Profiling of anabolic androgenic steroids and selective androgen receptor modulators for interference with adrenal steroidogenesis

Patt, Melanie; Beck, Katharina R.; Marco, Tobias Di; Jäger, Marie-Christin; González‐Ruiz, Víctor; Bernard, Julien; Rudaz, Serge; Hartmann, Rolf W.; Salah, Mohamed; Koppen, Chris J. van; Grill, Matthias; Odermatt, Alex

doi:10.1016/j.bcp.2019.113781

Cited by 17 publications

(19 citation statements)

References 61 publications

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“…LGD4. 36 For both SARMS, no significant effect on the concentrations of the steroidogenesis assay was found, which was in line with our findings taking into account that here only a concentration of 1 μM was investigated, whereas the effects noted for LGD4 were mainly found at higher concentration levels.…”

Section: Selective Ar Modulatorssupporting

confidence: 91%

“…A larger subset of AASs has recently been investigated using the steroidogenesis assay by another group corroborating the diverse findings within the same class of substances 36 . For two compounds, a direct comparison of the results was possible, albeit that this study only tested on one concentration level (1 μM) against a negative control.…”

Section: Resultsmentioning

confidence: 72%

“…Results were normalized to the dimethyl sulfoxide (DMSO) vehicle control A larger subset of AASs has recently been investigated using the steroidogenesis assay by another group corroborating the diverse findings within the same class of substances. 36 For two compounds, a direct comparison of the results was possible, albeit that this study only tested on one concentration level (1 μM) against a negative control. Nevertheless, STAN also showed a significant upregulation of PROG and 17OH-PROG together with a downregulation of ADION.…”

Section: Anabolic-androgenic Steroidsmentioning

confidence: 99%

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An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile

Piper

Heimbach

Adamczewski

et al. 2020

Drug Testing and Analysis

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The steroid profile, that is, the urinary concentrations and concentration ratios of selected steroids, is used in sports drug testing to detect the misuse of endogenous steroids such as testosterone. Since several years, not only population-based thresholds are applied but also the steroid profile is monitored via the Athlete Biological Passport whereby the individual reference ranges derived from multiple test results of the same athlete are compared to population-based thresholds. In order to maintain a high probative force of the passport, samples collected or analyzed under suboptimal conditions should not be included in the longitudinal review. This applies to biologically affected or degraded samples and to samples excluded owing to the presence of other substances potentially (or evidently) altering the steroid profile. Nineteen different doping agents comprising anabolic steroids, selective androgen receptor modulators, selective estrogen receptor modulators, ibutamoren, and tibolone were investigated for their effect on the steroid profile using an androgen receptor activation test, an androgen receptor binding assay, an aromatase assay, and a steroidogenesis assay. The in vitro tests were coupled with well-established liquid chromatography/mass spectrometry-based analytical approaches and for a subset of steroidal analytes by gas chromatography/mass spectrometry. The variety of tests employed should produce a comprehensive data set to better understand how a compound under investigation may impact the steroid profile. Although our data set may allow an estimate of whether or not a substance will have an impact on the overall steroid metabolism, predicting which parameter in particular may be influenced remains difficult.

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Section: Selective Ar Modulatorssupporting

confidence: 91%

Section: Resultsmentioning

confidence: 72%

Section: Anabolic-androgenic Steroidsmentioning

confidence: 99%

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An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile

Piper

Heimbach

Adamczewski

et al. 2020

Drug Testing and Analysis

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“…This study observe hperactivity of HPA axis due to a decrease in serum cortisone levels after AAS administration, which causes the detection of ROS production and an increase in AASinduced mineralocorticoid steroidogenesis (29). All this explains the increased regulation of the Nrf2 gene.…”

Section: Vol 13mentioning

confidence: 57%

“…In addition, there is a decrease in the synthesis of cortisone. Patt et al (2020) show that the effect of testosterone on bovine adrenal cells, stimulating receptor of angiotensin, as well as aldosterone synthesis in vivo and inhibition of adrenal corticosteroid synthesis (29), as suggested for AAS, should lead to negative feedback mediated by the HPA axis activation, ultimately leads to adrenal hyperplasia. This explains the increased mRNA levels of TSPO levels due to increased mineralocorticoid synthesis.…”

Section: Vol 13mentioning

confidence: 96%

Selenium Enriched Yeast Modifies the Effects of Methandienone in Male Rabbits on the HPA Axis and Adrenal Gland Oxidative Stress

Abed¹,

Al-Azawi²

2020

AJVS

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The aim of this study was to investigate the changes caused by anabolic androgenic steroids (methandienone) in the hypothalamic adrenal axis (HPA) and oxidative status in adrenal glands and a protective role role by using organic selenium (high-selenium yeast) in adult male rabbits which treated with Methandienone in combination with selenium. A total of 20 intact male rabbits were divided into four equal groups (n = 5 for each group):a control group receiving distilled water, the AAS group (T1) receiving Methandienone (oral dose of 0.35 mg / kg.B.W.),the selenium group (T2) receiving high-selenium yeast (3 μg/ kg B.W orally)and the combination group (T3) getting both methandienone and selenium. The dosing every day for 60 days. . The hormones β-endorphin, ACTH and cortisone were measured in serum during two periods, 30 and 60 days of the experiment and the expression levels of Nuclear factor erythroid-2 and related factor-2 (Nrf2) and Translocater protein (TSPO) genes were measured in adrenal gland. a significant increase in beta-endorphin and ACTH and a decrease in cortisone were found in both 30 and 60 day periods in the AAS group (T1) compared with another groups (control, T2 and T3). On the other hand, T3 group shows a decrease in serum β-Endorphin and ACTH and no significant changes in cortisone in both periods .These changes were a compared with to AAS group. Moreover, there is a significant increased in revers transcription (mRNA) of Nrf2 factor and TSPO genes in AAS group(T1) as compared with other groups (T2 and T3). In addition, we observed a significant decrease in levels of Nrf2 and TSPO mRNA in the selenium-yeast group compared to the AAS group (T1). In conclusion, these results showed that organic selenium (high selenium yeast) has a positive effect (protective role) against oxidative damage to the adrenal gland caused by AAS with no effect on the adrenal steroidogenesis, which are affected by AAS.

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Dried bear bile exerts its antidepressant effect by modulating adrenal FXR to reduce peripheral glucocorticoid levels

Tao,

Li,

Yuan

et al. 2024

Brain, Behavior, & Immunity - Health

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Profiling of anabolic androgenic steroids and selective androgen receptor modulators for interference with adrenal steroidogenesis

Cited by 17 publications

References 61 publications

An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile

An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile

Selenium Enriched Yeast Modifies the Effects of Methandienone in Male Rabbits on the HPA Axis and Adrenal Gland Oxidative Stress

Dried bear bile exerts its antidepressant effect by modulating adrenal FXR to reduce peripheral glucocorticoid levels

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