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Characterization of Resveratrol, Oxyresveratrol, Piceatannol and Roflumilast as Modulators of Phosphodiesterase Activity. Study of Yeast Lifespan
- Source :
- Pharmaceuticals, Volume 13, Issue 9, Pharmaceuticals, Vol 13, Iss 225, p 225 (2020)
- Publication Year :
- 2020
- Publisher :
- Multidisciplinary Digital Publishing Institute, 2020.
-
Abstract
- Our desire to live longer has led to an ever-increasing number of novel antiaging products. However, few molecules have any real effect and new ones need to be studied before they can be used commercially. In this contribution, activation of the caloric restriction (CR) pathway was studied using different three (resveratrol, oxyresveratrol and piceatannol)&mdash<br />a family with demonstrated bioactivity on phosphodiesterase activity. The high-affinity phosphodiesterase type 2 (PDE2) of Saccharomyces cerevisiae was expressed in Escherichia coli, purified and characterized. The activity and the inhibitory activity of each stilbene was studied, and the findings were compared in vitro and in silico with those obtained with roflumilast&mdash<br />a human PDE4 inhibitor widely used in chronic obstructive pulmonary diseases. Finally, an in vivo chronological lifespan assay using WT S. cerevisiae and &Delta<br />PDE2 S. cerevisiae strains was carried out. It was demonstrated that stilbenes can modulate yPDE2 activity, increasing the lifespan of the yeast by 18% over a control (in combination with other pathways). In addition, roflumilast increased the lifespan in the WT strain. The findings as a whole would increase the range of lifespan products available and suggest novel uses for approved drugs.
- Subjects :
- Saccharomyces cerevisiae
roflumilast
Pharmaceutical Science
lcsh:Medicine
lcsh:RS1-441
Resveratrol
stilbenes
resveratrol
Article
lcsh:Pharmacy and materia medica
chemistry.chemical_compound
In vivo
Drug Discovery
Lifespan
Phosphodiesterase
Roflumilast
Stilbenes
medicine
Piceatannol
biology
lcsh:R
biology.organism_classification
In vitro
Oxyresveratrol
chemistry
Biochemistry
Molecular Medicine
phosphodiesterase
lifespan
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 14248247
- Database :
- OpenAIRE
- Journal :
- Pharmaceuticals
- Accession number :
- edsair.doi.dedup.....841efd0277a0e6ba5230d32a59eae775
- Full Text :
- https://doi.org/10.3390/ph13090225