Boldenone undecylenate

Comprehensive steroid profiling by liquid chromatography coupled to high resolution mass spectrometry.[Pubmed:30196848]

J Steroid Biochem Mol Biol. 2018 Oct;183:106-115.

A steroidomics workflow has been developed in the objective of monitoring a wide range (n >150) of steroids in urine. The proposed workflow relies on the optimization of an adequate SPE extraction step followed by an UHPLC-HRMS/MS simultaneous analysis of both free and conjugated forms of C18, C19 and C21 steroid hormones. On the basis of 44 selected steroids, representative of main classes of steroids constituting the steroidome, the performances of the developed workflow were evaluated in terms of selectivity, repeatability (< 13%) and linearity (R2> 0.985 in the concentration range [0.01-10ng/mL]). As metabolites identification and characterization constitute the bottleneck of such profiling approaches, a homemade database was created encompassing a large number of characterized free and conjugated steroids (n> 150) for putative steroid-like biomarkers identification purposes. The efficiency of the workflow in highlighting fine modifications within the urinary steroidome was assessed in the frame of an anabolic treatment involving an intra-muscular administration of Boldenone undecylenate (2 mg/kg) to veals (n=6) and the investigation of potential steroid biomarkers. Besides monitoring known phase II metabolites of boldenone in the bovine specie, namely, boldenone glucuronide and sulfate, the applied strategy also permitted to observe, upon boldenone administration, a modified profile of epiboldenone glucuronide. Furthermore, 31 signals corresponding to non-identified steroid species could also be highlighted as impacted upon the exogenous steroid treatment. This study is the first to simultaneously investigate both free and conjugated C18, C19 and C21 steroid hormones in their native form using UHPLC-HRMS/MS and allowing their comprehensive profiling. This strategy was probed in-vivo.

Grape Seed Proanthocyanidin Ameliorates Cardiac Toxicity Induced by Boldenone Undecylenate through Inhibition of NADPH Oxidase and Reduction in the Expression of NOX2 and NOX4.[Pubmed:30116498]

Oxid Med Cell Longev. 2018 Jul 5;2018:9434385.

The effect of anabolic androgenic steroids on the cardiovascular system is poorly understood. Increased production of free radicals is coupled to the pathophysiology of many alterations within the circulatory system. The only function of the enzyme family NADPH oxidases (NOXs) is the generation of reactive oxygen species (ROS). Therefore, this study investigated the beneficial role of grape seed proanthocyanidin extract (GSPE) in ameliorating cardiac toxicity induced by the anabolic steroid Boldenone in male rats through NOX inhibition and reduction in the expression of NOX2 and NOX4. This study was conducted on forty male rats which are divided into four groups (normal control, positive control or GSPE, Boldenone, and posttreatment Boldenone with GSPE). A significant increase in relative body weight, relative heart weight, and hemodynamic parameters, as well as serum concentrations of lactate dehydrogenase, creatine kinase, creatine kinase-muscle brain, myoglobin, cholesterol, low-density lipoprotein cholesterol, risk factor 1/2, K(+), and Cl(-), in treated rats with Boldenone when compared with control. We also noted a significant increase in the levels of cardiac malondialdehyde, H2O2 generation in heart tissues, mRNA expression of NOX2 and NOX4, and immunoreactivity to proliferating cell nuclear antigen (PCNA). Posttreated rats with Boldenone and GSPE ameliorated cardiac toxicity via inhibition of NOX and a reduction in alteration of the expression of NOX2, NOX4, and PCNA induced by Boldenone. These novel insights into the antioxidative activity of GSPE should serve as a basis for the development of improved chemopreventive or therapeutic strategies for cardiac toxicity.

Unsuspected Clenbuterol Toxicity in a Patient Using Intramuscular Testosterone.[Pubmed:29849287]

Clin Pract Cases Emerg Med. 2017 May 23;1(3):197-200.

Clenbuterol is a beta-agonist that has been abused by fitness-oriented individuals for muscle growth and weight loss. We report a case of a 46-year-old man who presented tachycardic, hypokalemic, and hyperglycemic after injecting testosterone obtained from Brazil. He developed refractory hypotension and was started on an esmolol infusion for suspected beta-agonist toxicity. Laboratory analysis showed a detectable clenbuterol serum concentration. Analysis of an unopened ampule contained Boldenone undecylenate, clenbuterol, and vitamin E. This case illustrates a novel exposure that caused beta-agonist toxicity and was treated successfully with rapid-onset beta blocker.

Detection of prohibited substances in equine hair by ultra-high performance liquid chromatography-triple quadrupole mass spectrometry - application to doping control samples.[Pubmed:29430877]

Drug Test Anal. 2018 Feb 12.

The detection of drugs in human hair samples has been performed by laboratories around the world for many years and the matrix is popular in disciplines, such as workplace drug testing. To date, however, hair has not become a routinely utilised matrix in sports drug detection. The analysis of hair samples offers several potential advantages to doping control laboratories, not least of which are the greatly extended detection window and the ease of sample collection and storage. This article describes the development, validation, and utilisation of a sensitive ultra-high performance liquid chromatography-triple quadrupole mass spectrometry (UHPLC-MS/MS) method for the detection of 50 compounds. This provides significantly improved coverage for those analytes which would be of particular interest if detected in hair, such as anabolic steroid esters and selective androgen receptor modulators (SARMs). Qualitative validation of the method resulted in estimated limits of detection as low as 0.1 pg/mg for the majority of compounds, with all being detected at 2 pg/mg or below. The suitability of the method for the detection of prohibited substances in incurred material was demonstrated by the successful detection of several compounds, such as stanozolol, Boldenone undecylenate, clenbuterol, and GW-501516, in genuine equine hair samples. Estimated concentrations of the detected substances ranged from 0.27 to 8.6 pg/mg. The method has been shown to be fit-for-purpose for routine screening of equine hair samples by the analysis of over 400 genuine hair samples.

Evaluation of anabolic steroid induced renal damage with sonography in bodybuilders.[Pubmed:29148625]

J Sports Med Phys Fitness. 2018 Nov;58(11):1681-1687.

BACKGROUND: The aim of this study was to investigate the effect of anabolic steroids on kidneys in bodybuilders. METHODS: Twenty-two bodybuilders were included in the study. Participants were divided into three groups according to the scheme of steroid usage: group 1 (N.=8, intramuscular 500 mg testosterone enanthate, intramuscular 400 mg nandrolone decanoate and oral 40 mg methandrostenolone for 12 weeks), group 2 (N.=7, intramuscular 500 mg testosterone enanthate, intramuscular 300 mg nandrolone decanoate and intramuscular 300 mg Boldenone undecylenate for 16 weeks), and group 3 (N.=7, no steroid intake). Blood urea nitrogen (BUN), creatinine (Cr), urine micro-albumin and electrolyte levels were measured. Renal volume, cortical thickness and echogenicity were obtained in ultrasonographic scans. RESULTS: Renal volume, cortical thickness, echogenicity and protein intake value were significantly higher in group 2 than group 1 and 3. Plasma levels of BUN and Cr in group 2 were significantly higher than other groups (P<0.001). Urine microalbumin and electrolyte levels were normal in all groups. CONCLUSIONS: The results of this study indicate that high protein intake, steroid usage, particularly the schemes, including Boldenone undecylenate increases cortical echogenicity, thickness of renal parenchyma and renal volume in bodybuilders.

Biochemical and oxidative stress markers in the liver and kidneys of rats submitted to different protocols of anabolic steroids.[Pubmed:27896593]

Mol Cell Biochem. 2017 Jan;425(1-2):181-189.

The objective of this study was to evaluate the effects of different protocols (P1, P2, and P3) of Boldenone undecylenate (BU) and stanozolol (ST) on markers of liver and kidney function and variables of oxidative stress in these organs. For this, 54 male Wistar rats were divided into nine groups of six animals each. Each animal received intramuscularly 5.0 mg kg(-1) of BU or ST once a week for 4 weeks (P1); 2.5 mg kg(-1) of BU or ST once a week for 8 weeks (P2); and 1.25 mg kg(-1) of BU or ST once a week for 12 weeks (P3). For each protocol, a control group was used, and they received 0.1 ml of olive oil intramuscularly. Blood and fragments of liver and kidney were collected for alanine aminotransferase activity (ALT), alkaline phosphatase, albumin, creatinine, cholesterol, total protein, triglycerides, urea, reactive oxygen species, thiobarbituric acid reactive substances, total thiols, and glutathione evaluation. The results show that the BU in doses of 5 (day 30) and 2.5 mg kg(-1) (day 60) changes the ALT seric activity, possibly showing a hepatotoxic effect. High doses of BU may lead to increased levels of cholesterol (protocol P1) possibly due to inhibition of the normal steroid biosynthesis process. All protocols used caused changes in the redox balance of the organs studied (except in the liver, protocol P2), which indicates that these drugs might be harmful even at low doses.

Effects of boldenone undecylenate on growth performance, maintenance behaviour, reproductive hormones and carcass traits of growing rabbits.[Pubmed:27487497]

Pol J Vet Sci. 2016;19(2):245-51.

The present study was done to evaluate the effect of Boldenone undecylenate (BOL) on growth performance, maintenance behaviour, reproductive hormones and carcass traits of male rabbits. Sixty apparently healthy New Zealand White male rabbits, 5 weeks of age, were allotted to 3 equal groups. Each group was subdivided into 5 replicates, where the first group is control. The second group (B1) comprised rabbits that received 2 intramuscular injections of BOL (5 mg/kg) with 3 week intervals (9 and 12 weeks of age), while the third group (B2) included rabbits that received 3 intramuscular injections of BOL (5 mg/kg) with 2 week intervals (8, 10 and 12 weeks of age). The end of the trial was after 4 weeks from the last injection (16 weeks of age). The results revealed that the treated groups had a significant increase in total body weight, daily gain and feed efficiency, with a significant decrease in feed conversion ratio (FCR). Ingestive, locomotion and grooming behaviors were significantly higher in treated groups. Lateral pasture and exploratory behaviors were significantly higher in the control group. Administration of BOL resulted in a significant increase in dressing % and a significant decrease in testes %. Groups treated with BOL had a significantly (P<0.05) decreased serum testosterone level, simultaneously with a significantly increased estradiol level. The results indicate that BOL improves performance and carcass traits. Furthermore, there are hormonal-behavioral correlations through enhancement of ingestive and locomotion behaviors of treated animals.

Generation of phase II in vitro metabolites using homogenized horse liver.[Pubmed:26352508]

Drug Test Anal. 2016 Feb;8(2):241-7.

The successful use of homogenized horse liver for the generation of phase I in vitro metabolites has been previously reported by the authors' laboratory. Prior to the use of homogenized liver, the authors' laboratory had been using mainly horse liver microsomes for carrying out equine in vitro metabolism studies. Homogenized horse liver has shown significant advantages over liver microsomes for in vitro metabolism studies as the procedures are much quicker and have higher capability for generating more in vitro metabolites. In this study, the use of homogenized liver has been extended to the generation of phase II in vitro metabolites (glucuronide and/or sulfate conjugates) using 17beta-estradiol, morphine, and Boldenone undecylenate as model substrates. It was observed that phase II metabolites could also be generated even without the addition of cofactors. To the authors' knowledge, this is the first report of the successful use of homogenized horse liver for the generation of phase II metabolites. It also demonstrates the ease with which both phase I and phase II metabolites can now be generated in vitro simply by using homogenized liver without the need for ultracentrifuges or tedious preparation steps.

Boldenone Undecylenate (Ba 29038) is a synthetic steroid which has a similar effect as the natural steroid testosterone; it is frequently used in veterinary medicine, though it is also used in humans.

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