Abstract:
:Several phenylethanoid glycoside derivatives were designed and synthesized. Most of the synthetic compounds showed significant neuroprotective effects, including antioxidative and anti-apoptotic properties. Specifically, target compounds displayed potent effects against various toxicities such as H2O2 and 6-hydroxydopamine (6-OHDA) in PC12 cells. Among the synthetic derivatives, three compounds (5, 6, 8) exhibited much superior activities to the marketed drug Edaravone. The compounds were able to prevent the 6-OHDA-induced damage in PC12 cells in a dose-dependent manner. The anti-apoptotic effects could be observed via cell morphological changes. Moreover, the compounds significantly reduced the intracellular ROS increase resulting from 6-OHDA treatment. The preliminary structure-activity relationships were also explored. Compounds 5, 6, 8 may hold the potential as promising neuroprotective agents and new lead compounds for the treatment of neurodegenerative diseases or cerebral ischemia.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Liu YG,Li X,Xiong DC,Yu B,Pu X,Ye XSdoi
10.1016/j.ejmech.2015.03.038subject
Has Abstractpub_date
2015-05-05 00:00:00pages
313-23eissn
0223-5234issn
1768-3254pii
S0223-5234(15)00205-6journal_volume
95pub_type
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