Synthesis, Characterization, Molecular docking, and Biological Activities of Some Natural and Synthetic Urolithin Analogues.

Synthesis, Characterization, Molecular docking, and Biological Activities of Some Natural and Synthetic Urolithin Analogues. Chem Biodivers. 2020 Jun 04;: Authors: Gulcan HO, Noshadi B, Ercetin T, Luise C, Yuksel MY, Sippl W, Sahin MF, Gazi M Abstract Urolithins (i.e., hydroxyl 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 (i.e., Urolithin A and B), their methyl ether metabolites, as well as some synthetic urolithin analogues 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, for the first time, pointed out the possible mechanisms of the activities of the urolithins for the treatment of AD with the corresponding structure activity relationshi...
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research