• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Pharmacology, Biochemistry and Behavior >The extracts of Fructus Akebiae, a preparation containing 90% of the active ingredient hederagenin: Serotonin, norepinephrine and dopamine reuptake inhibitor
【24h】

The extracts of Fructus Akebiae, a preparation containing 90% of the active ingredient hederagenin: Serotonin, norepinephrine and dopamine reuptake inhibitor

机译：车前子提取物，其中含有90％的活性成分去角质生成素：5-羟色胺，去甲肾上腺素和多巴胺再摄取抑制剂

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

Fructus Akebiae is a traditional Chinese herbal extract that has been used for the treatment of depressive disorders in China. Previous studies demonstrated that Fructus Akebiae extracts (FAE) displayed a potent antidepressant-like activity in animal behavior tests and found that the specific active ingredient from the extracts of Fructus Akebiae is hederagenin. However, the underlying mechanism is unknown. Here we provide evidences that FAE enhances the signaling of central monoamines via inhibition of the reuptake of the extracellular monoamines including serotonin (5-HT), norepinephrine (NE) and dopamine (DA). In rat brain membrane preparations and HEK293 cells transfected with human serotonin transporter (SERT), NE transporter (NET) and DA transporter (DAT), we found that FAE displayed marked affinity to rat and cloned human monoamine transporters in ex vivo and in vitro experiments, using competitive radio ligand binding assay. In uptake assays using rat synaptosomes and transfected cells, FAE was found to significantly inhibit all three monoamine transporters in a dose- and time-dependent manner, with a comparable or better potency to their corresponding specific inhibitors. In contrast, FAE (10 μM), showed no significant affinity to a variety array of receptors tested from CNS. In support of our uptake data, in vivo microdialysis studies showed that administration of FAE (12.6, 25, 50 mg/kg) significantly increased extracellular concentrations of 5-HT, NE and DA in frontal cortex of freely moving rats. Taken together, our current study showed for the first time that FAE is a novel triple inhibitor of monoamine transporters, which may be one the mechanisms of its antidepressant activity.
机译：山茱ke是中国传统的中草药提取物，已被用于治疗抑郁症。先前的研究表明，五味子提取物（FAE）在动物行为测试中显示出强效的抗抑郁样活性，并且发现五味子提取物的特定活性成分是二十三碳精。但是，其潜在机制尚不清楚。在这里我们提供的证据表明，FAE通过抑制细胞外单胺（包括5-羟色胺（5-HT），去甲肾上腺素（NE）和多巴胺（DA））的再摄取来增强中央单胺的信号传导。在大鼠脑膜制剂和人血清素转运蛋白（SERT），NE转运蛋白（NET）和DA转运蛋白（DAT）转染的HEK293细胞中，我们发现FAE在离体和体外实验中对大鼠和克隆的人单胺转运蛋白表现出显着的亲和力，使用竞争性放射性配体结合测定法。在使用大鼠突触小体和转染细胞的吸收测定中，发现FAE以剂量和时间依赖性方式显着抑制所有三种单胺转运蛋白，其效价与其相应的特异性抑制剂相当或更好。相反，FAE（10μM）对经CNS测试的各种受体没有明显的亲和力。为了支持我们的摄取数据，体内微透析研究表明，FAE（12.6、25、50 mg / kg）的使用显着增加了自由运动大鼠额叶皮层中5-HT，NE和DA的细胞外浓度。综上所述，我们目前的研究首次表明，FAE是一种新型的单胺转运蛋白三重抑制剂，这可能是其抗抑郁活性的机制之一。

著录项

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