Back to Search
Start Over
Identification of Descarbonsildenafil in an Adulterated Dietary Supplement and Evaluation of Its Inhibitory Activity for Phosphodiesterase Type 5 (PDE5)
- Source :
- Food Hygiene and Safety Science (Shokuhin Eiseigaku Zasshi). 61:34-40
- Publication Year :
- 2020
- Publisher :
- Japanese Society for Food Hygiene and Safety, 2020.
-
Abstract
- Some illegal dietary supplements contain phosphodiesterase type 5 (PDE5) inhibitors, such as sildenafil, for exerting "therapeutic" effects in erectile dysfunction. This is apparently dangerous, and thus, should be appropriately regulated. Identification of descarbonsildenafil was first reported in Singapore in a coffee sample labeled to exert male sexual performance enhancement effects. However, it is unclear whether the compound possesses PDE5 inhibitory activity. We encountered during our survey of dietary supplements, a sexual enhancement product commercially available in Tokyo, in which a peak presumed to be of descarbonsildenafil was detected by LC-UV and electrospray ionization-tandem MS (ESI-MS/MS). The compound was isolated and identified as descarbonsildenafil with liquid chromatography-quadrupole time-of-flight-mass spectrometry (LC-QTOF-MS), NMR, and X-ray crystal structural analysis. In addition, descarbonsildenafil showed PDE5 inhibitory activity in PDE5 inhibition assay, and its IC50 value for PDE5A1 was found to be 30 nmol/L. The results of INADEQUATE NMR and X-ray crystal structural analysis in this study provide information for the identification of descarbonsildenafil. Since this study indicates that this compound is a PDE5 inhibitor having adequate activity, it is regulated as a drug component in Japan.
- Subjects :
- Drug
Sildenafil
media_common.quotation_subject
Dietary supplement
Food Contamination
Pharmacology
010403 inorganic & nuclear chemistry
Inhibitory postsynaptic potential
01 natural sciences
Sildenafil Citrate
chemistry.chemical_compound
Tandem Mass Spectrometry
medicine
Tokyo
IC50
media_common
Cyclic Nucleotide Phosphodiesterases, Type 5
Chemistry
010401 analytical chemistry
General Medicine
Phosphodiesterase 5 Inhibitors
medicine.disease
0104 chemical sciences
Erectile dysfunction
cGMP-specific phosphodiesterase type 5
Dietary Supplements
Performance enhancement
Subjects
Details
- ISSN :
- 18821006 and 00156426
- Volume :
- 61
- Database :
- OpenAIRE
- Journal :
- Food Hygiene and Safety Science (Shokuhin Eiseigaku Zasshi)
- Accession number :
- edsair.doi.dedup.....086b8d332daab8bd77a9d3cc07126697