Synthesis, Characterization, Molecular Docking, and Biological Activities of Some Natural and Synthetic Urolithin Analogs
| Autor: | Mustafa Fethi Sahin, Hayrettin Ozan Gulcan, Mustafa Gazi, Tugba Ercetin, Mine Yarim Yüksel, Chiara Luise, Wolfgang Sippl, Bahareh Noshadi |
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| Rok vydání: | 2020 |
| Předmět: |
Antioxidant
DPPH medicine.medical_treatment Bioengineering 01 natural sciences Biochemistry Antioxidants Structure-Activity Relationship chemistry.chemical_compound Ellagitannin medicine Humans Benzopyrans Enzyme Inhibitors Molecular Biology Butyrylcholinesterase chemistry.chemical_classification 010405 organic chemistry General Chemistry General Medicine Hydrolyzable Tannins 0104 chemical sciences Urolithin Molecular Docking Simulation 010404 medicinal & biomolecular chemistry Enzyme chemistry Docking (molecular) Molecular Medicine Monoamine oxidase B |
| Zdroj: | Chemistry & Biodiversity. 17 |
| ISSN: | 1612-1880 1612-1872 |
| Popis: | Urolithins (that is, hydroxy substituted benzo[c]chromen-6-one derivatives) are formed within the gastrointestinal tract following to the exposure to various ellagitannin rich diet, particularly involving pomegranate, nuts, and berries. Regarding the bioavailability deficiency of ellagitannins, the biological activities obtained through the extracts of these dietaries are attributed to the urolithin compounds, since they are bioavailable. Particularly, there are studies indicating the importance of ellagitannin-rich food for protective and alternative treatment of Alzheimer's Disease (AD). From this perspective, within this study, the major urolithins (that is, urolithins A and B), their methyl ether metabolites, as well as some synthetic urolithin analogs have been synthesized and screened for their biological activities in various enzyme inhibition (acetylcholinesterase, butyrylcholinesterase, monoamine oxidase B, cyclooxygenase 1, and cyclooxygenase 2) and antioxidant (DPPH radical scavenging) assay systems. The results pointed out the potential of urolithins to act as inhibitors on these receptors. Docking studies were also performed to investigate the possible interactions. |
| Databáze: | OpenAIRE |
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