• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Identification and optimization of piperine analogues as neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/keap1 pathway
【24h】

Identification and optimization of piperine analogues as neuroprotective agents for the treatment of Parkinson's disease via the activation of Nrf2/keap1 pathway

机译：哌啶类似物作为神经保护剂通过NRF2 / Keap1途径治疗帕金森病的探测和优化

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Parkinson's disease (PD) is a slowly progressive and complex neurodegenerative disorder. Up to date, there are no approved drugs that could slow or reverse the neurodegenerative process of PD. Here, we reported the synthesis of series of piperine analogues and the evaluation of their neuroprotective effects against hydrogen peroxide (H2O2) induced damage in the neuron-like PC12 cells. Among these analogues, 3b exhibited the most potent protection effect and its underlying mechanism was further investigated. Further results indicated that the ROS scavenging and cytoprotection effect of 3b might be related to the Nrf2 activation and upregulation of related phase II antioxidant enzymes, such as HO-1 and NQO1. In in vivo study, oral administration (100 mg/kg) of 3b significantly attenuated PD-associated behavioral deficits in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced mouse model of PD and protected tyrosine hydroxylase-immunopositive dopaminergic neurons. Our results provided evidence that 3b might be a promising candidate for Parkinson's disease treatment. (C) 2020 Elsevier Masson SAS. All rights reserved.
机译：帕金森病（PD）是一种缓慢的进步和复杂的神经变性障碍。迄今为止，没有批准的药物可以缓慢或逆转PD的神经变性过程。在这里，我们报道了一系列哌啶类似物的合成以及对其神经保护作用的评价对神经元样PC12细胞中的过氧化氢（H2O2）诱导的损伤。在这些类似物中，3B表现出最有效的保护效果，并进一步研究其潜在的机制。进一步的结果表明，3B的ROS清除和细胞保护作用可能与NRF 2活化和相关相II抗氧化酶的上调相关，例如HO-1和NQO1。在体内研究中，在1-甲基-4-苯基-1,2,3,6-四氢吡啶（MPTP）诱导的PD的小鼠模型中，口服给药（100mg / kg）3b中的3b显着减弱了PD相关的行为缺陷并受保护的酪氨酸羟化酶 - 免疫阳性多巴胺能神经元。我们的结果提供了证据表明，3B可能是帕金森病治疗的有希望的候选者。 （c）2020 Elsevier Masson SAS。版权所有。

著录项

  • 来源
  • 作者

    Wang Lun; Cai Xiaoying; Shi Mingsong; Xue Linlin; Kuang Shuang; Xu Ruiling; Qi Wenyan; Li Yan; Ma Xu; Zhang Ruijia; Hong Feng; Ye Haoyu; Chen Lijuan;

  • 作者单位

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ Sch Chem Engn Dept Pharmaceut &

    Biol Engn Chengdu 610065 Peoples R China;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

    Sichuan Univ State Key Lab Biotherapy Collaborat Innovat Ctr Bio Therapy West China Hosp;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 药学;
  • 关键词

    Parkinson's disease; Piperine analogues; Nrf2 activation; MPTP;

    机译：帕金森病;哌啶类似物;NRF2激活;MPTP;

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号