title: Synthesis and neuroprotective effect of E-3,4-dihydroxy styryl aralkyl ketones derivatives against oxidative stress and inflammation.
abstract: E-3,4-Dihydroxy styryl aralkyl ketones as well as their 3,4-diacetylated derivatives as the analogues of neuroprotective agent CAPE were designed and synthesized for improving stability and lipid solubility. The neuroprotective activities of target compounds 10a-g and 11a-g were tested by three models in vitro, including 1,1-diphenyl-2-picrylhydrazyl radical scavenging capacity, neuronal protecting effect against damage induced by H2O2 in PC12 cells and nitric oxide suppression effect in BV2 microglial cells. The results demonstrated that compounds 10f and 11f exhibited the most potent neuroprotective effect against oxidative stress and inflammation, which is higher than that of the lead compound CAPE.
authors.affiliation: Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
authors.forename: Xianling
authors.initials: X
authors.lastname: Ning
authors.forename: Ying
authors.initials: Y
authors.lastname: Guo
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Ma
authors.forename: Renzong
authors.initials: R
authors.lastname: Zhu
authors.forename: Chao
authors.initials: C
authors.lastname: Tian
authors.forename: Xiaowei
authors.initials: X
authors.lastname: Wang
authors.forename: Zhizhong
authors.initials: Z
authors.lastname: Ma
authors.forename: Zhili
authors.initials: Z
authors.lastname: Zhang
authors.forename: Junyi
authors.initials: J
authors.lastname: Liu
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007249:Inflammation / Q000188:drug therapy*; D051379:Mice; D017628:Microglia / Q000166:cytology / Q000187:drug effects; D015394:Molecular Structure; D018696:Neuroprotective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D009569:Nitric Oxide / Q000037:antagonists & inhibitors; D018384:Oxidative Stress / Q000187:drug effects*; D016716:PC12 Cells; D051381:Rats; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D018696:Neuroprotective Agents; D013343:Styrenes; D009569:Nitric Oxide