Synthesis, Characterization, Molecular docking, and Biological Activities of Some Natural and Synthetic Urolithin Analogues,Chemistry & Biodiversity

当前位置： X-MOL 学术 › Chem. Biodivers. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Synthesis, Characterization, Molecular docking, and Biological Activities of Some Natural and Synthetic Urolithin Analogues
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2020-07-20 , DOI: 10.1002/cbdv.202000197
Bahareh Noshadi _{1,

1} , Tugba Ercetin ₁ , Chiara Luise ₂ , Mine Yarim Yuksel ₃ , Wolfgang Sippl ₂ , Mustafa Fethi Sahin ₁ , Mustafa Gazi ₁ , Hayrettin Ozan Gulcan ₁

Affiliation

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 relationships. Docking studies were also performed to investigate the possible interactions with the corresponding receptors.

中文翻译：

一些天然和合成尿石素类似物的合成、表征、分子对接和生物活性

尿石素（即羟基取代的苯并[c]色烯-6-酮衍生物）是在接触各种富含鞣花单宁的饮食后在胃肠道内形成的，特别是涉及石榴、坚果和浆果。关于鞣花单宁的生物利用度不足，通过这些膳食提取物获得的生物活性归因于尿石素化合物，因为它们是生物可利用的。特别是，有研究表明富含鞣花单宁的食物对于阿尔茨海默病 (AD) 的保护性和替代性治疗的重要性。从这个角度来看，在本研究中，主要的尿石素（即尿石素 A 和 B）、它们的甲醚代谢物、以及一些合成的尿石素类似物已经合成并筛选了它们在各种酶抑制（乙酰胆碱酯酶、丁酰胆碱酯酶、单胺氧化酶 B、环氧合酶 1 和环氧合酶 2）和抗氧化剂（DPPH 自由基清除）测定系统中的生物活性。该结果首次指出了尿石素治疗AD的活性与相应的构效关系的可能机制。还进行了对接研究以研究与相应受体的可能相互作用。指出了尿石素活性治疗AD的可能机制及其相应的构效关系。还进行了对接研究以研究与相应受体的可能相互作用。指出了尿石素活性治疗AD的可能机制及其相应的构效关系。还进行了对接研究以研究与相应受体的可能相互作用。

更新日期：2020-07-20

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11