothelium, nebivolol-induced vasorelaxation was not blocked by ICI 182,780, strongly suggesting that nebivolol-elicited vasorelaxation is partially dependent on ER-mediated pathways. Further, we examined the binding of nebivolol to ER (MCF-7 cells) by radioligand binding assay and revealed specific binding kinetics with an estimated DC50 of 5 x 10 M, coinciding with the approximate EC50 of nebivolol as a vasorelaxant. In conclusion, the endothelium-dependent vascular response to nebivolol is attributed partially to its interaction with ER.
Animals↗
Inhibitors of type 1 17beta-hydroxysteroid dehydrogenase with reduced estrogenic activity: modifications of the positions 3 and 6 of estradiol.
Breast cancer is the second most frequent cancer affecting women. Among all endocrine therapies for the treatment of breast cancer, inhibition of estrogen biosynthesis is becoming an interesting complementary approach to the use of antiestrogens. The enzyme type 1 17beta-hydroxysteroid dehydrogenase (17beta-HSD) plays a critical role in the biosynthesis of estradiol catalyzing preferentially the reduction of estrone into estradiol, the most active estrogen. Consequently, this enzyme is an interesting biological target for designing drugs for the treatment of estrogen-sensitive diseases such as breast cancer. Our group has reported the synthesis and the biological evaluation of N-methyl, N-butyl 6beta-(thiaheptamamide)estradiol as a potent reversible inhibitor of type 1 17beta-HSD. Unfortunately, this inhibitor has shown an estrogen effect, thus reducing its possible therapeutic interest. Herein three strategies to modify the biological profile (estrogenicity and inhibitory potency) of the initial lead compound were reported. In a first approach, the thioether bond was replaced with a more stable ether bond. Secondly, the hydroxyl group at position 3, which is responsible for a tight binding with the estrogen receptor, was removed. Finally, the amide group of the side-chain was changed to a methyl group. Moreover, the relationship between the inhibitory potency and the configuration of the side-chain at position 6 was investigated. The present study confirmed that the 6beta-configuration of the side chain led to a much better inhibition than the 6alpha-configuration. The replacement of the 3-OH by a hydrogen atom as well as that of the amide group by a methyl was clearly unfavorable for the inhibition of type 1 17beta-HSD. Changing the thioether for an ether bond decreased by 10-fold the estrogenic profile of the lead compound while the inhibitory potency on type 1 17beta-HSD was only decreased by 5-fold. This study contributes to the knowledge required for the development of compounds with the desired profile, that is, a potent inhibitor of type 1 17beta-HSD without estrogen-like effects.
17-Hydroxysteroid Dehydrogenases↗
Dynamic testing of hypothalamic-pituitary function in abnormalities of ovulation.
A review of 26 unusual patients indicates that a combined luteinizing hormone-releasing hormone (LRH)-clomiphene test in conjunction with an estrogen provocation test not only was helpful in identifying underlying pathophysiology of anovulation but also proved useful in the clinical management of the patients. Dynamic testing per se does not establish a diagnosis but, in conjunction with history and other laboratory findings, it does make possible further subdivisions of groups of patients who otherwise appear similar, both clinically and from routine laboratory evaluations. It, therefore, tends to pinpoint a lesion and establish the area in which further tests should be made. It is concluded that the value of such investigations will be more evident as gynecologic endocrinology moves into investigation of the supratentorial control of hypothalamic function and as hypothalamic LRH becomes available as a therapeutic agent.
Amenorrhea↗
2-Methoxyestradiol induces mitochondria dependent apoptotic signaling in pancreatic cancer cells.
The antiproliferative action of 2-methoxyestradiol (2-ME), an endogenous estrogen metabolite is specific for cancer cells and is mediated by the induction of programmed cell death or apoptosis. But the identity of the downstream effectors of apoptotic signaling induced by 2-ME is not known. In the present study, we explored the effect of 2-ME on apoptosis in a panel of human pancreatic cancer cell lines. We have identified two categories of pancreatic cancer cell lines, which are either sensitive to 2-ME such as MIA PaCa-2, CFPAC-1, PANC-1, or non-sensitive to 2-ME such as Hs 766T. The results presented here indicated that the cell lines responsive to 2-ME could undergo apoptosis either by G2-M arrest (PANC-1) with Bcl-x(L) phosphorylation or by the accumulation of tetraploid cells in G1-S region (MIA PaCa-2) without Bcl-2/ Bcl-x(L) phosphorylation. Furthermore, 2-ME induced apoptosis in pancreatic cancer cells is mitochondria dependent as evident by the release of cytochrome c into the cytosol. 2-ME exposed cells exhibit Bid cleavage that is accompanied by the translocation of Bax into the mitochondria. Also 2-ME could induce phosphorylation of Bcl-x(L) in G2-M arrested cells, thus indicating the involvement of various anti- and pro-apoptotic regulators in the signaling cascade. The dissection of differential response of pancreatic cancer cell lines holds promise for future therapeutic intervention.
2-Methoxyestradiol↗
Value of xenografts in the investigation of prostatic function: preliminary communication.
Two of 33 prostatic tumour xenografts were established and passaged. Testosterone supplementation did not improve tumour take rates. The histological grade of the parent tumour was the principal factor affecting xenograft survival. Preliminary studies on established tumour xenografts suggest that their value lies in the study of tumour biology, and that they have no direct therapeutic application at present.
Animals↗
Inhibition of prolactin secretion by ergot alkaloids.
The effect of various ergot alkaloids on prolactin (Pr) secretion in adult female rats was determined by radioimmunoassay. Ergocorine (ECO) and ergocristine (ECR) in doses of 0.25 to 1.0 mg lowered serum Pr markedly by 1 h with the effect persisting for 24 h at the larger doses. Several other ergots had similar effects while the dihydro derivatives had diverse responses. The pro-oestrous surge of Pr could be blocked by ECR or ECO without interfering with the oestrous cycle. ECO or ECR could suppress the rise in serum Pr induced by oestradiol benzoate (OeB) (5-50 mug) in oophorectomized rats. Perphenazine (PE) stimulation of Pr could be partially antagonized by ECO depending on dose and timing of injections. ECO 2 mg produced an abrupt cessation of lactation with concomitant fall in serum Pr, and ovine prolactin restored this function. Evaluation of pituitary Pr concentration in lactating and intact rats receiving ECO leads to the conclusion that release of Pr from the pituitary is affected. ECO 1 or 2 mg produced a regression of dimethyl-benz(a)anthracene (DMBA) induced rat mammary tumours which could not be reversed by OeB 5 mug, with persisting low serum Pr. PE 1 mg was able to raise serum Pr and stimulated tumour growth. Several of the ergot alkaloids have a profound inhibiting effect on Pr secretion and may be used for studies on Pr action, as well as in medical therapeutics.
Animals↗
Modified elimination of prednisolone in epileptic patients on carbamazepine monotherapy, and in women using low-dose oral contraceptives.
The pharmacokinetics of prednisolone in serum after prednisolone-21-phosphate intravenous infusion was compared in 8 chronic epileptic patients on carbamazepine monotherapy for 2 to 12 months, in 5 healthy females having used low-dose oral contraceptives (30-40 micrograms ethinylestradiol + 50-250 micrograms levonorgestrel) for 7 to 24 months, and in 9 other healthy subjects (5 females not using oral contraceptives, and 4 males). Elimination half-lives were shorter in the patients than in the 9 healthy subjects (1.98 +/- 0.48 versus 2.73 +/- 0.76 h, mean +/- SD, 0.02 less than p less than 0.05), and total clearances higher (4.20 +/- 0.53 versus 2.96 +/- 0.54 ml X min-1 X kg-1, p less than 0.02), while the volumes of distribution did not differ significantly. Among the healthy subjects, the oral contraceptive group exhibited a longer elimination half-life, and a lower total clearance, than each of the other two groups, who gave similar results (respectively 4.75 +/- 1.27, 3.05 +/- 0.75, and 2.33 +/- 0.66 h, p less than or equal to 0.05; 1.91 +/- 0.57, 2.95 +/- 0.60, and 2.97 +/- 0.57 ml X min-1 X kg-1, p less than or equal to 0.05); the volumes of distribution were not significantly different. These findings suggest that long-term treatments by carbamazepine and by these low-dose oral contraceptives may respectively increase and decrease the therapeutic requirements of prednisolone.
Adult↗