PDE-5 inhibitors in selected herbal supplements from the Ghanaian market for better erectile function as tested by a bioassay

Toxicol In Vitro. 2021 Jun:73:105130. doi: 10.1016/j.tiv.2021.105130. Epub 2021 Mar 1.

Abstract

Herbal supplements sold as 'all natural' on various markets in Accra (Ghana) and advertised as highly efficacious in treating erectile dysfunction (ED) were bought and analysed by a PDE-5 enzyme inhibition assay. The claimed efficacy of these products could be the result of inherent plant constituents, but also of intentionally added pharmaceuticals. Medically, ED is treated with potent inhibitors of the phosphodiesterase-5 (PDE-5) enzyme, as in the case of sildenafil. To test the efficacy of the Ghanaian supplements, extracts were made and tested using a PDE-Glo phosphodiesterase assay, a luminescent high-throughput screening (HTS) method. Results revealed that about 90% of the selected samples were able to inhibit PDE-5 activity to a high extent. Estimated concentrations in sildenafil equivalents ranged from traces to very high, with 25 samples (62.5%) pointing at daily doses higher than 25 mg sildenafil equivalents and 9 (22.5%) of these at doses higher than the maximal recommended daily intake of 100 mg sildenafil equivalents. Further investigations are needed to confirm if the observed effects are due to inherent plant constituents or merely the result of added synthetic PDE-5 enzyme inhibitors, especially because doses above 100 mg sildenafil equivalents per day may result in severe health risks.

Keywords: Herbal supplement; PDE-5 inhibitors; Phosphodiesterase assay; Screening.

MeSH terms

  • Biological Assay
  • Cyclic Nucleotide Phosphodiesterases, Type 5 / metabolism*
  • Dietary Supplements*
  • Erectile Dysfunction / drug therapy
  • Ghana
  • High-Throughput Screening Assays
  • Humans
  • Male
  • Phosphodiesterase 5 Inhibitors / pharmacology*
  • Plant Extracts / pharmacology*

Substances

  • Phosphodiesterase 5 Inhibitors
  • Plant Extracts
  • Cyclic Nucleotide Phosphodiesterases, Type 5