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Regular exercise and anabolic androgenic steroids have opposing effects on the plasma lipoprotein profile and risk of cardio-metabolic diseases in humans. Studies in humans and animal models show conflicting results. Here, we used a mice model genetically modified to mimic human lipoprotein profile and metabolism. They under-express the endogenous LDL receptor gene (R1) and express a human transgene encoding the cholesteryl ester transfer protein (CETP), normally absent in mice. The present study was designed to evaluate the independent and interactive effects of testosterone supplementation, exercise training and CETP expression on the plasma lipoprotein profile and CETP activity. CETP/R1 and R1 mice were submitted to a 6-week swimming training and mesterolone (MEST) supplementation in the last 3 weeks. MEST treatment increased markedly LDL levels (40%) in sedentary CETP/R1 mice and reduced HDL levels in exercised R1 mice (18%). A multifactorial ANOVA revealed the independent effects of each factor, as follows. CETP expression reduced HDL (21%) and increased non-HDL (15%) fractions. MEST treatment increased the VLDL concentrations (42%) regardless of other interventions. Exercise training reduced triacylglycerol (25%) and free fatty acids (20%), increased both LDL and HDL (25-33%), and reduced CETP (19%) plasma levels. Significant factor interactions showed that the increase in HDL induced by exercise is explained by reducing CETP activity and that MEST blunted the exercise-induced elevation of HDL-cholesterol. These results reinforce the positive metabolic effects of exercise, resolved a controversy about CETP response to exercise and evidenced MEST potency to counteract specific exercise benefits.

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In this paper, mesterolone metabolic profiles were investigated carefully. Mesterolone was administered to one healthy male volunteer. Urinary extracts were analyzed by liquid chromatography quadruple time-of-flight mass spectrometry (LC-QTOFMS) for the first time. Liquid-liquid extraction was applied to processing urine samples, and dilute-shoot analyses of intact metabolites were also presented. In LC-QTOFMS analysis, chromatographic peaks for potential metabolites were hunt down by using the theoretical [M-H](-) as target ions in full scan experiment, and their actual deprotonated ions were analyzed in targeted MS/MS mode. Ten metabolites including seven new sulfate and three glucuronide conjugates were found for mesterolone. Because of no useful fragment ion for structural elucidation, gas chromatography-mass spectrometry instrumentation was employed to obtain structural details of the trimethylsilylated phase I metabolite released after solvolysis. Thus, their potential structures were proposed particularly by a combined MS approach. All the metabolites were also evaluated in terms of how long they could be detected, and S1 (1α-methyl-5α-androst-3-one-17ß-sulfate) together with S2 (1α-methyl-5α-androst-17-one-3ß-sulfate) was detected up to 9 days after oral administration, which could be the new potential biomarkers for mesterolone misuse.

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Mesterolone is a synthetic oral anabolic androgenic steroid used to treat hypogonadism. There are frequent reports of mesterolone abuse in human and equine sports to increase muscle mass and strength. However, limited information is available about how this drug exerts its effects on skeletal muscle. Satellite cells (SCs) are mononuclear myogenic stem cells that contribute to postnatal muscle growth and repair. As SC activation and subsequent differentiation to new myonuclei is a major event during muscle hypertrophy, this study investigated the influence of mesterolone on SC distribution within the pectoralis muscle of chickens. Specifically, this study tested the hypotheses that mesterolone induces avian skeletal muscle hypertrophy, and that mesterolone increases the number of SCs in avian skeletal muscle. Robust immunocytochemical techniques and morphometric analyses were used to calculate the numbers of SCs and myonuclei. Also, DNA concentration and Pax7 protein levels were measured to confirm immunocytochemical findings. Mesterolone significantly increased pectoralis mass and fiber size. All SC indices and number of myonuclei increased significantly by mesterolone administration. In addition, greater DNA concentration and Pax7 protein expression were found in mesterolone-treated birds. This study indicates that mesterolone can induce avian skeletal muscle hypertrophy and that this is correlated with increased number of SCs. We suggest that SCs are key cellular intermediaries for mesterolone-induced muscle hypertrophy.

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This study was conducted to determine the effect of scrotal insulation and post insulation Proviron® treatment on sperm morphological characteristics and mating behavior. Twelve healthy WAD bucks, free from any clinical or andrological disorder were used. Scrotal insulation was done using insulating bags for 30 days. After insulation, the bucks were divided into two groups. The treatment group received 100mg/head /week of Proviron® for 3 weeks. Semen collection was done using the electroejaculation method in all phases of the study. The proviron® treated bucks, when compared with insulation and post insulation untreated phases, showed significant reduction (p<0.05) in sperm cell abnormalities which reduced from 15.89 +/- 22.89 in post insulation untreated phase to 2.81 +/- 0.83 in post insulation treated phase. The Proviron® treated bucks also showed increased physical vigor by riding, mounting and fighting their untreated counterparts.

Este estudio se realizó para determinar el efecto de aislamiento escrotal y aislamiento posterior al tratamiento con Proviron® sobre las características morfológicas de los espermatozoides y el comportamiento del apareamiento. Fueron utilizadas 12 cabras enanas del Oeste Africano, sanas, libres de cualquier desorden clínico andrológico. El aislamiento escrotal se realizó utilizando bolsas de aislamiento durante 30 días. Después de aislamiento, los machos se dividieron en dos grupos. El grupo de tratamiento recibió 100mg/cada una por semana de Proviron® durante 3 semanas. La recolección de semen se realizó mediante el método de electroeyaculación en todas las fases del estudio. Las cabras tratadas con Proviron®, cuando se compararon con las fases post-aislamiento no tratadas, mostraron una reducción significativa (p<0,05) en las anormalidades de células espermáticas, las cuales se redujeron desde 15,89 +/- 22,89 en las fases post-aislamiento sin tratamiento a 2,81 +/- 0,83 en las fases post-aislamiento tratadas. Las cabras tratadas con Proviron® también mostraron un incremento en el vigor físico, la monta y la lucha contra sus homólogos no tratados.

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Light and electron microscopy and quantitative morphometry were used to determine the effects of exercise and mesterolone on the soleus muscles of mice. Both exercise and mesterolone caused a significant hypertrophy of extrafusal muscle fibres. The hypertrophy of Type I fibres was greater than that of Type II fibres. There was no hyperplasia. Mitochondria were more numerous and larger than in the muscles of sedentary animals. Capillarity increased and small centrally nucleated muscle fibres appeared, usually in small clusters and most often in the muscles of animals exposed to mesterolone. A small proportion of satellite cells exhibited signs of activation but there were more in the muscles of mesterolone-treated animals than after exercise. Muscles from animals that had been both exercised and treated with mesterolone exhibited the largest changes: muscle mass and muscle fibre hypertrophy was greater than in all other groups of animals, capillarity was higher and >30% of all recognized satellite cells exhibited signs of activation. Groups of small centrally nucleated muscle fibres were commonly seen in these muscles. They appeared to be the result of splits in the form of sprouts from existing muscle fibres. With both exercise and mesterolone, alone or in combination, there was an increase in the proportion of Type I muscle fibres and a decrease in the proportion of Type II.

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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.

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Se informa de la experiencia obtenida en cinco niños con diagnóstico de anemia aplástica adquirida, a quienes se les administró globulina antitimocito. Uno de los niños no había recibido ningún tratamiento previo. Los otros cuatro habían recibido medicación con andrógenos (mesterolona) con pobre respuesta; dos de los cuales tenían menos de un mes de recibir este medicamento. Las reacciones secundarias observadas fueron: eritema máculopapular, prurito, artralgias y fiebre. En ningún caso hubo necesidad de suspender el tratamiento por intolerancia. A todos los niños se les administró mesterolona después de la aplicación de la globulina antitimocito. Se practicó un estudio de médula ósea antes del tratamiento y 12 semanas después de iniciado éste. No se observaron cambios en las diferentes series celulares. Dos de los niños fallecieron meses después por hemorragias e infección. Tres continúan con aplicación de mesterolona. Dos de ellos han tenido menor frecuencia de internamientos para transfusión de sangre y presentan evidente mejoría de la celularidad de médula ósea

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With regard to hair growth induced by therapeutics, we have to consider various aspects of the activity of the hair follicle. This means that a study on the efficacy of hair growth therapeutics requires a selective investigation of different kinds of follicular activity. The decision which of the non-invasive, semi-invasive or invasive techniques available should be applied in a specific case depends on the reliability of the method in relation to the technical requirement, on the one hand, and the acceptance by the volunteer as well as the clinical type and degree of hair loss, on the other. Trichorhizogram results as the only means of evaluating the efficacy of hair growth therapeutics seem problematical, since an increase of the anagen rate does not absolutely correlate with a prolongation of the anagen phase.

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10 male test persons with androgenetic alopecia (Hamilton stage IV) were topically treated with an alcoholic 17 alpha-propylmesterolone solution (PM, 3%) for 3 months. Before and after treatment, we took deep biopsies from the fronto-temporal scalp region. Microsurgically, we isolated anagen hair bulbs, connective tissue with epidermis, and fat from the biopsy samples in order to determine cell cycle kinetics by means of DNA-flow cytometry. By comparison, cell cycle kinetics of the pre- and post-treatment samples did not show any significant changes with regard to connective tissue and fat, whereas in anagen hair bulbs, we found a significant increase of both S-phase cells (%) and the proliferation index (%). These results imply that PM, if topically applied, enhances the proliferative activity of hair matrix cells.

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17 alpha-Propylmesterolon, a new topically active antiandrogen, was administered to 25 patients with papulopustular or comedo acne and severe seborrhoea. The patients were supplied with a 3% solution of 17 alpha-propylmesterolone in 70% alcohol and were advised to apply it to the face twice daily for a mean duration of 14 weeks. Clinical follow-ups and thin-layer-chromatography determination of the sebum secretion rate (SER) and the lipid fractions were performed monthly. At the end of the treatment period 72% of the patients had improved. Comedo acne was reduced by 2 grades, papulopustular acne by 1.8 grade. The mean reduction of seborrhoea was 2 grades. SER was reduced in 62.5% of the patients to 76.4 +/- 8.8% of pretreatment values. In addition to sebaceous gland lipids, epidermal lipids were also inhibited effectively. This finding is in accordance with the marked reduction of comedones. Thus, in addition to sebaceous gland inhibition, epidermal structures may also be the target of the antiandrogen.

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The antidepressant effects of amitriptyline and mesterolone, a synthetic androgen, were compared in a double-blind parallel treatment design. The drugs were equally effective in reducing depressive symptoms. Mesterolone produced significantly fewer adverse side effects than amitriptyline.

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Mesterolone, 150 mg daily by mouth, was given to 26 patients (10 men, 16 women) with renal anaemia on chronic haemodialysis (3 times for 5 hours). At the beginning of treatment the patients had been dialysed for at least 6 months under stable conditions: iron deficiency had been excluded or treated. Progressive improvement in the anaemia was observed during the treatment period. After 39 months the haemoglobin concentration had risen from 74 +/- 4 g/l to 95 +/- 5 g/l, haematocrit from 0.22 +/- 0.01 to 0.28 +/- 0.02, and the red-cell count from 2.44 +/- 0.12 X 10(12)/l to 3.09 +/- 0.2 X 10(12)/l. Side effects were rare; some patients developed increased appetite with a rise in body weight, while some women developed acne or hirsutism. There was no effect of mesterolone on liver function. The results indicate that mesterolone can favourably influence renal anaemia and that the side effects of this testosterone derivative are not such as to prohibit its use in women.

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Treatment with 17 alpha-methyltestosterone and with some synthetic androgens prevents attacks of hereditary angioedema (HAE). However, the potential hepatotoxicity of 17 alpha-alkylated androgens raises the problem of long-term prophylactic use of these agents. Therefore we compared the efficacy in preventing HAE attacks of 17 alpha-alkylated steroids (danazol and stanozolol) with non-17 alpha-alkylated derivatives (quinbolone, nandrolone decanoate and mesterolone). As the latter group proved ineffective, it seems that a drug's efficacy in preventing HAE attacks is connected to its 17 alpha-alkylation. Moreover, our long-term observations with the minimum effective dose of danazol seem to indicate the absence of important collateral effects.

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The response to Mesterolone, in doses of 25 mg/day, was examined in 42 pathospermic patients. Treatment lasted for 100 days. The pronounced response to the Mesterolone treatment was observed in hypozoo- and oligozoospermia with low initial fructose content in the ejaculate. Fructose content attained its normal range after the treatment. During the therapeutic period 11 wives became pregnant. The authors conclude that Mesterolone does not influence plasma FSH, LH and testosterone levels, it has only peripheral effects.

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Hormone levels were measured in patients with Klinefelter's syndrome after treatment with 100 mg mesterolone cipionate (twice monthly). There was no difference in plasma testosterone and FSH levels in treated and untreated patients. The basal and maximum LH levels were lower, but remained raised. The urinary excretion of testosterone as measured by liquid gaschromatography was higher in treated patients after treatment was discontinued.-From these results it is concluded that in spite of reported decreases of plasma testosterone during therapy with mesterolone cipionate this drug does not lead to severe impairment of the endogenous hormone production after discontinuing treatment.

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42 subfertile patients with normal levels of plasma testerone (26 subnormal, suffering from oligospermia) have been treated with a combination of clomiphene citrate (50 mg Clomid daily) and mesterolon (50 mg Proviron daily) over a period of at least 3-6 months. The treatment resulted in pregnancy in 6 cases and in a significant improvement of the sperm count in 16. In 7, however, whilst the sperm count improved the qualitative results were unsatisfactory as many sperms were immature. Restricted spermatogenesis and a sperm count below 5 million/ml must be considered unfavourable but does not constitute a counter-indication to the combined therapy. No hazardous complications were observed.

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