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PubMed1987

Applications of hormones in the metabolic regulation of growth and lactation in ruminants.

Exogenous natural and synthetic estrogenic and androgenic steroid hormones are used commercially to stimulate metabolic processes associated with increased rate and efficiency of body growth in ruminants. However, mechanisms of action of steroid hormone-induced effects on metabolism are relatively unknown. Application of peptide hormones to muscle growth, fat deposition, and lactation has lagged because of lack of sufficient quantities of the hormones. However, with recombinant DNA technology synthesis of large quantities of peptide hormones is now feasible. Most efforts have focused on growth hormone (GH), growth hormone-releasing factor (GRF), and prolactin (PRL) effects on lactation. For example, administration of GH or GRF stimulates yields of milk, milk fat, protein, and lactose as much as 41% in cattle. The mechanism of GH action probably involves somatomedin C acting at extramammary sites and (or) directly at the mammary cell. PRL is lactogenic but has no significant effect on established lactation in cattle. Daily exposure of cattle to 16 h light and 8 h of darkness stimulates milk yield and body growth and reduces fat accretion in the carcass, but the hormonal signals responsible for these photoperiod-induced responses are unknown. Photoperiod manipulations are relatively easy to apply to ruminants, but development of suitable delivery systems for animals will greatly enhance application of peptide hormones to further studies of metabolism as well as commercial livestock production systems.

Animals↗
PubMed2005

Flame retardants, surfactants and organotins in sediment and mysid shrimp of the Scheldt estuary (The Netherlands).

Sediment and mysids from the Scheldt estuary, one of the largest and most polluted estuaries in Western Europe, were analyzed for a number of contaminants that have been shown to possess endocrine-disrupting activity, i.e. organotins, polybrominated diphenyl ethers (PBDEs), hexabromocyclododecane (HBCD), tetrabromobisphenol A (TBBPA), nonylphenol ethoxylates (NPE) and transformation products, nonylphenol (NP) and nonylphenol ether carboxylates (NPEC). In addition, in vitro estrogenic and androgenic potencies of water and sediment extracts were determined. Total organotin concentrations ranged from 84 to 348 ng/g dw in sediment and 1110 to 1370 ng/g dw in mysid. Total PBDE (excluding BDE-209) concentrations ranged from 14 to 22 ng/g dw in sediment and from 1765 to 2962 ng/g lipid in mysid. High concentrations of BDE-209 (240-1650 ng/g dw) were detected in sediment and mysid (269-600 ng/g lipid). Total HBCD concentrations in sediment and mysid were 14-71 ng/g dw and 562-727 ng/g lipid, respectively. Total NPE concentrations in sediment were 1422 ng/g dw, 1222 ng/g dw for NP and 80 ng/g dw for NPEC and ranged from 430 to 1119 ng/g dw for total NPE and from 206 to 435 ng/g dw for NP in mysid. Significant estrogenic potency, as analyzed using the yeast estrogen assay, was detected in sediment and water samples from the Scheldt estuary, but no androgenic activity was found. This study is the first to report high levels of endocrine disruptors in estuarine mysids.

Animals↗
PubMedDate not supplied

Ligand structure influences autologous downregulation of estrogen receptor-alpha messenger RNA.

A series of A- and D-ring substituted estrogen analogues have been examined for their effect on estrogen receptor-alpha (ERalpha) mRNA downregulation. Recently it has been proposed that ERalpha autologous downregulation occurs via transcriptional repression exerted by the binding of the ERalpha-ligand complex to the 5' region of the coding region of the ERalpha gene. Placement of the phenolic hydroxyl group on the various carbons of the aromatic A-ring of estratrien-17betaol (carbons 1-3) produced ligands which diminished the steady state level of ERalpha mRNA in relation to their affinity for receptor. 4-Hydoxyestratrien-17betaol, on the other hand, was inactive in the downregulation of ERalpha mRNA. Although this A-ring isomer brought about apparent processing of the nuclear receptor, the ERalpha reappeared in the cytosol within 24 h. Unlike the stimulation of genes regulated via estrogen response elements, maximum autologous negative regulation of the ERalpha gene required the presence of an hydroxyl group on carbon 17 of the D-ring. These results suggest that the conformational alterations elicited in the ERalpha molecule by various ligands create surfaces capable of interacting with other transcription factors in a manner which is different when the receptor functions via a response element mechanism relative to interactions during autologous negative regulation of the ERalpha gene.

Down-Regulation↗
PubMed1999

Pharmacokinetics of 7 alpha-methyl-19-nortestosterone (MENT) delivery using subdermal implants in healthy men.

We studied the pharmacokinetics of 7 alpha-methyl-19-nortestosterone (MENT), a potent synthetic androgen, administered by subdermal implants. The implants contained 112 +/- 4 mg of MENT acetate in a polyethylene vinyl acetate copolymer. MENT acetate released from the implants is rapidly hydrolyzed to MENT in vivo. Fifteen healthy Finnish men were randomized to have either one, two, or four implants inserted in the medial aspect of the upper arm. The implants remained in place for 4 weeks. Blood samples were obtained before implant insertion, 1, 2, 3, and 4 weeks after insertion, and 1 and 2 weeks after removal. Serum MENT concentrations were determined by gas chromatography with mass selective detection. The MENT levels attained in each implant group remained at a steady level during the 4 weeks of implant use. The mean steady state MENT concentrations in the one, two, and four implant groups were 0.6, 1.4, and 2.3 nmol/L, respectively. Serum MENT concentrations during implant use were clearly dose dependent; the between-subject effect of implants as well as the differences between each pair of groups were all statistically significant. The release rate of MENT from one, two, and four implants was calculated to be approximately 0.3, 0.8, and 1.3 mg/day, respectively. This study suggests that MENT acetate implants are a promising method for long-term androgen administration in hypogonadism and male contraception.

Adult↗
PubMed1991

Oral contraceptive containing desogestrel in the maintenance of the remission of hirsutism: monthly versus bimonthly treatment.

A treatment to keep hirsutism in remission while minimizing lipid disturbances was attempted in 20 formerly hirsute patients with hirsutism scores already greatly reduced after oral contraceptives (OCs) treatment. After OCs discontinuation for one to three months, they were thereafter treated for two years as follows: 9 patients received ethinyl estradiol (30 micrograms/day) plus desogestrel (150 micrograms/day) in three-week cycles every month (monthly); 6 patients received the same formulation during three-week cycles every other month (bimonthly); 5 patients received no treatment. In the untreated patients, abnormal hirsutism scores reappeared within 12-18 months; the levels of testosterone and free testosterone, initially high following discontinuation of OCs, remained elevated. Monthly treatment kept hirsutism in remission, and testosterone and free testosterone levels decreased. Bimonthly treatment was equally effective keeping hirsutism in remission, although testosterone levels did not decrease. Bimonthly treatment was not better than monthly treatment in relation to changes in plasma lipids (cholesterol, HDL-cholesterol, triglycerides).

Analysis of Variance↗
PubMed1991

Steroids and cAMP in follicles of postpartum beef cows treated with norgestomet.

To determine time of occurrence of follicular changes that may be associated with the length of the subsequent luteal phase, follicles were collected at different times before ovulation from cows expected to have corpora lutea of short (control) or normal (norgestomet-treated) life span. Beginning on d 20 to 23 postpartum (d 0 of study), 34 crossbred beef cows received either a 6-mg implant of norgestomet for 9 d or served as untreated controls. Ovaries were removed from norgestomet-treated cows on d 6 (N6; n = 9), d 8 (N8; n = 8), or the day after implant removal (N10; n = 8). Control cows were ovariectomized on d 6 (C6; n = 4) or d 10 (C10; n = 5). The largest and second largest follicles greater than 8 mm (F1 and F2, respectively) were dissected from the ovaries. Granulosal and thecal layers and follicular fluid were separated and assayed for estradiol-17 beta, progesterone, androstenedione, and testosterone. Cyclic 3'5'adenosine monophosphate (cAMP) was determined in thecal and granulosal tissue. Diameters of the F1 (14.6 +/- .4 mm) and F2 (10.6 +/- .4 mm) did not differ due to treatment. A greater proportion (P less than .05) of the F1 (20/33) than of the F2 (4/27) had estradiol:progesterone ratios of greater than 1 in follicular fluid. Contents of estradiol, androstenedione, and testosterone in theca and granulosa and follicular fluid, androstenedione in theca, and testosterone in theca and follicular fluid (all P less than .05).(ABSTRACT TRUNCATED AT 250 WORDS)

Androstenedione↗
PubMed1993

7 alpha-methyl-nortestosterone (MENT): the optimal androgen for male contraception.

UNLABELLED: Many methods of contraception involve the use of drugs that affect the secretion of hormones essential for reproduction. Oestrogens and progestins have been used for contraction in women as inhibitors of gonadotrophin secretion and ovulation. Similarly, androgens must be used in methods of fertility control for men that block gonadotrophin secretion. Androgen supplementation currently involves large, frequent doses of testosterone esters that are associated with wide fluctuations of plasma testosterone levels. Hence, there is a need for an androgen preparation that provides appropriate, continuous replacement doses over long periods. To achieve this goal, 7 alpha-methyl-19-nortestosterone (MENT), a synthetic androgen that is considerably more potent than testosterone, is suitable. As a consequence, it is feasible to administer this androgen as a substitute for testosterone for 1 year by subdermal implants. Another important feature of MENT is that it does not undergo 5 alpha- reduction in prostate as does testosterone. As a consequence, a dose of MENT sufficient to maintain normal muscle mass and gonadotrophin secretion will not hyperstimulate the prostate because its action in this organ is not amplified as is that of testosterone. Thus, MENT can be administered to men with the assurance that it will be less prone to cause diseases of the prostate than testosterone. CONCLUSIONS: (i) MENT is the first androgen that has a health benefit compared to testosterone; (ii) MENT will be promoted as one component of a two-implant system for male contraception, the other component being an implant that will release an LHRH analogue; (iii) MENT has potential uses in patients with a variety of disorders, including hypogonadism, prostatic hyperplasia and muscle wasting.

Animals↗
PubMed1998

In vitro effect of estradiol, progesterone, testosterone, and of combined estradiol/progestins on low density lipoprotein (LDL) oxidation in postmenopausal women.

OBJECTIVE: One of the mechanisms currently proposed to explain the cardioprotective effect of hormone replacement therapy (HRT) is the antioxidative property of estrogens. Considering that HRT involves the administration of an estrogen, usually combined with a progestin and sometimes with an androgen, we investigated the following in vitro: (1) the effect of estradiol, progesterone, and testosterone on the oxidation of low density lipoprotein; (2) the possible pro-oxidative effect of progesterone and testosterone on native low density lipoprotein; and (3) the possible modification of the antioxidant effect of estradiol on low density lipoprotein induced by progestins. DESIGN: Low density lipoprotein was isolated from blood samples obtained from 20 untreated postmenopausal women and divided in multiple aliquots, each containing 0.5 mg LDL protein. In Protocol 1 (n = 10) different doses of estradiol, progesterone, and testosterone ranging from 0 to 26 micrograms/ml were tested inducing oxidation with 15 microM copper sulfate. In Protocol 2 (n = 6) we studied the rate of oxidation of low density lipoprotein incubated with progesterone or testosterone without any oxidative induction. In Protocol 3 (n = 10) we studied the concomitant effect of 15 microM estradiol with four separate progestins (progesterone, medroxyprogesterone acetate, norethindrone, and norgestrel) in different doses (0, 5, 15, and 50 microM). After incubation for 4 h at 37 degrees C, malonaldehyde was measured as a marker of low density lipoprotein oxidation. The results were expressed in mean +/- SD. RESULTS: Protocol 1: Estradiol induced a dose-dependent decrease in malonaldehyde generation, from a baseline of 61.8 +/- 30.2 nmol/mg protein to 11.6 +/- 7.1 nmol/mg protein at the highest dose of estradiol tested (p < 0.0001). Progesterone or testosterone did not modify malonaldehyde generation. Protocol 2: Progesterone and testosterone did not show pro-oxidative action. Protocol 3: Estradiol 15 microM alone induced a 35% decrease in malonaldehyde generation, from a baseline of 75.4 +/- 25.4 to 49.3 +/- 18.8 nmol/mg protein (p < 0.0001). Norgestrel and norethindrone did not modify the antioxidant effect of estradiol (p > 0.05). Progesterone and medroxyprogesterone acetate induced a further reduction of malonaldehyde concentration to 37.2 +/- 20.8 and 38.6 +/- 18.2 nmol/mg protein, only at the highest dose tested (p < 0.02 and p < 0.01, respectively). CONCLUSIONS: Our results demonstrate that, in contrast with the potent antioxidant effect of estradiol, progesterone and testosterone did not show any pro- or antioxidant effect on low density lipoprotein in vitro. Furthermore, progestins did not counteract the antioxidant effect of estradiol in vitro.

Copper Sulfate↗