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PubMed1995

Functional motion changes during sperm transit to the site of fertilization and in-vitro applications: a review.

Continued research to define the parameters of sperm function should aid the evaluation of various approaches in infertility as well as the efficacy of contraceptives for men which do not necessarily achieve azoospermia. Many treatment forms have been advocated for male factor infertility but have yielded little effect. These included, for example, gonadotrophins, clomiphene citrate, the weakly androgenic steroid, mesterolone. Often, improvements in oligoasthenozoospermia that are not related to genital infection, do not attain normozoospermic levels. Owing to lack of success with various treatment modalities, assisted reproductive technology encompassing artificial insemination by husband or donor following in vitro enhancement of sperm function have assumed an important role in male infertility. Agents that have been shown to induce and support sperm capacitation processes such as hyperactivation, could serve an important role. These include human follicular fluid (HFF), maternal serum, fetal cord serum and methyl xanthine derivatives.

Anabolic Agents↗
PubMed1983

Inhibin production by bovine ovarian tissues in vitro and its regulation by androgens.

No detectable amounts of inhibin were produced by cultured ovarian stroma or luteal tissue. Follicular tissue produced inhibin in vitro and removal of the granulosa cells from the follicle wall caused inhibin production to fall by 80%. Granulosa cells alone had the greatest ability of any ovarian cell type to produce inhibin in vitro, and are probably the major site of follicular inhibin production. Cyproterone acetate at concentrations of 35 and 350 microM inhibited basal and testosterone (3.5 microM)-stimulated inhibin production by cultured intact follicle wall and granulosa cells. In addition, each concentration of cyproterone acetate inhibited progesterone but not oestradiol-17 beta production by the follicle wall and granulosa cell cultures. The synthetic, non-aromatizable androgens, methylestrenolone and mesterolone, at concentrations of 5 and 25 microM, mimicked the effect of testosterone and stimulated granulosa cell inhibin production, methylestrenolone being the more potent. These findings provide further evidence that androgens regulate follicular inhibin and progesterone production and that these may be receptor-mediated processes, and suggest that inhibin production may be a general property of androgenic compounds. Preliminary examination of the physicochemical characteristics of inhibin indicated that the inhibin activity of bovine granulosa cell culture medium was (a) retained by an Amicon XM100A filter with a nominal molecular weight cut-off point of 100 000; and (b) destroyed by heating to 80 degrees C for 30 min.

Androgens↗
PubMed1977

Effect of sexual steroid hormones and of clomiphene on the behavioral response to L-dopa in mice.

The scope of the present work was to ascertain the effects of some steroid hormones on the behavioral response of mice to L-Dopa. The drugs considered were: testosterone, mesterolone, cyproterone, estradiol, progesterone and clomiphene. The male sex steroids, having either androgen or antiandrogen properties, were able to potentiate the behavioral effect of L-Dopa in mice, while female sex steroids failed to demonstrate this activity. Clomiphene proved to be the most active in enhancing the behavioral effects of L-Dopa in mice.

Animals↗
PubMed1997

Effects of various modes of androgen substitution therapy on erythropoiesis.

In order to investigate differential effects of androgens on erythropoiesis, 55 men with clincally and biochemical confirmed hypogonadism were randomly assigned to 4 groups receiving different forms of androgen substitution: Mesterolone (MES) 100 mg/d, testosterone undecanoate (TU) 160 mg/d, testosterone enanthate (TE) 250 mg i.m./21 days or 1200 mg crystalline testosterone (TPEL) subcutaneously implanted at study begin. Previous testosterone medication had been suspended at least 3 months prior to study begin. Testosterone (T), dihydrotestosterone (DHT), hemoglobin (HB) and hematocrit (HC) were assessed before, during and after substitution of androgens. MES did not increase serum T and TU raised average T levels during substitution to 5.7 +/- 0.3 nmol/l, thereby doubling baseline concentrations. TE resulted in a 6fold increase of baseline T yielding 13.5 +/- 0.7 nmol/l and TPEL increased serum T 8.5fold to 23.2 +/- 1.1 nmol/l. Average DHT levels during substitution were 4.3 +/- 0.2 (MES), 3.3 +/- 0.2 (TU), 4.0 +/- 0.4 (TE) and 5.5 +/- 0.4 (TPEL) nmol/l. The groups receiving TPEL, TU or TE showed a significant rise of HB and HC compared to baseline, whereas in the MES group these parameters did not change significantly. MES increased HB by 5.6 +/- 1.8 g/l, TU by 12.7 +/- 2.8 g/l, TE by 21.1 +/- 2.6 g/l and TPEL by 21.7 +/- 4.0 g/l. HC was raised by 1.8 +/- 0. 4% in the MES group, 3.9 +/- 1.1% in the TU group and 6.4 +/- 0.9% and 6.5 +/- 1.6% in the TE and TPEL groups, respectively. Except for 1 subject in the TPEL group, the HB and HC stayed within the normal limits. We conclude that, T, but not DHT, stimulates erythropoiesis in a dose dependent manner. T levels within the low normal range for men are required for maximal stimulation of erythropoiesis.

Adult↗
PubMed1999

Determination of anabolic steroids by gas chromatography/negative-ion chemical ionization mass spectrometry and gas chromatography/negative-ion chemical ionization tandem mass spectrometry with heptafluorobutyric anhydride derivatization.

A gas chromatography/mass spectrometry (GC/MS) method is described which uses negative ion chemical ionization (NCI) and tandem mass spectrometry (MS/MS) for the determination of eight anabolic steroids in human urine. Eight anabolic steroids were derivatized by heptafluorobutyric anhydride (HFBA), and were determined using GC/NCI-MS and GC/NCI-MS/MS. The linear correlation coefficients for calibration in NCI-MS/MS were in the range 0.9880-0.9988. This method of derivatization with HFBA for use with GC/NCI was useful in determinations of 19-norandrosterone, boldenone, 19-noretiocholanolone, 2-methylandrosterone, nandrolone, 1-methyleneandrosterone, 1-methylandrosterone, 4-dihydroboldenone and mesterolone. The detection limits of this procedure were 5-20 ppb at a signal-to-noise (S/N) ratio of 3.

Anabolic Agents↗
PubMed2001

Mass spectrometry of steroid glucuronide conjugates. II-Electron impact fragmentation of 3-keto-4-en- and 3-keto-5alpha-steroid-17-O-beta glucuronides and 5alpha-steroid-3alpha,17beta-diol 3- and 17-glucuronides.

The steroid glucuronide conjugates of 16,16,17-d(3)-testosterone, epitestosterone, nandrolone (19-nortestosterone), 16,16,17-d(3)-nortestosterone, methyltestosterone, metenolone, mesterolone, 5alpha-androstane-3alpha,17beta-diol, 2,2,3,4,4-d(5)-5alpha-androstane-3alpha,17beta-diol, 19-nor-5alpha-androstane-3alpha,17beta-diol, 2,2,4,4-d(4)-19-nor-5alpha-androstane-3alpha,17beta-diol and 1alpha-methyl-5alpha-androstane-3alpha/beta,17beta-diol were synthesized by means of the Koenigs-Knorr reaction. Selective 3- or 17-O-conjugation of bis-hydroxylated steroids was performed either by glucuronidation of the corresponding steroid ketole and subsequent reduction of the keto group or via a four-step synthesis starting from a mono-hydroxylated steroid including (a) protection of the hydroxy group, (b) reduction of the keto group, (c) conjugation reaction and (d) removal of protecting groups. The mass spectra and fragmentation patterns of all glucuronide conjugates were compared with those of the commercially available testosterone glucuronide and their characterization was performed by gas chromatography/mass spectrometry and nuclear magnetic resonance spectroscopy. For mass spectrometry the substances were derivatized to methyl esters followed by trimethylsilylation of hydroxy groups and to pertrimethylsilylated products using labelled and unlabelled trimethylsilylating agents. The resulting electron ionization mass spectra obtained by GC/MS quadrupole and ion trap instruments, full scan and selected reaction monitoring experiments are discussed, common and individual fragment ions are described and their origins are proposed.

Deuterium↗
PubMed1984

Relative binding affinity of anabolic-androgenic steroids: comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding globulin.

It is unclear whether anabolic steroids act on skeletal muscle via the androgen receptor (AR) in this tissue, or whether there is a separate anabolic receptor. When several anabolic steroids were tested as competitors for the binding of [3H]methyltrienolone (MT; 17 beta-hydroxy-17 alpha-methyl-4,9,11-estratrien-3-one) to the AR in rat and rabbit skeletal muscle and rat prostate, respectively, MT itself was the most efficient competitor. 1 alpha-Methyl-5 alpha-dihydrotestosterone (1 alpha-methyl-DHT; mesterolone) bound most avidly to sex hormone-binding globulin (SHBG) [relative binding affinity (RBA) about 4 times that of DHT]. Some anabolic-androgenic steroids bound strongly to the AR in skeletal muscle and prostate [ RBAs relative to that of MT: MT greater than 19-nortestosterone ( NorT ; nandrolone) greater than methenolone (17 beta-hydroxy-1-methyl-5 alpha-androst-1-en-3-one) greater than testosterone (T) greater than 1 alpha-methyl-DHT]. In other cases, AR binding was weak (RBA values less than 0.05): stanozolol (17 alpha-methyl-5 alpha- androstano [3,2-c]pyrazol-17 beta-ol), methanedienone (17 beta-hydroxy-17 alpha-methyl-1,4-androstadien-3-one), and fluoxymesterolone (9 alpha-fluoro-11 beta-hydroxy-17 alpha-methyl-T). Other compounds had RBAs too low to be determined (e.g. oxymetholone (17 beta-hydroxy-2-hydroxymethylene-17 alpha-methyl-5 alpha-androstan-3-one) and ethylestrenol (17 alpha-ethyl-4- estren -17 beta-ol). The competition pattern was similar in muscle and prostate, except for a higher RBA of DHT in the prostate. The low RBA of DHT in muscle was probably due to the previously reported rapid reduction of its 3-keto function to metabolites, which did not bind to the AR [5 alpha-androstane-3 alpha, 17 beta-diol and its 3 beta-isomer (3 alpha- and 3 beta-adiol, respectively)]. Some anabolic-androgenic steroids (only a few synthetic) bound to SHBG (1 alpha-methyl-DHT much greater than DHT greater than T greater than 3 beta-adiol greater than 3 alpha-adiol = 17 alpha-methyl-T greater than methenolone greater than methanedienone greater than stanozolol). The ratio of the RBA in rat muscle to that in the prostate (an estimate of the myotrophic potency of the compounds) was close to unity, varying only between about 0.4 and 1.7 in most cases.(ABSTRACT TRUNCATED AT 400 WORDS)

Androgens↗
PubMed1998

Azoospermia associated with a mutation in the ligand-binding domain of an androgen receptor displaying normal ligand binding, but defective trans-activation.

Although male infertility affects a significant proportion of couples trying to conceive, the cause of defective spermatogenesis is not known in a large number of cases. Ligand binding studies indicate that a number of these subjects may have defects of the androgen receptor (AR). Genetic screening in subjects with defective spermatogenesis and in 110 fertile controls identified an azoospermic (no sperm in any ejaculates) patient with an amino acid substitution (Gln-->Glu) in residue 798 of the AR gene. This germline mutation was pathogenic because it was not observed in fertile controls, was associated with features of minimal androgen insensitivity in our patient, has been related to more severe grades of androgen insensitivity, and caused a subtle, but significant, decrease in receptor trans-activation function in vitro that is consistent with the phenotype. Despite being located in the middle of the ligand-binding domain of the receptor, the Q798E mutation did not cause any ligand binding defect, indicating that this highly conserved residue has a trans-activation function but does not directly form part of the ligand binding pocket of the receptor. The trans-activation defect of the mutant receptor can be rectified in vitro with the androgenic drug, fluoxymesterone, but not with mesterolone or nortestosterone. Further studies are required to determine the therapeutic relevance of this finding.

Adult↗
PubMed2004

The role of the biochemistry department in the diagnosis of pituitary apoplexy.

A 47-year-old man presented with severe clinical hypoglycaemia. He had long-standing insulin-dependent diabetes with previously good glycaemic control. Intense headaches and vomiting initiated hospitalization. A brain computed tomography (CT) scan was normal, and a lumbar puncture showed elevated cerebrospinal fluid (CSF) protein [0.67 g/L; normal range (NR) 0.15-0.45 g/L], suggesting resolving viral meningitis. Routine thyroid function tests were abnormal (free thyroxine 10.6 pmol/L, NR 9-22.5 pmol/L; thyroid-stimulating hormone 0.16 mU/L, NR 0.35-5 mU/L). In the absence of evident thyroid therapy, the laboratory policy required an urgent cortisol assay to be added; this was very abnormal (42 nmol/L), suggesting hypopituitarism. Later analysis showed that concentrations of gonadotrophins and adrenocorticotrophin were low. An urgent pituitary magnetic resonance imaging scan revealed an unsuspected pituitary tumour with recent haemorrhage (pituitary apoplexy). The patient was given intravenous hydrocortisone and then stabilized on oral hydrocortisone, thyroxine and mesterolone. He made a full recovery and the hypoglycaemia resolved. The normal brain CT scan was falsely reassuring and the CSF protein was not due to viral meningitis but to haemorrhage into the pituitary tumour. If laboratory policy had not required the urgent cortisol assay be added, the diagnosis of hypopituitarism would have been delayed or even missed altogether. This could have led to the death of the patient.

Administration, Oral↗
PubMed1984

Treatment of male fertility disturbances. Current concepts.

Medical therapy of male infertility aims to improve or normalise the fertility status of a subfertile patient. However, this can be a frustrating task due to limited knowledge about the pathophysiology of male reproductive functions, and the fact that pharmacological therapy is mainly empirical and less often specific. Nevertheless, the spectrum of treatment approaches has increased within the last decade and comprises hormonal and non-hormonal compounds. Hormonal therapy is performed with antioestrogens (clomiphene, tamoxifen), gonadotrophin-releasing hormone (GnRH), prolactin inhibitors (bromocriptine), gonadotrophins (hMG, hCG), androgens (testosterone, mesterolone), and testosterone aromatase inhibitors (testolactone). Tissue hormone-releasing proteases (kallikrein) can also be applied, liberating kinins as mediator substances with different effects at the cellular level. Non-hormonal therapy includes improvement of testicular microcirculation by oxpentifylline, antimicrobial and anti-inflammatory agents, drugs to improve or allow emission and ejaculation, and psychotropic and antispasmodic drugs to diminish functional disturbances induced by emotional stress. Treatment schedules are either specifically or empirically based. If treatment is based on a pathophysiological concept which implies strong patient selection, success of treatment is excellent. In contrast, despite an increased number of compounds, empirically based therapies remain unpredictable and the results are moderate and often not reproducible. However, when different drugs are compared with a placebo group in selected, well-controlled patients with idiopathic normogonadotrophic oligozoospermia, pregnancy rates will be in the range of 30 to 40% within an observation period of 1 year, as compared with the spontaneous conception rate of between 10 and 20%.

Anti-Infective Agents↗
PubMed1999

Detection of anabolic steroids in head hair.

We developed a gas chromatography/mass spectrometry method for detection and quantitation of anabolic steroids in head hair. Following alkaline digestion and solid-phase extraction, the MO-TMS derivatives gave a specific fragmentation pattern with EI ionization. For stanozolol, the TMS-HFBA derivative showed several diagnostic ions. For androstanolone, mestanolone (methylandrostanolone), and oxymetholone two chromatographic peaks for cis and trans isomers of derivatives were seen. Recoveries were 35 to 45% for androstanolone, oxymetholone, chlorotestosterone-acetate, dehydromethyltestosterone, dehydrotestosterone, fluoxymesterone, mestanolone, methyltestosterone, and nandrolone; 52% for mesterolone, trenbolone; 65% for bolasterone; 24% for methenolone and 17% for stanozolol. Limits of detection were 0.002 to 0.05 ng/mg and of quantitation were 0.02 to 0.1 ng/mg. Seven white male steroid abusers provided head hair samples (10 to 63 mg) and urine. In the hair samples, methyltestosterone was detected in two (confirmed in urine); nandrolone in two (also confirmed in urine); dehydromethyltestosterone in four (but not found in urine); and clenbuterol in one (but not in urine). Oxymethalone was found in urine in one, but not in the hair. One abuser had high levels of testosterone: 0.15 ng/mg hair, and 1190 ng/mL urine. We conclude that head hair analysis has considerable potential for the detection and monitoring of steroid abuse.

Anabolic Agents↗
PubMed1987

Relative binding affinity at metribolone androgenic binding sites of various antiandrogenic agents.

Sebaceous glands are androgen sensitive structures with activity reduced by antiandrogens. We characterized the relative binding affinity of cyproterone acetate, 17 alpha-propyl-mesterolone, spironolactone (canrenoic acid), ethisterone and dexamethasone by means of the competitive binding analysis at metribolone (R1881) androgen binding sites. Using the DCC-assay (dextran-coated charcoal absorption) with the Scatchard plot and saturation analysis we quantified R1881 androgen binding sites from sebaceous glands situated in the ventral side of the pinna of the Syrian hamster. As parameters for ligand affinity at these binding sites served the ligand concentration for 50% displacement of 3H-labelled synthetic steroid R1881 in constant concentrations. The in vitro measurements of the used steroids were compared to the biologic sebosuppressive effect in vivo. 17 alpha-Propylmesterolone showed the highest affinity at the androgenic binding site followed by ethisterone, cyproterone acetate and spironolactone. The results, however, do not admit an interpretation about the mode of action of the given substances, which display their biologic activity either after systemic or topic administration. In vivo distribution problems and metabolizing procedures might be due to this discrepancy.

Androgen Antagonists↗
PubMed1978

[Vertebrate hormones influence on the reproduction of Biomphalaria glabrata and on Schistosoma mansoni infection (author's transl)].

The influence of fifteen vertebrate hormones on the B. glabrata reproduction and on S. mansoni infection have been studied. Hecogenine and pregnadienolone significantly increased the snail's number of eggs; testosterone, diethylstilbestrol and estradiol valerianate decreased their number of eggs and the mesterolone and progesterone produced a slight decrease in the number of eggs. Crude hecogenine, pregnenolone, prednisone, estradiol, cholic acid, diosgenin, estrone and pregnadione have not shown any significant alteration on the snail reproduction. None of these hormones presented any influence upon the S. mansoni cycle in B. glabrata. Molluscicidal, oocidal and cercarcidal activities have been observed with diethylstilbestrol in concentrations below 10 ppm.

Animals↗
PubMedDate not supplied

[Androgen substitution in the andrological disease picture].

Androgen deficiency is due to an insufficient synthesis of testosterone by the Leydig cells. This is either caused by a primary defect (primary hypoandrogenism) or by an inadequate hypophyseal stimulation (secondary hypoandrogenism). The clinical symptoms may include a late puberty, diminished terminal hairs, small testes, sexual impotence, and abnormal seminal fluid, but none of these conditions as an unique sign allows the diagnosis. This is achieved by low testosterone plasma levels (or low urinary excretion). The primary hypoandrogenism is additionally characterized by high gonadotropin levels, while the secondary form shows low FSH and LH. Hormone substitution is done with hCG and hMG in secondary hypoandrogenism only when fertility is aspired. In all other cases and in primary hypoandrogenism testosterone is given, either as oral form (testosterone undecaonate) or as depot injection (testosterone enanthate). Synthetic derivates like methyltestosterone are hazardous (hepatomas) or, like mesterolone, are too weak in their androgenic effect.

Androgens↗
PubMed1984

[Diagnosis of a toxic liver lesion based on spermiographic changes].

8% of andrological patients are exposed to harmful substances at work. Testicular function can be impaired by mechanical and thermic irritation, but, above all, many chemical substances have a detrimental effect on spermatogenesis. A case is presented of a 23 year-old painter who showed a significant rapid decrease in sperm quality in spite of a course of treatment with mesterolone. The toxic agents were nitro lacquer thinners and resin dispersions, which had caused toxic liver damage, as seen from the raised liver enzyme activities. The elimination of the noxious substances resulted in a normalization of liver enzyme activities and a restitution of fertility.

Adult↗
PubMed1983

[Recent aspects of therapy with androgenic and anabolic steroids].

From the pharmacology of the therapeutically available androgen preparations and the clinical experience results that a highly dosed androgen long-term therapy is effectively possible only by testosterone esters which are to be injected intramuscularly (e.g. testosterone oenanthate). It is indicated in all forms of endocrine hypogonadism, certain aplastic anaemias and if necessary in extreme male high growth. In partial androgen deficiency (pubertas tarda, Klinefelter's syndrome, climacterium virile and others) orally applicable androgens such as testosterone-undecanoate (Andriol) and mesterolone (Vistimon) can be used. The latter is to be preferred when a hyperoestrogenism is present, e.g. in liver cirrhosis. When 17-alpha-alkylated oral androgens are used, their often not sufficiently confirmed anabolic effect and their potential liver toxicity should more be taken into consideration.

Adolescent↗
PubMedDate not supplied

Electrophysiological and psychological changes induced by steroid hormones in men and women.

The effects of hormonal changes during the menstrual cycle and of oral contraceptives on the EEG, heart-rate and a number of performance tasks were investigated in 16 female subjects (Ss). Powerspectral analysis in the EEG revealed significantly increased alpha-frequencies and heart-rates during the luteal phase of the menstrual cycle whereas the mean theta-frequency and power decreased. A number of psychological test variables, such as reaction time to a tone, to a flickering light and to a colour-tone sequence and the time to solve simple arithmetic problems was shorter at the periovulatory time. Another minimum was reached during the perimenstrual phase. The flicker-fusion-frequency was higher during these two periods. No such effects could be observed when the same Ss were treated with oral contraceptives. It is concluded that the phenomena observed during the luteal phase of the cycle may be the expression of a slight general arousal effect, possibly medicated by progesterone via the noradrenergic system. In a subsequent double blind study 30 male Ss were treated with an gestagenic compound (D-Norgestrel, 2.5 mg/die), an estrogenic compound (estradiolvalerate, 5 mg/die), an androgenic substance (Mesterolone, 100 mg/die) or with placebo. Only treatment with the progestational compound revealed significant changes in the EEG and the performance tests. These changes were qualitatively similar to those observed during the luteal phase of the female Ss. Under both conditions, i.e. the luteal phase and D-Norgestrel treatment, the body-temperature was significantly increased. Hence, the question whether gestagens exert their effects directly on CNS structures which modulate EEG appearance and behavior or indirectly via increased body-temperature cannot be answered convincingly.

Adolescent↗
PubMed1995

The management of male subfertility by in vitro fertilisation techniques.

Although IVF was developed for the treatment of tubal infertility, it is clear that it has a significant application in treatment of couples where the problem is one of male subfertility. This is particularly relevant because, despite the developments in reproductive medicine, in most males there is no identifiable cause for the poor semen quality. Therefore, for these men there is no efficacious method of treatment. Varicocele ligation and the use of agents such as clomiphene citrate, mesterolone empirical antibiotic therapy, and anabolic steroids have not been show to be beneficial when subject to controlled trials. The concept of improving the chance of fertilisation by taking the oocytes to the sperm in vitro is therefore the first feasible therapeutic option available to these subfertile couples. However, these possibilities should not obviate the need for a thorough assessment of the subfertile male and continuing research into the basis of male infertility. During the past decade new methods of sperm preparation, modified methods of insemination, and the use of microinjection have been developed. IVF is now a realistic option for couples if the male is subfertile. It has been suggested by some critics of these techniques that the brunt of the discomfort and risk has to be borne by the women where the problem appears to be solely with the male partner. Nevertheless, as having children is a 'couple' decision, prospective couples need to consider whether such procedures are acceptable to them.(ABSTRACT TRUNCATED AT 250 WORDS)

Female↗