Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2013 Feb 6;13(2):2148-63.
doi: 10.3390/s130202148.

In vitro androgen bioassays as a detection method for designer androgens

Elliot R Cooper  1 , Kristine C Y McGrath, Alison K Heather
Affiliations
Review

In vitro androgen bioassays as a detection method for designer androgens

Elliot R Cooper et al. Sensors (Basel). .

Abstract

Androgens are the class of sex steroids responsible for male sexual characteristics, including increased muscle mass and decreased fat mass. Illicit use of androgen doping can be an attractive option for those looking to enhance sporting performance and/or physical appearance. The use of in vitro bioassays to detect androgens, especially designer or proandrogens, is becoming increasingly important in combating androgen doping associated with nutritional supplements. The nutritional sports supplement market has grown rapidly throughout the past decade. Many of these supplements contain androgens, designer androgens or proandrogens. Many designer or proandrogens cannot be detected by the standard highly-sensitive screening methods such as gas chromatography-mass spectrometry because their chemical structure is unknown. However, in vitro androgen bioassays can detect designer and proandrogens as these assays are not reliant on knowing the chemical structure but instead are based on androgen receptor activation. For these reasons, it may be advantageous to use routine androgen bioassay screening of nutraceutical samples to help curb the increasing problem of androgen doping.

PubMed Disclaimer

Figures

Figure 1.
Figure 1.
The androgen response in cells. Androgens diffuse through the plasma membrane into the cytosol where they bind to the androgen receptor (AR). The androgen receptor is held in the cytosol by heat shock proteins (HSP) and other cofactors. The binding of androgens to the androgen receptor induces a conformational change in the receptor that frees it from the inhibitory factors and exposes a nuclear localization signal. The androgen/AR complex translocates to the nucleus where the receptor dimerizes and binds to the androgen response elements (ARE) located in the regulatory regions of target genes. Once bound to the DNA, AR enhances gene transcription by RNA polymerase.
Figure 2.
Figure 2.
Yeast and mammalian cell-based androgen bioassays. Both bioassays are based on the transfection of two plasmid vectors. One plasmid vector is an androgen receptor (AR) expression vector that allows high level constitutive expression of AR within cells that contain no (yeast) or low level (mammalian) of endogenous AR. The second plasmid vector is an androgen response element (ARE) driven reporter gene vector. For yeast cells, the most efficient reporter gene, to date, is β-galactosidase. For mammalian cells, a number of reporter genes are used, with secreted alkaline phosphatase (SEAP) a favored choice because of its ease of detection. Yeast cells do not express androgen metabolizing enzymes. Mammalian cells such as human hepatocytes express a number of different metabolizing enzymes including aromatase, 5α-reductase and hydroxysteroid reductases (HSD).
See this image and copyright information in PMC

Similar articles

See all similar articles

Cited by

References

    1. Barroso O., Mazzoni I., Rabin O. Hormone abuse in sports: The antidoping perspective. Asian J. Androl. 2008;10:391–402. - PubMed
    1. Palacios S. Androgens and female sexual function. Maturitas. 2007;57:61–65. - PubMed
    1. Yesalis C.E. Anabolic Steroids in Sport and Exercise. 2nd ed. Human Kinetics Publishers; Champaign, IL, USA: 2000.
    1. Hartgens F., Kuipers H. Effects of androgenic-anabolic steroids in athletes. Sports Med. 2004;34:513–554. - PubMed
    1. Mauras N., Hayes V., Welch S., Rina A., Helgeson K., Dokler M., Veldhuis J.D., Urban R.J. Testosterone deficiency in young men: Marked alterations in whole body protein kinetics, strength, and adiposity. J. Endocrinol. Metab. 1998;83:1886–1892. - PubMed