Phosphodiesterase (PDE5) inhibition assay for rapid detection of erectile dysfunction drugs and analogs in sexual enhancement products

Drug Testing and Analysis
Michael F Santillo, Mapa S T Mapa

Abstract

Products marketed as dietary supplements for sexual enhancement are frequently adulterated with phosphodiesterase-5 (PDE5) inhibitors, which are erectile dysfunction drugs or their analogs that can cause adverse health effects. Due to widespread adulteration, a rapid screening assay was developed to detect PDE5 inhibitors in adulterated products. The assay employs fluorescence detection and is based on measuring inhibition of PDE5 activity, the pharmacological mechanism shared among the adulterants. Initially, the assay reaction scheme was established and characterized, followed by analysis of 9 representative PDE5 inhibitors (IC50 , 0.4-4.0 ng mL-1 ), demonstrating sensitive detection in matrix-free solutions. Next, dietary supplements serving as matrix blanks (n = 25) were analyzed to determine matrix interference and establish a threshold value; there were no false positives. Finally, matrix blanks were spiked with 9 individual PDE5 inhibitors, along with several mixtures. All 9 adulterants were successfully detected (≤ 5 % false negative rate; n = 20) at a concentration of 1.00 mg g-1 , which is over 5 times lower than concentrations commonly encountered in adulterated products. A major distinction of the PDE5 inhibition as...Continue Reading

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Citations

May 7, 2020·Analytical and Bioanalytical Chemistry·Michael F Santillo
Sep 5, 2018·International Journal of Molecular Sciences·Ashfaq AhmadJoseph K Ritter
Jan 24, 2021·Fundamental & Clinical Pharmacology·Mélissa Yéléhé-OkoumaJulien Scala-Bertola
Sep 3, 2019·Shokuhin eiseigaku zasshi. Journal of the Food Hygienic Society of Japan·Miho SakamotoKoichi Saito

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