The Biological Actions of Dehydroepiandrosterone Involve Multiple Receptors

    January 2006 in “ Drug Metabolism Reviews ”
    Stephanie J. Webb, Thomas Geoghegan, Russell A. Prough, Kristy K. Michael Miller
    TLDR DHEA affects multiple receptors and may help with metabolic issues, but its safety and effectiveness in humans are unclear.
    The document reviewed the biological actions of dehydroepiandrosterone (DHEA), highlighting its interaction with multiple receptors, including PPARα, PXR, and estrogen receptors. DHEA demonstrated various effects in rodent models, such as reducing body fat and modulating diabetes, atherosclerosis, and obesity. Despite its availability as a dietary supplement, there was limited evidence supporting its efficacy and safety in humans. The study found that DHEA activated PXR and estrogen receptors, with a higher affinity for ERβ, and influenced PPARα phosphorylation, affecting transcriptional activity. DHEA also modulated glucocorticoid metabolism and the IGFBP-1 axis, suggesting potential benefits for metabolic syndrome and atherosclerosis. However, concerns about its carcinogenic potential and conversion to sex steroids were noted, emphasizing the need for further research on its mechanisms and safety.
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