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 (1.0mg/kg) and imipramine (30mg/kg). The extracts were standardized to the identical total amounts of the acids (0.1; 0.5; 1.0 and 2.0mg/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 0.5mg/kg was applied. Of the other extract, with the ratio 1:1.5, four times that amount was required (2.0mg/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 2.0mg/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.

译文

缬草是治疗失眠焦虑最常用的草药之一。缬草提取物通过变构调节GABAA受体,这是与戊酸有关的作用,它是药理学研究确定的活性化合物之一。戊酸的衍生物,即乙酰氧基戊酸或羟基戊酸,不变构调节GABAA受体,但它们与相同的结合位点结合。因此,问题是它们是否会干扰戊酸的作用。分别在高架加迷宫试验和尾部悬吊试验中测试了两种缬草提取物的抗焦虑和抗抑郁活性。参考物质是地西epa (1.0 mg/kg) 和丙咪嗪 (30 mg/kg)。将提取物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,但酸之间的比例不同 (12:1和1:1.5)。当施用0.5mg/kg时,比例为12:1的提取物显著延长了在张开臂上花费的时间。在比例为1:1.5的其他提取物中,所需量的四倍 (2.0 mg/kg)。两种测试的提取物均未显示出任何抗抑郁作用,相反,比率为1:1.5的提取物延长了不动相。但是,由于1.0和2.0mg/kg提取物剂量降低了核心体温,因此延长可能与温度现象有关,并且不指示特定的抑郁作用。总之,缬草提取物的抗焦虑活性似乎与戊烯酸相当相关,而且,关于戊烯酸总量 (即戊烯酸与乙酰氧基戊烯酸) 的标准化具有误导性。

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