Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 남상집 | * |
dc.date.accessioned | 2019-07-22T16:30:45Z | - |
dc.date.available | 2019-07-22T16:30:45Z | - |
dc.date.issued | 2019 | * |
dc.identifier.issn | 0141-8130 | * |
dc.identifier.issn | 1879-0003 | * |
dc.identifier.other | OAK-25089 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/250152 | - |
dc.description.abstract | Six synthetic (1-6) and six natural (7-12) chalcones were tested for human monoamine oxidases (hMAOs) and acetylcholinesterase (AChE) inhibitory activities. Compounds 4-dimethylaminochalcone (2), 4'-chloro-4-dimethylaminochalcone (5), and 2,4'-dichloro-4-dimethylaminochalcone (1) potently inhibited hMAO-B with IC50 values of 0.029, 0.061, and 0.075 mu M, respectively. 4-Nitrochalcone (4) and 4-chlorochalcone (3) also potently inhibited hMAO-B with IC50 values of 0.066 and 0.082 mu M, respectively (23- and 2.6-fold less than compound 2). Compound 2 had a high selectivity index (113.1) for hMAO-B over hMAO-A (IC50 = 3.28 mu M). Compounds 1 and 2,2'-dihydroxy-4',6'-dimethoxychalcone (12) potently inhibited hMAO-A with IC50 values of 0.18 and 039 mu M, respectively. In addition, compounds 4 and 2 also effectively inhibited AChE with IC50 values of 125 and 6.07 mu M, respectively, and thus, exhibited dual-targeting. Compound 2 reversibly and competitively inhibited hMAO-B with a K-i value of 0.0066 mu M. Docking simulations showed binding affinities of compounds 1 to 5 for hMAO-B were higher than those for hMAO-A or AChE and suggested these five chalcones form hydrogen bonds with MAO-B at Cys172 but that they do not form hydrogen bonds with hMAO-A or AChE. These findings suggest compound 2 be considered a promising and dual-targeting lead compound for the treatment of Alzheimer's disease. (C) 2019 Elsevier B.V. All rights reserved. | * |
dc.language | English | * |
dc.publisher | ELSEVIER | * |
dc.subject | 4-Dimethylaminochalcone | * |
dc.subject | Human monoamine oxidase | * |
dc.subject | Acetylcholinesterase | * |
dc.subject | Dual-targeting function | * |
dc.subject | Docking simulation | * |
dc.title | Potent and selective inhibition of human monoamine oxidase-B by 4-dimethylaminochalcone and selected chalcone derivatives | * |
dc.type | Article | * |
dc.relation.volume | 137 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 426 | * |
dc.relation.lastpage | 432 | * |
dc.relation.journaltitle | INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES | * |
dc.identifier.doi | 10.1016/j.ijbiomac.2019.06.167 | * |
dc.identifier.wosid | WOS:000484644100047 | * |
dc.identifier.scopusid | 2-s2.0-85068356120 | * |
dc.author.google | Oh, Jong Min | * |
dc.author.google | Kang, Myung-Gyun | * |
dc.author.google | Hong, Ahreum | * |
dc.author.google | Park, Ji-Eun | * |
dc.author.google | Kim, Soo Hyun | * |
dc.author.google | Lee, Jae Pil | * |
dc.author.google | Baek, Seung Cheol | * |
dc.author.google | Park, Daeui | * |
dc.author.google | Nam, Sang-Jip | * |
dc.author.google | Cho, Myoung-Lae | * |
dc.author.google | Kim, Hoon | * |
dc.contributor.scopusid | 남상집(57208839798) | * |
dc.date.modifydate | 20240220120010 | * |