期刊论文详细信息
BMC Complementary and Alternative Medicine
The anxiolytic effects of a Valerian extract is based on Valerenic acid
Axel Brattström1  Beat Meier2  Helmut Schröder3  Falko Felgentreff3  Axel Becker3 
[1] Alexander Puschkin Str. 50, 39108 Magdeburg, Germany;Inst. Biotechnology, Zürich University of Applied Sciences, Wädenswil, Switzerland;Inst. Pharmacology and Toxicology, Otto-von-Guericke University, Magdeburg, Germany
关键词: Binding;    Anxiety;    Elevated plus maze;    Valerenic acid;    Valerian extract;   
Others  :  1087189
DOI  :  10.1186/1472-6882-14-267
 received in 2014-05-19, accepted in 2014-07-22,  发布年份 2014
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【 摘 要 】

Background

Valerian is commonly used for the treatment of insomnia and anxiety. Valerian extracts allosterically modulate GABA-A receptors and induced an anxiolytic activity. This activity is closely related to valerenic acid. In the present experiments it was investigated whether acetoxy valerenic acid may interfere with the anxiolytic action of valerenic acid.

Methods

Situational anxiety was measured using male CD-1 mice in the elevated plus maze test after oral administration of the test substances. In addition the body core temperature was measured. For the 3H-GABA binding assay dissected tissue from frontal cortex of male RjHan:WI rats were used. Statistical evaluation was performed by means of the non-parametric Kruskal-Wallies H-test, followed by the two-tailed Mann–Whitney U-test.

Results

Adding of acetoxy valerenic acid abolished the anxiolytic action of valerenic acid. There was no effect on body core temperature. Moreover, the valerian extract did not show any affinity to benzodiazepine binding sites.

Conclusion

The determining compound for the observed anxiolytic effect of the valerian extract is its content of valerenic acid.

【 授权许可】

   
2014 Becker et al.; licensee BioMed Central Ltd.

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【 参考文献 】
  • [1]Benke D, Barberis A, Kopp S, Altmann KH, Schubiger M, Vogt KE, Rudolph U, Möhler H: GABAA receptors as in vivo substrate for the anxiolytic action of valerenic acid, a major constituent of valerian root extracts. Neuropharmacology 2009, 56(1):174-181.
  • [2]Khom S, Strommeier B, Ramharter J, Schwarz T, Schwarzer C, Erker T, Ecker GF, Mulzer J, Hering S: Valerenic acid derivatives as novel subunit-selective ligands – in vitro and in vivo characterization. Br J Pharmacol 2010, 161(1):65-78.
  • [3]Murphy K, Kubin ZJ, Shepherd JN, Ettinger RH: Valeriana officinalis root extracts have potent anxiolytic effects in laboratory rats. Phytomedicine 2010, 17:674-678.
  • [4]Khom S, Baburin I, Timin E, Hohaus A, Trauner G, Kopp B, Hering S: Valerenic acid potentiates and inhibits GABAA receptors: molecular mechanism and subunit specificity. Neuropharmacology 2007, 53(1):178-187.
  • [5]Trauner G, Khom S, Baburin I, Benedek B, Hering S, Kopp B: Modulation of GABAA receptors by valerian extracts is related to the content of valerenic acid. Planta Med 2007, 74:19-24.
  • [6]Felgentreff F, Becker A, Meier B, Brattström A: Valerian extract characterized by high valerenic acid and low azetoxy valerenic acid contents demonstrates anxiolytic activity. Phytomedicine 2012, 19:1216-1222.
  • [7]Navarrete A, Avula B, Choi YW: Chemical fingerprinting of valerian species: simultaneous determination of valerenic acids, flavonoids, and phenylpropanoids using liquid chromatography with ultraviolet detection. J AOAC Int 2006, 89:8-18.
  • [8]Yakimova KS, Sann H, Schmid HA, Pierau FK: Effects of GABA agonists and antagonists on temperature-sensitive neurons in the rat hypothalamus. J Physiol 1996, 494:217-230.
  • [9]Zarrindast MR, Dibayan M: Involvement of GABAA receptor sites in diazepam induced hypothermia. Gen Pharmacol 1998, 20:855-859.
  • [10]Nikolov RP, Yakimova KS: Effects of GABA-transaminase inhibitor Vigabatrin on thermoregulation in rats. Amino Acids 2011, 40(5):1441-1445.
  • [11]Rodgers RJ: Animal models of anxiety: where next? Behav Pharmacol 1997, 8:477-496.
  • [12]Goppel M, Franz G: Stability control of valerian ground material and extracts: a new HPLC-method for the routine quantification of valerenic acids and lignans. Pharmazie 2003, 59:446-452.
  • [13]Fernández S, Wasowski C, Paladini AC, Marder M: Sedative and sleep-enhancing properties of linarin, a flavonoid-isolated from Valeriana officinalis. Pharmacol Biochem Behav 2004, 77(2):399-404.
  • [14]Marder M, Viola H, Wasowski C, Fernández S, Medina JH, Paladini AC: 6-methylapigenin and hesperidin: new valeriana flavonoids with activity on the CNS. Pharmacol Biochem Behav 2003, 75(3):537-545.
  • [15]Yuan CS, Mehendale S, Xiao Y, Aung HH, Xie JT, Ang-Lee MK: The gamma-aminobutyric acidergic effects of valerian and valerenic acid on rat brainstem neuronal activity. Anaesth Analg 2004, 98(2):353-358.
  • [16]Sampath C, Haug K, Thanel S, Hamburger M, Derendorf H, Frye R, Butterweck V: Pharmacokinetics of valerenic acid in rats after intravenous and oral administrations. Planta Med 2012, 78:575-581.
  • [17]Awad R, Levac P, Cybulska P, Merali Z, Trudeau VL, Arnason JT: Effects of traditionally used anxiolytic botanicals on enzymes of the γ-aminobutyric acid (GABA). Can J Physiol Pharmacol 2007, 85:933-942.
  • [18]Del Valle-Mojica LM, Ayala-Marin YM, Ortiz-Sanchez CM, Torres-Hernandez BA, Abdalla-Mukhaimer S, Ortiz JG: Selective interactions of Valeriana officinalis extracts and valerenic acid with [3H] glutamate binding to rat synaptic membranes. Evid Based Complementary Altern Med 2011. doi:10.1155/2011/403591
  • [19]de Gage Billoti S, Begaud B, Bazin F, Verdoux H, Dartigues JF, Peres K, Kurth T, Pariente A: Benzodiazepine use and risk of dementia: prospective population based study. BMJ 2012. doi:10.1136/bmj.e6231
  • [20]Olsen RW, Sieghart W: Internationale Union of Pharmacology. LXX. Subtypes of γ-aminobutyric acid A receptors: classification on the basis of subunit composition, pharmacology, and function. Update. Pharmacol Rev 2008, 60(3):242-260.
  • [21]Ramerstorfer J, Furtmüller R, Sarto-Jackson I, Varagic Z, Sieghart W: The GABAA receptor α+β-interface: a novel target for subtype selective drugs. J Neurosci 2011, 31:870-877.
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