AI Article Synopsis
- Hydroxylated 6H-benzo[c]chromen-6-one derivatives (urolithins) are metabolites from ellagitannins found in certain foods and have been linked to cognitive enhancement in Alzheimer's treatment, despite their weak ability to inhibit key enzymes related to the disease.
- A new series of chemical derivatives was specifically created and evaluated for their ability to inhibit acetylcholinesterase and butyrylcholinesterase enzymes, which are important targets in Alzheimer's therapy.
- The synthesized compounds showed biological activity similar to that of established Alzheimer's medications, such as rivastigmine, galantamine, and donepezil, both in laboratory and animal studies.
Article Abstract
Hydroxylated 6H-benzo[c]chromen-6-one derivatives (i.e., urolithins) are the main bioavailable metabolites, and biomarkers of ellagitannins present in various nutrition. Although these dietaries, the sources of urolithins, are employed in folk medicine as cognitive enhancer in the treatment of Alzheimer's Disease, urolithins have negligible potential to inhibit acetylcholinesterase and butyrylcholinesterase enzymes, the validated targets of Alzheimer's Disease. Therefore, within this research, a series of 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives has been designed, synthesized, and their biological activities were evaluated as potential acetylcholinesterase and butyrylcholinesterase inhibitors. The compounds synthesized exerted comparable activity in comparison to rivastigmine, galantamine, and donepezil both in in vitro and in vivo studies.
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| http://dx.doi.org/10.1016/j.bmc.2014.08.016 | DOI Listing |
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