Valerian extract characterized by high valerenic acid and low acetoxy valerenic acid contents demonstrates anxiolytic activity
Valerian extract characterized by high valerenic acid and low acetoxy valerenic acid contents demonstrates anxiolytic activity
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DOI：
10.1016/j.phymed.2012.08.003
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发表时间：
2012-10-15
期刊：
影响因子：
7.9
通讯作者：
Brattstroem, A.
中科院分区：
文献类型：
--
作者：
Felgentreff, F.;Becker, A.;Brattstroem, A.
缬草是治疗失眠和焦虑最常用的草药之一。缬草提取物变构调节GABAA受体，这一作用与戊酸有关，是药理研究确定的活性化合物之一。戊烯酸的衍生物，即乙酰戊烯酸或羟基戊烯酸，不会变构调节GABAA受体，但它们结合到相同的结合位点。因此，问题是它们是否会干扰戊酸的作用。两种缬草提取物分别在升高加迷宫试验和悬尾试验中检测抗焦虑和抗抑郁活性。对照物为地西泮（1.0 mg/kg）和丙咪嗪（30 mg/kg）。将提取液标准化为相同总量的酸（0.1、0.5、1.0和2.0 mg/kg），即戊烯酸和乙酰氧基戊烯酸，但酸的比例不同（12:1和1:1.5）。当剂量为0.5 mg/kg时，比例为12:1的提取物显著延长了小鼠在张开臂上的停留时间。另一种提取物按1:1.5的比例，需要量为前者的4倍（2.0 mg/kg）。两种提取物均无抗抑郁作用，相反，比例为1:1.5的提取物延长了静止期。然而，由于1.0和2.0 mg/kg的提取物剂量降低了核心体温，这种延长可能与温度现象有关，并不表明有特定的抑制作用。综上所述，缬草提取物的抗焦虑活性似乎与戊酸有关，而且，关于戊酸总量的标准化，即戊酸和乙氧基戊酸，是误导的。(C) 2012 Elsevier GmbH版权所有。
Valerian is one of the most commonly used herbal remedies for the treatment of insomnia and anxiety. Valerian extracts allosterically modulate GABAA receptors, an action related to valerenic acid, which is one of the active compounds determined from pharmacological studies. Derivatives of valerenic acid, i.e. acetoxy valerenic acid or hydroxy valerenic acid, do not allosterically modulate GABAA receptors, but they bind to identical binding sites. Therefore, the question arises whether they might interfere with the effects of valerenic acid. Two valerian extracts were tested in the elevated plus maze test and the tail suspension test for anxiolytic and antidepressive activity, respectively. Reference substances were diazepam (1.0 mg/kg) and imipramine (30 mg/kg). The extracts were standardized to the identical total amounts of the acids (0.1; 0.5; 1.0 and 2.0 mg/kg), i.e. valerenic and acetoxy valerenic acid, but the ratio between the acids was different (12:1 and 1:1.5). The extract with the ratio 12:1 prolonged the time spent on the open arm significantly when 0.5 mg/kg was applied. Of the other extract, with the ratio 1:1.5, four times that amount was required (2.0 mg/kg). Both of the tested extracts did not show any antidepressive effect, rather the other way around, the extract with the ratio 1:1.5 prolonged the immobility phase. However, since the core body temperature was reduced by the 1.0 and 2.0 mg/kg extract dose, the prolongation may be related to the temperature phenomenon and is not indicative of a specific depressive action. In conclusion, the anxiolytic activity of the valerian extract seems rather related to valerenic acid and, moreover, standardization with respect to the total amount of valerenic acids, i.e. valerenic acid together with acetoxy valerenic acid, is misleading. (C) 2012 Elsevier GmbH. All rights reserved.