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Synthesis,Characterization, Molecular Docking,and Biological Activities of Some Natural and Synthetic Urolithin Analogs
Authors:Bahareh Noshadi  Tugba Ercetin  Chiara Luise  Mine Yarim Yuksel  Wolfgang Sippl  Mustafa Fethi Sahin  Mustafa Gazi  Hayrettin Ozan Gulcan
Abstract:Urolithins (that is, hydroxy substituted benzoc]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.
Keywords:urolithins  cholinesterases  monoamine oxidase B  cyclooxygenases  antioxidants  enzymes
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