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P Kiousi, Y S Angelis, A G Fragkaki, W Abushareeda, M Alsayrafi, C Georgakopoulos, E Lyris
This manuscript describes the direct detection of mesteroloe sulfo-conjugated metabolites by liquid chromatography/quadrupole/time of flight mass spectrometry (LC/Q/TOFMS) with special focus on evaluation of their retrospective detectability and their structure elucidation. A comparison of their long-term detectability, with the mesterolone main metabolite (1α-methyl-5α-androstan-3α-ol-17-one) excreted in glucuronide fraction and detected by gas chromatography/high resolution mass spectrometry (GC/HRMS), is also presented...
December 2015: Journal of Mass Spectrometry: JMS
S Rzeppa, G Heinrich, P Hemmersbach
Improvements in doping analysis can be effected by speeding up analysis time and extending the detection time. Therefore, direct detection of phase II conjugates of doping agents, especially anabolic androgenic steroids (AAS), is proposed. Besides direct detection of conjugates with glucuronic acid, the analysis of sulfate conjugates, which are usually not part of the routine doping control analysis, can be of high interest. Sulfate conjugates of methandienone and methyltestosterone metabolites have already been identified as long-term metabolites...
November 2015: Drug Testing and Analysis
Malcolm Carruthers, Paul Cathcart, Mark R Feneley
INTRODUCTION: Testosterone treatment has evolved rapidly over the past 25 years as new, more effective and convenient methods have become available. This study reports experience with seven different methods, introduced on the market in the UK. AIM: To establish the symptom response when testosterone treatment was initiated on the basis of clinical features and symptoms of androgen deficiency, and the resulting endocrine, biochemical and physiological responses...
2015: Aging Male: the Official Journal of the International Society for the Study of the Aging Male
Harun Dugeroglu, Mustafa Ozturk, Murat Atmaca, Ismet Seven
OBJECTIVE: To investigate the effects of mesterolone on prostate in patients treated for aging male syndrome. METHODS: The cross-sectional study was conducted from June to September, 2009, at endocrinology and metabolism department of Yuzuncu Yil University, Van, Turkey, andcomprised patients with symptoms of aging male syndrome and/or low testosterone. They were given mesterolone 50 mg/day per oral for two months. Aging Male Symptoms and International Prostate Symptom Score questionaires and prostate-related quality of life scores were completed and prostate ultrasonography (USG) was performed before and after the treatment...
December 2014: JPMA. the Journal of the Pakistan Medical Association
Jianghai Lu, María Fernández-Álvarez, Sheng Yang, Genye He, Youxuan Xu, Rodigo Aguilera
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...
January 2015: Journal of Mass Spectrometry: JMS
V Brancaleone, V Vellecco, D S Matassa, R d'Emmanuele di Villa Bianca, R Sorrentino, A Ianaro, M Bucci, F Esposito, G Cirino
BACKGROUND AND PURPOSE: Hydrogen sulphide (H2S) is a gaseous mediator strongly involved in cardiovascular homeostasis, where it provokes vasodilatation. Having previously shown that H2 S contributes to testosterone-induced vasorelaxation, here we aim to uncover the mechanisms underlying this effect. EXPERIMENTAL APPROACH: H2 S biosynthesis was evaluated in rat isolated aortic rings following androgen receptor (NR3C4) stimulation. Co-immunoprecipitation and surface plasmon resonance analysis were performed to investigate mechanisms involved in NR3C4 activation...
March 2015: British Journal of Pharmacology
Malik Shoaib Ahmad, Salman Zafar, Marium Bibi, Saira Bano, Atia-Tul-Wahab, Atta-Ur-Rahman, M Iqbal Choudhary
Fermentation of mesterolone (1) with Cunninghamella blakesleeana yielded four new metabolites, 1α-methyl-1β,11β,17β-trihydroxy-5α-androstan-3-one (2), 1α-methyl-7α,11β,17β-trihydroxy-5α-androstan-3-one (3), 1α-methyl-1β,6α,17β-trihydroxy-5α-androstan-3-one (4) and 1α-methyl-1β,11α,17β-trihydroxy-5α-androstan-3-one (5), along with three known metabolites, 1α-methyl-11α,17β-dihydroxy-5α-androstan-3-one (6), 1α-methyl-6α,17β-dihydroxy-5α-androstan-3-one (7) and 1α-methyl-7α,17β-dihydroxy-5α-androstan-3-one (8)...
April 2014: Steroids
Karina Fontana, Gerson E R Campos, Robert S Staron, Maria Alice da Cruz-Höfling
In an attempt to shorten recovery time and improve performance, strength and endurance athletes occasionally turn to the illicit use of anabolic-androgenic steroids (AAS). This study evaluated the effects of AAS treatment on the muscle mass and phenotypic characteristics of transgenic mice subjected to a high-intensity, aerobic training program (5d/wk for 6 weeks). The transgenic mice (CETP(+/-)LDLr(-/+)) were engineered to exhibit a lipid profile closer to humans. Animals were divided into groups of sedentary (Sed) and/or training (Ex) mice (each treated orally with AAS or gum arabic/vehicle: Sed-C, Sed-M, ex-C, ex-M)...
2013: PloS One
Andrew R McKinney, Adam T Cawley, E Bruce Young, Carmel M Kerwick, Karen Cunnington, Rhiannon T Stewart, Joseph I Ambrus, Anthony C Willis, Malcolm D McLeod
BACKGROUND: Effective control of the use of anabolic-androgenic steroids (AASs) in animal sports is essential in order to ensure both animal welfare and integrity. In order to better police their use in Australian and New Zealand greyhound racing, thorough metabolic studies have been carried out on a range of registered human and veterinary AASs available in the region. RESULTS: Canine metabolic data are presented for the AASs boldenone, danazol, ethylestrenol, mesterolone, methandriol, nandrolone and norethandrolone...
April 2013: Bioanalysis
Marco Galesio, Cristina Núñez, Mario S Diniz, Richard Welter, Carlos Lodeiro, José Luis Capelo
To make the use of MALDI-based mass spectrometry feasible for the fast analysis of oxosteroids, three new aromatic probes have been designed to be used simultaneously as derivatisation agents and MALDI matrices. This concept brings a number of benefits: the sample handling is reduced, the workflow is less time consuming allowing high throughput and the interferences caused by the MALDI matrix are avoided. Identification was successfully attained for all oxosteroids used in this study. As proof-of-concept, the identification of oxosteroids in urine was performed to evaluate the robustness of the new methodology...
October 15, 2012: Talanta
Karina Fontana, Thalita Rocha, Maria Alice da Cruz-Höfling
Anabolic-androgenic steroids (AAS) and exercise share comparable effects on myogenic differentiation, force development, fiber growth and skeletal muscle plasticity. The participation of nitric oxide synthase (NOS) on these effects was only demonstrated in response to exercise. Using immunohistochemistry and western blotting we examined the effect of AAS on the expression of NOS I and III isoforms in three muscles, distinct metabolically and physiologically: soleus (SOL), tibialis anterioris (TA) and gastrocnemius (GAS)...
November 2012: Histology and Histopathology
Cindy V Josol, Myrna Buenaluz-Sedurante, Mark Anthony Sandoval, Gerry Castillo
A 55-year-old Filipina with Grave's disease, diabetes, hypertension, bronchial asthma, Parkinson's disease and a history of adverse drug reaction to penicillin consulted due to high-grade fever and sore throat. Patient was diagnosed with aplastic anaemia secondary to methimazole and was treated with high-dose granulocyte colony stimulating factor, thrombopoietin and mesterolone. Antibiotics used included levofloxacin, clindamycin, amikacin and fluconazole. Due to bleeding and slow recovery of blood parameters, 30 units of platelets and 7 units of packed red blood cells were transfused during her 22-day admission...
2010: BMJ Case Reports
Mark R Feneley, Malcolm Carruthers
INTRODUCTION: For men with androgen deficiency on testosterone replacement therapy (TRT), clinical concern relates to the development of prostate cancer (PCa). AIM: An updated audit of prostate safety from the UK Androgen Study was carried out to analyze the incidence of PCa during long-term TRT. MAIN OUTCOME MEASURES: Diagnosis of PCa in men receiving TRT, by serum prostate-specific antigen (PSA) testing and digital rectal examination (DRE), and its relation to different testosterone preparations...
August 2012: Journal of Sexual Medicine
Giovanni Corona, Giulia Rastrelli, Linda Vignozzi, Mario Maggi
INTRODUCTION: Since the phenotype and clinical need of the hypogonadal individuals changes dramatically over time, versatile therapies are needed. AREAS COVERED: The authors review the available evidence on possible therapies. EXPERT OPINION: In the case of primary hypogonadism starting early in life, substitution with testosterone (T) is the only choice. For secondary congenital hypogonadism, we recommend starting with gonadotrophins to allow the testes to reach pubertal size...
June 2012: Expert Opinion on Emerging Drugs
Yulia B Monakhova, Thomas Kuballa, Sigrid Löbell-Behrends, Sibylle Maixner, Matthias Kohl-Himmelseher, Winfried Ruge, Dirk W Lachenmeier
Dietary supplements and medicines are widely marketed over the Internet. Such products may be counterfeited and lack some or all of the labelled ingredients, or, in the case of lifestyle supplements, illegally contain pharmacologically active substances, such as anorectic or androgenic compounds. The market control - especially in the case of customs seizures - is complex, as reference substances necessary for identification and calibration in traditional high performance liquid chromatography (HPLC) or gas chromatography-mass spectrometry (GC-MS) analysis are often unavailable, or extremely expensive...
June 2013: Drug Testing and Analysis
Mohammed Z Allouh, Mohammed H Aldirawi
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...
May 2012: Anatomical Record: Advances in Integrative Anatomy and Evolutionary Biology
M Galesio, M Mazzarino, X de la Torre, F Botrè, J L Capelo
A comparison between ultrasonication and microwave irradiation as tools to achieve a rapid sample treatment for the analysis of banned doping substances in human urine by means of gas chromatography-mass spectrometry (GC-MS) was performed. The following variables were studied and optimised: (i) time of treatment, (ii) temperature, (iii) microwave power and (iv) ultrasonic amplitude. The results were evaluated and compared with those achieved by the routine method used in the World Anti-Doping Agency (WADA) accredited Antidoping Laboratory of Rome...
January 2011: Analytical and Bioanalytical Chemistry
Karina Fontana, Fernanda M Almeida, Tatiana Carla Tomiosso, Edson Rosa Pimentel, Maria Alice da Cruz Höfling
The effect of mesterolone and intensive treadmill training (6 weeks, 5 days/week, means: 15.82 m/min and 45.8 min/day) in Achilles tendon remodeling was evaluated. Sedentary mice treated with mesterolone (Sed-M) or vehicle (Sed-C, placebo/control) and corresponding exercised (Ex-M and Ex-C) were examined. SDS-polyacrylamide gel electrophoresis was used for determining collagen bands and hydroxyproline concentration. Collagen fibril diameter, the area and number of fibrils contained in an area probe, and the ultrastructure of fibroblasts (tenocytes) were determined...
February 2010: Cell and Tissue Research
Karina Fontana, Kathryn E White, Gerson E R Campos, Maria-Alice da Cruz-Höfling, John B Harris
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...
2010: Journal of Electron Microscopy
M Iqbal Choudhary, S Adnan, A Shah, Atta-Ur-Rahman
Microbial transformation of two anabolic steroids, ethylestrenol (1) and nandrolone (2), were carried out. Ethylestrenol (1), when incubated with Rhizopus stolonifer (TSY 0471), yielded two oxidative metabolites named 17alpha-ethyl-3beta,17beta-dihydroxy-19-norndrost-4-ene (3) and 17alpha-ethyl-17beta-hydroxy-19-norandrost-4-en-3-one (4), while incubation of compound 2 with the same fungus yielded two oxidative metabolites, 19-norandrost-4-en-3,17-dione (5) and 6alpha,17beta-dihydroxy-19-norandrost-1,4-dien-3-one (6)...
2008: Natural Product Research
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