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Steroids Mar 2020Two valuable forensic tools based on enzyme-linked immunoassays (ELISAs) for the analysis of 17α-methylated steroids were developed using haptens of stanazolol and its...
Two valuable forensic tools based on enzyme-linked immunoassays (ELISAs) for the analysis of 17α-methylated steroids were developed using haptens of stanazolol and its conjugates with biotin. Haptens containing terminal carboxylic group were conjugated to bovine serum albumin (BSA), rabbit serum albumin (RSA) or ovalbumin (OVA). Eight batches of antisera (RAbs) obtained by immunization of rabbits were tested in an indirect competitive ELISA system using immobilization of RSA conjugate (RSA/hapten) and competitor immobilization of the biotinylated conjugate (AB-ELISA) to avidin (avidin/hapten). The best results were achieved with the RAb 212 antibodies in RSA/ST-3 and avidin/ST-10 assembled variants. For the RSA/ST-3 system, an IC of 0.3 ng/mL and a detection limit of 0.02 ng/mL were measured. In case of avidin/ST-10 variant, IC was of 3.9 ng/mL and a detection limit of 0.57 ng/mL were obtained. The effect of solvent was tested as well as the stability of coated microtiter plates over four-month period. The cross-reactivity of the developed assays with other anabolic steroids was tested and high sensitivity towards 17α-methylated steroids was observed. RSA/ST-3 assay showed significant cross-reactivity with 17α-methyltestosterone (81.2%), oxymetholone (30.4%), methandienone (10.0%) and methyl dihydrotestosterone (7.7%). Similarly, in the avidin/ST-10 assay, 17α-methyltestosterone (34.5%), mestanolone (32.1%), oxymetholone (22.7%), methandienone (14.2%), 9-dehydromethyltestosterone (12.5%) and oxandrolone (1.2%) exhibited high cross-reactivity. The functionality of the developed systems was verified by the successful identification of a series of 17α-methylated anabolic steroids in a set of real samples including pharmaceutical preparations seized by the Police of the Czech Republic on the black market.
Topics: Animals; Calibration; Cattle; Enzyme-Linked Immunosorbent Assay; Forensic Medicine; Immune Sera; Methylation; Molecular Conformation; Rabbits; Serum Albumin; Stanozolol; Stereoisomerism; Testosterone Congeners
PubMed: 31812623
DOI: 10.1016/j.steroids.2019.108550 -
British Journal of Haematology Oct 2019
Topics: Adult; Aged; Aged, 80 and over; Androgens; Danazol; Female; Humans; Male; Middle Aged; Myelodysplastic Syndromes; Oxymetholone; Retrospective Studies; Thrombocytopenia; Treatment Outcome; Young Adult
PubMed: 31368111
DOI: 10.1111/bjh.16121 -
Steroids Oct 2019A long-term metabolite of the doping agent oxymetholone (OXM-M2, 17β-hydroxymethyl-2,17α-methyl-18-norandrost-13-en-3-one) which has been identified by GC-MS/MS was...
A long-term metabolite of the doping agent oxymetholone (OXM-M2, 17β-hydroxymethyl-2,17α-methyl-18-norandrost-13-en-3-one) which has been identified by GC-MS/MS was synthesized from commercially available materials. Two efficient synthetic routes to access both C-17 epimers of tentative metabolites were developed. The identity and molecular configuration of the in vivo metabolite: 17β-hydroxymethyl-2α,17α-methyl-18-norandrost-13-en-3-one was confirmed by single crystal X-ray diffraction.
Topics: Crystallography, X-Ray; Humans; Models, Molecular; Molecular Conformation; Oxymetholone
PubMed: 31229510
DOI: 10.1016/j.steroids.2019.108430 -
Andrologia Aug 2019Testicular tissue and sex hormones are sensitive to the anabolic steroids (oxymetholone/OM) due to increased free radical damage and hormonal changes. The Nasturtium...
Testicular tissue and sex hormones are sensitive to the anabolic steroids (oxymetholone/OM) due to increased free radical damage and hormonal changes. The Nasturtium officinale L. have various antioxidant compounds. The aim of the present study was to investigate N. officinale effect on OM-induced oxidative injury in mouse testis and sperm parameters. Thirty BALB/c mice were divided into five groups, including control, OM (5 ml/kg) and three N. officinale doses (25, 50 and 100 mg/kg) + OM. At the end of the study (40 days), serum luteinising hormone (LH), follicle-stimulating hormone (FSH), testosterone, nitric oxide (NO) levels, ferric reducing ability of power (FRAP) and testis stereological factors were measured. The sperm parameters were evaluated. Liquid chromatography-electrospray ionisation-tandem mass spectrometry (LC-ESI/MS) analysis was yielded a fingerprint of N. officinale phenolic constituents. 100 mg/kg of N. officinale extract significantly reduced the serum level of testosterone and a significant increase in LH and FSH in comparison with the control group. This dose also significantly improved the stereological factors and sperm parameters. 50 and 100 mg/kg of N. officinale extract significantly increased the testis tissue FRAP levels, and 100 doses reduced the serum levels of NO. Fourteen compounds and 34 peaks were identified in the extract with LC-ESI/MS. Nasturtium officinale extract has protective effects against testicular toxicity caused by OM.
Topics: Anabolic Agents; Animals; Antioxidants; Chromatography, High Pressure Liquid; Male; Mice; Models, Animal; Nasturtium; Oxidative Stress; Oxymetholone; Plant Extracts; Spectrometry, Mass, Electrospray Ionization; Sperm Count; Spermatozoa; Tandem Mass Spectrometry; Testis; Testosterone
PubMed: 31025410
DOI: 10.1111/and.13294 -
Neuroscience and Biobehavioral Reviews May 2019Supraphysiologic-dose anabolic-androgenic steroid (AAS) use is associated with physiologic, cognitive, and brain abnormalities similar to those found in people at risk... (Review)
Review
Supraphysiologic-dose anabolic-androgenic steroid (AAS) use is associated with physiologic, cognitive, and brain abnormalities similar to those found in people at risk for developing Alzheimer's Disease and its related dementias (AD/ADRD), which are associated with high brain β-amyloid (Aβ) and hyperphosphorylated tau (tau-P) protein levels. Supraphysiologic-dose AAS induces androgen abnormalities and excess oxidative stress, which have been linked to increased and decreased expression or activity of proteins that synthesize and eliminate, respectively, Aβ and tau-P. Aβ and tau-P accumulation may begin soon after initiating supraphysiologic-dose AAS use, which typically occurs in the early 20s, and their accumulation may be accelerated by other psychoactive substance use, which is common among non-medical AAS users. Accordingly, the widespread use of supraphysiologic-dose AAS may increase the numbers of people who develop dementia. Early diagnosis and correction of sex-steroid level abnormalities and excess oxidative stress could attenuate risk for developing AD/ADRD in supraphysiologic-dose AAS users, in people with other substance use disorders, and in people with low sex-steroid levels or excess oxidative stress associated with aging.
Topics: Alzheimer Disease; Amyloid beta-Peptides; Androgens; Animals; Brain; Dementia; Humans; Hypogonadism; Oxidative Stress; Phosphorylation; Risk Factors; Testosterone Congeners; tau Proteins
PubMed: 30817935
DOI: 10.1016/j.neubiorev.2019.02.014 -
Caspian Journal of Internal Medicine 2018The prevalence of using anabolic steroids such as oxymetholone is increasing. This highlights the need for closely monitoring side effects of this drug. Acute renal...
BACKGROUND
The prevalence of using anabolic steroids such as oxymetholone is increasing. This highlights the need for closely monitoring side effects of this drug. Acute renal failure (ARF) has been reported as a complication of rhabdomyolysis in anabolic steroids users.
CASE PRESENTATION
We present one 33-year-old man complaining of decreased urine volume, urine color change, and lower abdominal pain. He is engaged with a rare side effect of oxymetholone abuse. During assessments of potential medical issues associated with the intake of anabolic steroids, known side effects are known to be transient, but the need for appropriate interventions remains essential.
CONCLUSIONS
Rhabdomyolysis due to drug use and the consequent acute kidney injury are among the lethal risks associated with anabolic steroid abuse. In most cases, the symptoms are extensive and often misleading. Therefore, detailed history taking, physical scrutiny, paraclinical testing, and early diagnosis are crucial for rhabdomyolysis patients.
PubMed: 30510659
DOI: 10.22088/cjim.9.4.406 -
Journal of the International Society of... Oct 2018A proprietary composition GMCT contains extracts of two popular Asian herbs viz., Garcinia mangostana (GM) fruit rind and Cinnamomum tamala (CT) leaf. We systematically... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
A proprietary composition GMCT contains extracts of two popular Asian herbs viz., Garcinia mangostana (GM) fruit rind and Cinnamomum tamala (CT) leaf. We systematically evaluated physical performance and muscle strength enhancing ability of GMCT in a preclinical mouse model followed by a 42-days double-blind placebo controlled human trial in resistance trained adult males.
METHODS
Four groups of Swiss albino mice (20-30 g body weight) (n = 6) were fed a standard laboratory diet and given Carboxymethylcellulose sodium (CMC), 150 mg/kg GMCT (GMCT-150), 300 mg/kg GMCT (GMCT-300) or 50 mg/kg Oxymetholone (OXY) via oral gavage for 21 days. On day 22, the animals' physical performance and muscle strength were assessed in a forced swimming test (FST) and forelimb grip strength experiment, respectively. In the human trial, thirty-eight resistance-trained young adults (mean age 26.32 ± 4.39 years, body weight 67.79 ± 12.84 kg, BMI 22.92 ± 3.54 kg/m) completed the trial. The participants received either GMCT (n = 19; 800 mg daily) or matched placebo (n = 19) for 42 days. As primary variables, 1-RM bench press, 1-RM leg press, and leg extension repetitions were measured at baseline and on days 14, 28 and 42 of the intervention. Anthropometric parameters and serum markers such as free testosterone, insulin-like growth factor 1 (IGF-1), insulin and lactate were also measured before and after the intervention.
RESULTS
GMCT-300 mice showed significant improvement in swimming time (GMCT: 395.3 ± 81.70 s vs. CMC: 271.6 ± 56.86 s; p = 0.0166), distance (GMCT: 341.22 ± 65.88 m vs. CMC: 260.84 ± 49.15 m; p = 0.0461) and grip strength (GMCT: 43.92 ± 6.97 N vs. CMC: 35.0 ± 6.92 N; p = 0.0490), compared with the CMC group. At the end of the 42-day human trial, the per protocol analyses reveal that mean changes from baseline 1-RM bench press (GMCT: 23.47 ± 10.07 kg vs. PL: 3.42 ± 2.06 kg; p < 0.0001), leg press (GMCT: 29.32 ± 16.17 kg vs. PL: 5.21 ± 1.72 kg; p < 0.0001), number of leg extension repetitions (GMCT: 6.58 ± 2.57 vs. PL: 2.05 ± 1.22; p < 0.0001) in GMCT group were significantly improved, compared with placebo. Intergroup difference analyses show that the changes from baseline left arm (GMCT: 1.09 ± 0.36 cm vs. PL: 0.68 ± 0.42 cm; p = 0.0023), right arm (GMCT: 1.50 ± 0.44 cm vs. PL: 1.11 ± 0.43 cm; p = 0.0088) circumference and lean mass (GMCT: 2.29 ± 2.09 kg vs. PL: 0.52 ± 2.58 kg; p = 0.0404) in GMCT group were also significantly improved, compared with placebo. In comparison to placebo, GMCT supplementation did not improve free testosterone, IGF-1, insulin or lactate levels. Parameters of clinical biochemistry, hematology, urine and vital signs of the participants were within the normal range.
CONCLUSION
GMCT supplementation is effective in increasing muscle strength, muscle size and, total lean mass, as well as endurance performance.
TRIAL REGISTRATION
Clinical Trial Registry of India (CTRI/2015/01/005374), Registered on Jan 07, 2015; CTRI Website URL - http://ctri.nic.in.
Topics: Adult; Animals; Cinnamomum; Double-Blind Method; Fruit; Garcinia mangostana; Humans; Insulin; Insulin-Like Growth Factor I; Lactic Acid; Male; Mice; Muscle Strength; Physical Endurance; Plant Extracts; Plant Leaves; Resistance Training; Testosterone; Young Adult
PubMed: 30348185
DOI: 10.1186/s12970-018-0257-4 -
PloS One 2018Helium, a minor component of natural gas and radioactive minerals, is most commonly used as a carrier in gas chromatography-mass spectrometry (GC-MS). Its scarcity leads...
Helium, a minor component of natural gas and radioactive minerals, is most commonly used as a carrier in gas chromatography-mass spectrometry (GC-MS). Its scarcity leads to limited availability and higher costs. In this experiment, hydrogen from a safe source of a hydrogen generator was tested as a substitutive carrier gas for the detection of adulterant in traditional Chinese medicine (TCM) and food supplements by GC-MS analysis. We found that the limits of detection (LODs) of using hydrogen were from 10 to 1000 μg/g. The levels of LODs tested among 170 drugs remain the same whether hydrogen or helium was used as a carrier gas with the exception of 7 drugs-benzbromarone, estradiol benzoate, bezafibrate, mefenamic acid, oxymetholone, piperidenafil and cetilistat. The real sample analysis results using hydrogen were as satisfactory as those using helium. In addition, the retention time was shortened after the chromatographic performance was optimized. In summary, it is worth considering hydrogen as a carrier gas due to its affordable costs, energy efficiency, carbon reduction and chromatographic advantages to detect adulterated drugs in TCM and dietary supplement using GC-MS.
Topics: Chlorzoxazone; Dietary Supplements; Drug Contamination; Drugs, Chinese Herbal; Gas Chromatography-Mass Spectrometry; Helium; Humans; Hydrogen; Limit of Detection; Oxymetholone; Pyrimidinones; Sildenafil Citrate; Sulfones
PubMed: 30304050
DOI: 10.1371/journal.pone.0205371 -
Steroids Oct 2018Counterfeiting and adulteration of pharmaceuticals is a prevalent problem worldwide and represents a major health risk to the population, with anabolic steroids being...
Counterfeiting and adulteration of pharmaceuticals is a prevalent problem worldwide and represents a major health risk to the population, with anabolic steroids being one of the main classes of drugs consumed and obtained from dubious sources. In this work, we propose the use of the H NMR technique to evaluate formulations containing anabolic steroids, with analysis of 40 samples of anabolic drugs that are used in injectable and capsule forms. The samples analyzed presented the following active ingredients: testosterone propionate, testosterone phenylpropionate, testosterone isocaproate, testosterone decanoate, testosterone cypionate, testosterone undecanoate, stanozolol, drostanolone propionate, trenbolone acetate, oxymetholone, and methandrostenolone. The H NMR spectroscopic measurements were performed using a 600 MHz Bruker Avance III spectrometer, with deuterated chloroform (CDCl) containing 0.1% TMS as solvent. Of the 40 samples analyzed, eight did not show the presence of the active principle stated on the label. Three types of adulteration were found in the analyzed samples: absence of the active ingredient, adulteration with other substances, and concentration values below those indicated on the label. Sildenafil citrate was found in four samples. The GC-MS technique was used to confirm the adulteration results found using H NMR. Quantitative determination by NMR was performed using internal standard and ERETIC 2 methods, and the results obtained were statistically the same.
Topics: Gas Chromatography-Mass Spectrometry; Proton Magnetic Resonance Spectroscopy; Sildenafil Citrate; Steroids; Testosterone Congeners
PubMed: 30003910
DOI: 10.1016/j.steroids.2018.07.002 -
Journal of Pediatric Hematology/oncology Apr 2019Fanconi anemia (FA) is an autosomal recessive, progressive bone marrow failure disorder characterized by congenital defects and marked cancer predisposition....
Fanconi anemia (FA) is an autosomal recessive, progressive bone marrow failure disorder characterized by congenital defects and marked cancer predisposition. Hematopoietic stem cell transplant is the therapy of choice for FA patients with progressive pancytopenia. These patients receive multiple transfusions for cytopenias. Oxymetholone has been used with variable success to improve cytopenias. Eltrombopag has been shown to induce bilineage or trilineage hematopoiesis in aplastic anemia and patients with myelodysplastic marrow. We report a case of FA where eltrombopag in conjunction with oxymetholone induced trilineage hematopoiesis and eliminated transfusion requirement before transplant, thereby enhancing favorable outcome after hematopoietic stem cell transplant.
Topics: Benzoates; Drug Therapy, Combination; Fanconi Anemia; Hematopoiesis; Hematopoietic Stem Cell Transplantation; Humans; Hydrazines; Oxymetholone; Pancytopenia; Pyrazoles
PubMed: 29668547
DOI: 10.1097/MPH.0000000000001168