• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>CNS drug reviews >Role of Hyperforin in the Pharmacological Activities of St. John's Wort.
【24h】

Role of Hyperforin in the Pharmacological Activities of St. John's Wort.

机译：Hyperforin在圣约翰草的药理活性中的作用。

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

The phloroglucinol derivative hyperforin has been recently shown to be a major antidepressant component in the extract of Hypericum perforatum. Experimental studies clearly demonstrated its activity in different behavioral models of depression. Moreover clinical studies linked the therapeutic efficacy of Hypericum extracts to their hyperforin content, in a dose-dependent manner. The molecular mechanism of action of hyperforin is still under investigation. Hyperforin has been shown to inhibit, like conventional antidepressants, the neuronal uptake of serotonin, norepinephrine and dopamine. However, hyperforin inhibits also the uptake of gamma-aminobutyric acid (GABA) and L-glutamate. The uptake inhibition by hyperforin does not involve specific binding sites at the transporter molecules; its mechanism of action seems to be related to sodium conductive pathways, leading to an elevation in intracellular Na(+) concentration. Other additional mechanisms of action of hyperforin, involving ionic conductances as well synaptosomal and vesicular function, have been suggested. In addition to its antidepressant activity, hyperforin has many other pharmacological effects in vivo (anxiolytic-like, cognition-enhancing effects) and in vitro (antioxidant, anticyclooxygenase-1, and anticarcinogenic effects). These effects could be of clinical importance. On the other hand, the role of hyperforin in the pharmacological interactions occurring during Hypericum extract therapy must be fully investigated. Hyperforin seems to be responsible for the induction of liver cytochrome oxidase enzymes and intestinal P-glycoprotein. Several pharmacokinetic studies performed in rats and humans demonstrated oral bioavailability of hyperforin from Hypericum extract. Only recently a new chromatographic method for detection of hyperforin in the brain tissue has been developed and validated. Taking into account the chemical instability of hyperforin, current efforts are directed to the synthesis of new neuroactive derivatives.
机译：邻苯三酚衍生物金丝桃素最近被证明是贯叶连翘提取物中的主要抗抑郁成分。实验研究清楚地证明了其在不同的抑郁行为模型中的活性。此外，临床研究还以剂量依赖的方式将金丝桃属植物提取物的治疗功效与其金丝桃素含量相关联。 Hyperforin作用的分子机制仍在研究中。与常规抗抑郁药一样，Hyperforin可以抑制5-羟色胺，去甲肾上腺素和多巴胺的神经元摄取。但是，hyperforin也会抑制γ-氨基丁酸（GABA）和L-谷氨酸的摄取。 Hyperforin的吸收抑制作用不涉及转运蛋白分子上的特异性结合位点。其作用机制似乎与钠传导途径有关，导致细胞内Na（+）浓度升高。已经提出了hyperforin的其他其他作用机制，包括离子电导以及突触和囊泡功能。除了其抗抑郁活性外，hyperforin在体内和体外还有许多其他药理作用（抗焦虑，认知增强作用）和在体外（抗氧化剂，抗环加氧酶-1和抗癌作用）。这些作用可能具有临床重要性。另一方面，必须充分研究金丝桃素在金丝桃提取物治疗期间发生的药理相互作用中的作用。 Hyperforin似乎负责诱导肝细胞色素氧化酶和肠道P-糖蛋白。在大鼠和人体中进行的几项药代动力学研究表明，贯叶连翘提取物中的hyperforin具有口服生物利用度。直到最近，才开发和验证了一种新的色谱方法，用于检测脑组织中的高蛋白。考虑到hyperforin的化学不稳定性，目前的努力是针对新的神经活性衍生物的合成。

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