Some phosphodiesterase type-5 (PDE5) inhibitors are active ingredients of prescription drugs that are widely used in the treatment of erectile dysfunction (ED). Recently, a large number of substances with this activity have been developed. Illegal addition of PDE5 inhibitors to foods could lead to cardiovascular diseases and even death, which poses a serious threat to food safety, therefore an on-site rapid screening method is urgently needed. Herein, a host functionalized bimetallic nanoclusters, CD/Au Ag NCs, were synthesized through self-assembly of 6-Aza-2-thiothymine gold nanoclusters (ATT-Au NCs), Arginine silver nanoclusters (Arg-Ag NCs) and carboxymethyl β-cyclodextrin (β-CMCD). The introduction of Rhodamine 6G (R6G) could quench the fluorescence of CD/Au Ag NCs based on the inner filter effect (IFE) and fluorescence resonance energy transfer effect (FRET). Importantly, it was discovered that several PDE5 inhibitors exhibited a higher binding affinity to β-CMCD and could displace R6G binding with CD cavity, which disrupted the fluorescence quenching effects and resulted in the fluorescence recovery of CD/Au Ag NCs. This fluorescence turn-on signal could be utilized for the detection of PDE5 inhibitors. At present, emerging PDE5 inhibitor analogues pose a great challenge to food safety due to their unknown efficacy and safety. The proposed method holds the advantages of high sensitivity, simple probe synthesis, easy operation, and simultaneous detection of multiple PDE5 inhibitors. Meanwhile, the successful application in functional food sample demonstrated its high application potential in multiple PDE5 inhibitors screening.
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http://dx.doi.org/10.1016/j.aca.2023.341883 | DOI Listing |
AAPS PharmSciTech
January 2025
Department of Dermatology, Venereology and Andrology, Faculty of Medicine, Assiut University, Assiut, Egypt.
The present work focuses on the production of sildenafil co-evaporates loaded emulgels as topical dosage forms for the treatment of premature ejaculation and erectile dysfunction. Topical administration of sildenafil citrate (SILD) co-evaporates is expected to improve the bioavailability profile of the drug and to avoid the severe side effects accompanying the traditional SILD dosage forms, especially for prohibited cardiovascular cases. Firstly, the solubility of SILD was improved via solid dispersion via co-evaporation technique using PEG-5KDa and PVP-K90 as hydrophilic carriers.
View Article and Find Full Text PDFNat Chem
January 2025
Physical and Theoretical Chemistry Laboratory, Department of Chemistry, University of Oxford, Oxford, UK.
Understanding the dynamics of membrane protein-ligand interactions within a native lipid bilayer is a major goal for drug discovery. Typically, cell-based assays are used, however, they are often blind to the effects of protein modifications. In this study, using the archetypal G protein-coupled receptor rhodopsin, we found that the receptor and its effectors can be released directly from retina rod disc membranes using infrared irradiation in a mass spectrometer.
View Article and Find Full Text PDFFood Addit Contam Part A Chem Anal Control Expo Risk Assess
January 2025
Shanxi Key Laboratory of Food and Drug Safety Prevention and Control, Inspection and Testing Center of Shanxi Province, Taiyuan, Shanxi, China.
Two novel phosphodiesterase 5 (PDE-5) inhibitors were detected in pressed candy using high-performance liquid chromatography (HPLC)-diode array detection. Following extraction with acetonitrile and sonication, the compounds were isolated and purified semi-preparative liquid chromatography. Structural characterisation was achieved through high-resolution mass spectrometry (HRMS) and nuclear magnetic resonance (NMR) spectroscopy.
View Article and Find Full Text PDFJ Comput Chem
January 2025
Centre for Inflammation, Centenary Institute and University of Technology Sydney, Faculty of Science, School of Life Sciences, Sydney, New South Wales, Australia.
Phosphodiesterase 5 (PDE5) inhibitors have shown great potential in treating Alzheimer's disease by improving memory and cognitive function. In this study, we evaluated fluspirilene, a drug commonly used to treat schizophrenia, as a potential PDE5 inhibitor using computational methods. Molecular docking revealed that fluspirilene binds strongly to PDE5, supported by hydrophobic and aromatic interactions.
View Article and Find Full Text PDFChest
January 2025
Pulmonary Division, Lady Davis Carmel Medical Center, Faculty of Medicine Technion Institute of Technology, Haifa, Israel.
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