There is increasing pressure on meat producers worldwide due to the need for higher yields and improved meat quality. This is why anabolic androgenic steroids (AAS) have been widely used in most countries, due to their ability to accelerate animal muscle growth. However, out of concern for their side effects, EU states have banned their use and implemented control mechanisms. But they are reaching their limits, and therefore, it is necessary to look for new ways and investigate the mechanism of action of AAS on muscle tissue. This study replicated the administration of banned AAS (testosterone, nandrolone and their combination) and observed their effect on pig muscle. The pig model was purposely chosen for the study, as no such research has been carried out on this species. At the same time, pork is one of the most consumed meats in Europe. It focused on histological changes in muscle structure, specifically the size of muscle fibres and the number of satellite cells per muscle fibre. Furthermore, ultrastructural changes in muscle fibres, the diameter of myofibrils, the number of myofibrils per area, the distance between myofibrils and the size of sarcomeres were examined. The results using the techniques of histology, fluorescent labelling and transmission electron microscopy showed that, after the application of AAS, there is an increase in the diameter of muscle fibres, an increase in the diameter of myofibrils, a decrease in the number of myofibrils per surface area and, in the case of testosterone, an increase in the distance between myofibrils and an increase in the length of sarcomeres. There was also a significant increase in the number of satellite cells per muscle fibre. The detected statistically significant differences between control and experimental groups provide evidence that selected histological parameters could be additional mechanisms for detecting the presence of AAS in pork meat in the future.
- Klíčová slova
- anabolic steroids, electron microscopy, histology, muscles, pigs,
- MeSH
- anabolika * farmakologie MeSH
- androgeny farmakologie MeSH
- kosterní svalová vlákna * účinky léků ultrastruktura MeSH
- kosterní svaly účinky léků ultrastruktura MeSH
- myofibrily * účinky léků ultrastruktura MeSH
- nandrolon * farmakologie aplikace a dávkování MeSH
- prasata MeSH
- satelitní buňky kosterního svalu účinky léků MeSH
- testosteron * farmakologie aplikace a dávkování MeSH
- transmisní elektronová mikroskopie veterinární MeSH
- zvířata MeSH
- Check Tag
- mužské pohlaví MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- anabolika * MeSH
- androgeny MeSH
- nandrolon * MeSH
- testosteron * MeSH
Synthetic derivatives of steroid hormones, specifically anabolic-androgenic steroids (AAS), have gained prominence due to their observed benefits in enhancing meat quality. The study replicated the administration of banned AAS and investigated their impacts on pigs to contribute to the understanding of animal biochemistry and to explore the feasibility of detecting AAS administration by employing a non-targeted analysis. The effects were corroborated by evaluating changes in the expression of selected proteins, as well as examining haematological and biochemical profiles and histological alterations. Exposure to AAS influenced the expression of proteins related to drug-metabolizing enzymes, muscle and lipid metabolism, kidney function, reproductive processes, immune system functions, and carcinogenic changes. The effects of AAS appear intricate and contingent on factors such as the specific drug used, dosage, and duration of administration. The results underscore that protein expression analysis holds promise as a valuable tool for detecting illicit AAS use in the fattening process.
- Klíčová slova
- drugs, histology, muscle, proteomics, testes,
- MeSH
- anabolické androgenní steroidy * toxicita MeSH
- nandrolon * toxicita MeSH
- prasata MeSH
- testosteron MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- anabolické androgenní steroidy * MeSH
- nandrolon * MeSH
- testosteron MeSH
PURPOSE OF THE STUDY Persistent catabolism is one of the main causes of delayed healing in polytrauma patients. The purpose of this study is to verify the effect of early administration of an anabolic steroid in combination with vitamin D on the process of bone healing in polytrauma patients. MATERIAL AND METHODS In this prospective study, the patients with a serious trauma were divided into two groups (a control group and a treatment group), with the treatment group being treated with nandrolone decanoate, an anabolic steroid in combination with vitamin D. In all the patients, bone metabolism markers and sex hormone levels (men only) were monitored through lab testing for the period of 70 days and the results of both the groups were subsequently compared. RESULTS The study included a total of 64 patients, 32 in the control group and 32 in the treatment group. The differences between the groups in gender (p = 0.387) as well as in the age of patients (p = 0.436) were statistically non-significant. There was a significant difference in the Injury Severity Score (48 in the treatment group as against 41 in the control group, p = 0.022). Even though this difference was statistically significant, it cannot be considered clinically significant since all the patients met the major trauma criteria. No positive effect of this treatment on bone metabolism parameters was established; on the very contrary, the only statistically significant changes were observed in the control group. To be specific, in levels of one of the bone formation markers, bone alkaline phosphatase on Day 7 after the injury (an increased level in the control group; p = 0.002) and in one of the bone resorption markers (bone acid phosphatase) on Day 70 after the injury (an increased level in the treatment group; p = 0.042). In the treatment group, 70 days after the injury a higher 25(OH)vitamin D level (p < 0.001) was reported and starting from Day 7 in men in the treatment group a significantly lower testosterone level and free testosterone level were observed. The level of androgenic hormones dramatically dropped in both the groups during the first days after the trauma, the dynamics of its normalization was faster in patients in the control group than in the treatment group. DISCUSSION The administration of nandrolone decanoate, an anabolic steroid, in combination with vitamin D did not produce the expected effect, i.e. an improvement in bone healing markers in polytrauma patients. One would expect that in polytrauma patients with a bone fracture or fractures during bone healing higher levels of all the markers of bone resorption as well as bone formation will persist. Similar increases in bone metabolism levels, however, were observed also in patients with injuries in other somatic regions. This indicates the importance of bone tissue involvement in the overall response of the organism to polytrauma. A faster normalization of the levels of testosterone, dihydrotestosterone and free testosterone in the control group compared to the treatment group corresponds with the supplemental effect of anabolic steroids and reduced production of these hormones as a feedback to hypothalamic-pituitary-adrenal axis. CONCLUSIONS In the follow-up period, the positive effect of anabolic steroid and vitamin D administration on bone metabolism in polytrauma patients was not confirmed. Key words: polytrauma, anabolic steroids, vitamin D, bone metabolism.
- MeSH
- anabolika * škodlivé účinky MeSH
- lidé MeSH
- nandrolon dekanoát MeSH
- polytrauma * farmakoterapie MeSH
- prospektivní studie MeSH
- systém hypofýza - nadledviny MeSH
- systém hypotalamus-hypofýza MeSH
- vitamin D MeSH
- Check Tag
- lidé MeSH
- mužské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- klinické zkoušky kontrolované MeSH
- Názvy látek
- anabolika * MeSH
- nandrolon dekanoát MeSH
- vitamin D MeSH
This study reports the development and validation of a new, simple, and accurate high-performance thin-layer chromatography (HPTLC)-densitomeric method for the determination of nandrolone decanoate in a commercially available injection formulation. Chromatographic analysis was performed on glass CN modified silica gel 60F254 plates developed using n-hexane-ethyl acetate in volume ratio 42.5:7.5 as the mobile phase. Densitometric scanning was carried out at the wavelength of 245 nm. This chromatographic system gave compact spot and a symmetrical peak of nandrolone decanoate with retardation factor (RF) value at 0.57 (±0.02). The linearity of this method with the high correlation coefficient of calibration plot ranges from 0.780 to 12.500 μg/spot. The developed method is characterized by good precision (coefficient of variation CV < 2%) and high accuracy close to 100.3% (R = 99.0%). Values of limits of detection and quantification equal to 0.231 and 0.700 μg/spot, respectively, confirm the sensitivity of the developed method. The analysis of the pharmaceutical formulation of nandrolone decanoate indicates drug content of 50.5 mg/mL and 101.0% in relation to the label claim. This is in good agreement with the recommendation of the International Council for Harmonisation (ICH) guidelines as well as the pharmacopoeial requirements. The low CV value (<1%) of nandrolone decanoate content in the tested injection formulation confirms the suitability of the proposed HPTLC-densitometric method for routine control of this compound in examined pharmaceuticals.
- Klíčová slova
- HPTLC, densitometry, nandrolone decanoate, steroids,
- MeSH
- chromatografie na tenké vrstvě * metody normy MeSH
- denzitometrie * metody normy MeSH
- léčivé přípravky analýza MeSH
- nandrolon dekanoát analýza MeSH
- příprava léků MeSH
- reprodukovatelnost výsledků MeSH
- senzitivita a specificita MeSH
- vysokoúčinná kapalinová chromatografie * metody normy MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- léčivé přípravky MeSH
- nandrolon dekanoát MeSH
OBJECTIVE: The aim of this prospective, unicentric, cohort study was to evaluate the effect of dienogest use in the therapy of symptomatic endometriosis of rectovaginal septum in patients of fertile age. STUDY DESIGN: Prospective, unicentric, cohort study. SETTING: Department of Obstetrics and Gynaecology, Brno University Hospital and Masaryk University Medical School, Brno. MATERIAL AND METHODS: Prospective analysis of the group of 32 patients in reproductive age who have previously been diagnosed with endometriosis of rectovaginal septum. These patients were treated conservatively with dienogest 2 mg per day during a 24-week period. Through questionnaires and clinical assessment, we have studied the presence of symptoms like dyspareunia, diffuse pelvic pain, Biberoglu-Behrman(B-B) score assessment and subjective pain perception using Visual Analogue Scale (VAS) of pain. Data were collected at the beginning of therapy, after 4, 12 and 24 weeks of dienogest use. RESULTS: Continual use of dienogest during the 24-week period diminishes symptoms of dyspareunia by 62% (p.
- Klíčová slova
- Endometriosis, dienogest, dyspareunia, pelvic pain, rectovaginal septum,
- MeSH
- antagonisté hormonů terapeutické užití MeSH
- endometrióza farmakoterapie patologie MeSH
- kohortové studie MeSH
- kvalita života MeSH
- lidé MeSH
- měření bolesti MeSH
- nandrolon analogy a deriváty terapeutické užití MeSH
- pánevní bolest etiologie MeSH
- prospektivní studie MeSH
- rektum patologie MeSH
- vagina patologie MeSH
- výsledek terapie MeSH
- Check Tag
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- antagonisté hormonů MeSH
- dienogest MeSH Prohlížeč
- nandrolon MeSH
A sensitive and robust confirmatory method for determination of steroid esters in blood serum is essential for reliable monitoring of possible illegal use of steroid hormones as growth promoters in meat production. A previously used sample preparation methodology was improved. The procedure consists of protein precipitation and removal of phospholipids by dispersive SPE Supel™ QuE Z-Sep (Sigma-Aldrich) followed by clean-up on alumina column and LC-MS/MS measurement. The modified method has been validated according to Commission Decision 2002/657/EC. Validation parameters for determination of six testosterone esters and five nortestosterone esters in bovine and porcine blood serum are presented in this article. Decision limits for all analytes were observed in the range 10-20 pg mL-1. The method described is considerably robust for bovine and porcine serum analyses and can be applied both for screening and confirmatory determination in routine residue monitoring.
- Klíčová slova
- LC-MS/MS, Steroid esters, blood serum, natural hormones,
- MeSH
- chromatografie kapalinová MeSH
- estery krev MeSH
- nandrolon krev MeSH
- prasata MeSH
- skot MeSH
- tandemová hmotnostní spektrometrie MeSH
- testosteron krev MeSH
- zvířata MeSH
- Check Tag
- skot MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- estery MeSH
- nandrolon MeSH
- testosteron MeSH
STUDY OBJECTIVE: To study the safety and efficacy of dienogest 2 mg in adolescents with suspected endometriosis. DESIGN: A 52-week, open-label, single-arm study. SETTING: In 21 study centers, in 6 European countries. PARTICIPANTS: Adolescents aged 12 to younger than 18 years with clinically suspected or laparoscopically confirmed endometriosis. INTERVENTIONS: Dienogest 2 mg once daily. MAIN OUTCOME MEASURES: The primary end point was relative change in lumbar spine (L2-L4) bone mineral density (BMD) measured using dual-energy x-ray absorptiometry. A key secondary end point was change in endometriosis-associated pain assessed using a visual analogue scale. RESULTS: Of 120 patients screened, 111 comprised the full-analysis set (ie, patients who took ≥1 dose of study drug and had ≥1 post-treatment observation) and 97 (87.4%) completed the study. Mean lumbar BMD at baseline was 1.1046 (SD, 0.1550) g/cm2. At the end of dienogest treatment (EOT; defined as at 52 weeks or premature study discontinuation), mean relative change in BMD from baseline was -1.2% (SD, 2.3%; n = 103). Follow-up measurement 6 months after EOT in the subgroup with decreased BMD at EOT (n = 60) showed partial recovery in lumbar BMD (mean change from baseline: -2.3% at EOT, -0.6% 6 months after EOT). Mean endometriosis-associated pain score was 64.3 (SD, 19.1) mm at baseline and decreased to 9.0 (SD, 13.9) mm by week 48. CONCLUSION: In adolescents with suspected endometriosis, dienogest 2 mg for 52 weeks was associated with a decrease in lumbar BMD, followed by partial recovery after treatment discontinuation. Endometriosis-associated pain was substantially reduced during treatment. Because bone accretion is critical during adolescence, results of the VISanne study to assess safety in ADOlescents (VISADO) study highlights the need for tailored treatment in this population, taking into account the expected efficacy on endometriosis-associated pain and an individual's risk factors for osteoporosis.
- Klíčová slova
- Adolescent, Bone mineral density, Dienogest, Endometriosis, Pelvic pain,
- MeSH
- absorpční fotometrie MeSH
- antagonisté hormonů škodlivé účinky terapeutické užití MeSH
- bederní obratle MeSH
- dítě MeSH
- endometrióza farmakoterapie MeSH
- kostní denzita účinky léků MeSH
- lidé MeSH
- měření bolesti MeSH
- mladiství MeSH
- nandrolon škodlivé účinky analogy a deriváty terapeutické užití MeSH
- pánevní bolest farmakoterapie MeSH
- Check Tag
- dítě MeSH
- lidé MeSH
- mladiství MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
- Geografické názvy
- Evropa MeSH
- Názvy látek
- antagonisté hormonů MeSH
- dienogest MeSH Prohlížeč
- nandrolon MeSH
Avidin-biotin technology was used for the implementation of an enzyme-linked immunosorbent assay (AB-ELISA) as a sensitive method for the detection of anabolic androgenic steroids (AAS) present in dietary supplements. Using click chemistry, novel haptens (linker-optimized biotinylated nandrolone (NT) and testosterone (T) at positions C-3 and C-17, respectively) were designed and synthesized to be then applied as four different immobilized competitors in a proposed set of four indirect competitive AB-ELISAs. Four rabbit polyclonal antibodies of various specificities were prepared using four different immunogens synthesized from C-3 and C-17 carboxymethyloxime and hemisuccinate derivatives of NT and T, respectively. Assembled AB-ELISAs were characterized to establish method parameters such as a half-maximum inhibition concentration (0.18-12.99 ng/mL), limit of detection (0.004-0.032 ng/mL) and linear working range (the best with 0.02-1.38 ng/mL). The stability of the set simulating storage in different conditions was demonstrated. Cross reactivity (CR) was tested for 59 steroids including both endogenous and synthetic analogues in four assembled AB-systems. The focus was placed on the practical use of the method in detection of various AAS in 49 samples of counterfeit dietary supplements. The concordance between ultra high performance liquid chromatography-mass spectrometry (UHPLC-MS) and the CR corrected data from AB-ELISA indicated the potential of this method even to quantification of T propionate, NT phenyl propionate, and NT decanoate in such a complex matter. Copyright © 2016 John Wiley & Sons, Ltd.
- Klíčová slova
- ELISA, anabolics, avidin, biotin, dietary supplements, nandrolone, testosterone,
- MeSH
- anabolika analýza MeSH
- avidin chemie MeSH
- biotin chemie MeSH
- ELISA metody MeSH
- králíci MeSH
- limita detekce MeSH
- nandrolon analýza MeSH
- potravní doplňky analýza MeSH
- testosteron analýza MeSH
- zvířata MeSH
- Check Tag
- králíci MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- hodnotící studie MeSH
- Názvy látek
- anabolika MeSH
- avidin MeSH
- biotin MeSH
- nandrolon MeSH
- testosteron MeSH
Here, we report synthesis and biological evaluation of fluorescent nandrolone-3-carboxymethyloxime derivatives conjugated with green-emitting bodipy dye via PEG linkers. All the newly-synthesized compounds were evaluated for their effect on cell proliferation in vitro in MCF-7, LNCaP, PC-3 and HEK 293T model cell lines using WST-1 assay. By means of live-cell fluorescence microscopy, the intracellular localization of nandrolone-bodipy conjugates was revealed in endoplasmic reticulum. Moreover, we performed competitive localization study with nonfluorescent nandrolone, metandrolone, boldenone, trenbolone, and testosterone.
- Klíčová slova
- Androgens, Cytotoxicity, Fluorescent conjugates, Nandrolone,
- MeSH
- fluorescenční barviva chemická syntéza chemie MeSH
- fluorescenční mikroskopie MeSH
- HEK293 buňky MeSH
- HeLa buňky MeSH
- lidé MeSH
- MFC-7 buňky MeSH
- molekulární konformace MeSH
- nádorové buněčné linie MeSH
- nandrolon chemie farmakologie MeSH
- proliferace buněk účinky léků MeSH
- sloučeniny boru chemie farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene MeSH Prohlížeč
- fluorescenční barviva MeSH
- nandrolon MeSH
- sloučeniny boru MeSH
BACKGROUND: This study compared the bleeding pattern, cycle control and safety of an oral contraceptive (OC) comprising estradiol valerate/dienogest (E2V/DNG; administered using a dynamic dosing regimen) with a monophasic OC containing ethinyl estradiol 20 mcg/levonorgestrel 100 mcg (EE/LNG). E2V releases estradiol (E2), which is identical to endogenously produced 17beta-estradiol. STUDY DESIGN: This was a randomized, multicenter, double-blind, double-dummy trial lasting seven cycles in healthy women aged 18-50 years. RESULTS: Overall, 798 women were randomized and received allocated treatment (399 per group). There were significantly fewer bleeding/spotting days reported by women who received E2V/DNG than those who received EE/LNG [17.3+/-10.4 vs. 21.5+/-8.6, respectively, p<.0001, Reference Period 1 (Days 1-90); and 13.4+/-9.vs. 15.9+/-7.1, respectively, p<.0001, Reference Period 2 (Days 91-180)]. Through Cycles 1-7, the occurrence of scheduled withdrawal bleeding per cycle was 77.7-83.2% with E2V/DNG and 89.5-93.8% with EE/LNG (p<.0001 per cycle). The duration and intensity of scheduled withdrawal bleeding were reduced with E2V/DNG vs. EE/LNG. The incidence of intracyclic bleeding was similar with E2V/DNG (10.5%-18.6%) and EE/LNG (9.9%-17.1%) (p>.05 per cycle). No unintended pregnancies occurred with E2V/DNG, but there was one unintended pregnancy with EE/LNG. Adverse drug reactions occurred in 10.0% and 8.5% of women taking E2V/DNG and EE/LNG, respectively. Overall, 79.4% of women were satisfied with E2V/DNG and 79.9% with EE/LNG. CONCLUSIONS: A novel OC composed of E2V/DNG is associated with an acceptable bleeding profile that is comparable to that of an EE-containing OC.
- MeSH
- dospělí MeSH
- dvojitá slepá metoda MeSH
- estradiol škodlivé účinky analogy a deriváty farmakologie MeSH
- ethinylestradiol škodlivé účinky farmakologie MeSH
- fixní kombinace léků MeSH
- kontraceptiva orální kombinovaná škodlivé účinky farmakologie MeSH
- levonorgestrel škodlivé účinky farmakologie MeSH
- lidé středního věku MeSH
- lidé MeSH
- menstruační cyklus účinky léků MeSH
- menstruační poruchy chemicky indukované MeSH
- metroragie chemicky indukované MeSH
- mladiství MeSH
- mladý dospělý MeSH
- nandrolon škodlivé účinky analogy a deriváty farmakologie MeSH
- spokojenost pacientů statistika a číselné údaje MeSH
- výsledek terapie MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- mladiství MeSH
- mladý dospělý MeSH
- ženské pohlaví MeSH
- Publikační typ
- časopisecké články MeSH
- multicentrická studie MeSH
- práce podpořená grantem MeSH
- randomizované kontrolované studie MeSH
- srovnávací studie MeSH
- Názvy látek
- estradiol valerate-dienogest MeSH Prohlížeč
- estradiol MeSH
- ethinyl estradiol, levonorgestrel drug combination MeSH Prohlížeč
- ethinylestradiol MeSH
- fixní kombinace léků MeSH
- kontraceptiva orální kombinovaná MeSH
- levonorgestrel MeSH
- nandrolon MeSH