Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eastern Mediterranean University, via Mersin 10, TR-99628, Famagusta, North Cyprus, Turkey.
Institute of Pharmacy, Martin Luther University of Halle-Wittenberg, Kurt-Mothes-Str.3, DE-06120, Halle/Saale, Germany.
Chem Biodivers. 2020 Aug;17(8):e2000197. doi: 10.1002/cbdv.202000197. Epub 2020 Jul 20.
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.
尿石素（即羟基取代的苯并[c]色烯-6-酮衍生物）在胃肠道内形成，这是在暴露于各种富含鞣花单宁的饮食后发生的，特别是涉及石榴、坚果和浆果。鉴于鞣花单宁的生物利用度不足，通过这些饮食的提取物获得的生物活性归因于尿石素化合物，因为它们是可生物利用的。特别是，有研究表明富含鞣花单宁的食物对阿尔茨海默病（AD）的预防和替代治疗很重要。从这个角度来看，在这项研究中，主要的尿石素（即尿石素 A 和 B）、它们的甲基醚代谢物以及一些合成的尿石素类似物已被合成，并在各种酶抑制（乙酰胆碱酯酶、丁酰胆碱酯酶、单胺氧化酶 B、环加氧酶 1 和环加氧酶 2）和抗氧化（DPPH 自由基清除）测定系统中筛选其生物活性。结果表明尿石素有作为这些受体抑制剂的潜力。还进行了对接研究以研究可能的相互作用。
