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Chemistry News> June
06/05/07 valerenic acid
New research results at the University of Vienna
A team of scientists from the University of Vienna has taken an important step towards elucidating the mechanism of action of valerian. The starting point for this scientific success was research into so-called GABAA.Receptors that are responsible for inhibiting neuronal activities and whose activation promotes sleep.
Fig .: Valerenic acid
Valerian extracts are used as so-called "herbal hypnotics". A young research team led by Steffen Hering, head of the Department of Pharmacology and Toxicology, noticed that valerian extracts have a high level of GABA activityA.Have receptors. A joint research project with Brigitte Kopp, deputy head of the Department of Pharmacognosy, was initiated. Kopp provided a number of pure substances from the valerian plant. The doctoral candidate Sophia Khom finally found what she was looking for in valerenic acid, an active ingredient isolated from valerian extracts. In the following, Khom investigated the molecular point of attack of valerenic acid on GABAA.-Receptor.
Valerian ingredient with an effect comparable to that of anesthetics
She found that valerenic acid does not attack the Valium® receptor, but rather at a point where drugs belonging to the group of injection anesthetics work. Anesthesia means "the non-sensation", thus switching off the nervous system. Anesthetics with a similar effect as valerenic acid do not switch off the sensations, but have a strong sleep-promoting effect. They are therefore administered intravenously in combination with painkillers before operations in order to put patients into a deep sleep quickly.
Khom investigated the effect of valerenic acid on different types of GABAA.Receptors. Valerenic acid only works on those receptors on which other anesthetics are also effective. Using molecular biological methods, changes were made in the structure of the receptors (amino acids exchanged, i.e. mutations set). It was found that mutations at GABAA.-Channels that prevent the effects of anesthetics such as etomidate and propofol also cancel the effects of valerenic acid.
An American research group found out that valerenic acid can be detected in the blood plasma after administration of valerian extracts. It has not yet been clarified which concentrations of it reach the brain. Research on this topic and the mechanism of action of valerenic acid is ongoing at the University of Vienna. "An interesting active ingredient that could be responsible for the sleep-promoting effect of valerian, which has been used for centuries, has now been identified," says pharmacologist Steffen Hering.
Valerenic Acid Potentiates and Inhibits GABAA. Receptors: Molecular Mechanism and Subunit Specificity
S. Khom, I. Baburin, E. Timin, A. Hohaus, G. Trauner, B. Kopp and S. Hering, Neuropharmacology2007
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