Valerenic acid
Encyclopedia
Valerenic acid is a sesquiterpenoid
constituent of the essential oil of the Valerian
plant. Not to be confused with valeric acid
.
Valerian is used as a herbal sedative
which may be helpful in the treatment of insomnia
.
The precise mechanism of this action has not been established. It is likely that several different components of the plant contribute to the effect. Valerenic acid is thought to be at least partly responsible for the sedative effects.
A study in 2004 found valerenic acid to act as a subtype-selective GABAA receptor agonist
in neonatal rat brainstem preparations. The mechanism of this action could not be elucidated in this study.
A study in 2007 on GABA receptors of various composition, expressed in Xenopus
oocytes (frog eggs), found valerenic acid to act mainly at α1β2 and α1β3 subtypes of these receptors. Only channels incorporating β2 or β3 subunits were stimulated by valerenic acid. Modulation of ion channel action was not significantly dependent on incorporation of α1, α2, α3 or α5 subunits.
A study in 2005, in vitro (receptor material not specified in abstract), found valerian extract as well as valerenic acid to be 5HT5A receptor (serotonin receptor) partial agonists.
Part of the binding studies focused on the 5HT5A receptor, which is distributed in the suprachiasmatic nucleus
. This is a tiny region of the brain, which is implicated in the sleep-wake cycle.
A study in 2006 found valerian extract as well as valerenic acid to inhibit NF-κB, a protein complex that controls the transcription
of DNA
, in HeLa
(cultured human cancer) cells. This was measured with the IL-6 / Luc (Interleukin-6 luciferase
) assay as a measurement tool. The study mentioned that such inhibition may be connected to the reported anti-inflammatory
action of the valerian plant.
Sesquiterpene
Sesquiterpenes are a class of terpenes that consist of three isoprene units and have the molecular formula C15H24. Like monoterpenes, sesquiterpenes may be acyclic or contain rings, including many unique combinations...
constituent of the essential oil of the Valerian
Valerian (herb)
Valerian is a hardy perennial flowering plant, with heads of sweetly scented pink or white flowers which bloom in the summer months. Valerian flower extracts were used as a perfume in the sixteenth century....
plant. Not to be confused with valeric acid
Valeric acid
Valeric acid, or pentanoic acid, is a straight-chain alkyl carboxylic acid with the chemical formula C5H10O2. Like other low-molecular-weight carboxylic acids, it has a very unpleasant odor. It is found naturally in the perennial flowering plant valerian , from which it gets its name. Its...
.
Valerian is used as a herbal sedative
Sedative
A sedative or tranquilizer is a substance that induces sedation by reducing irritability or excitement....
which may be helpful in the treatment of insomnia
Insomnia
Insomnia is most often defined by an individual's report of sleeping difficulties. While the term is sometimes used in sleep literature to describe a disorder demonstrated by polysomnographic evidence of disturbed sleep, insomnia is often defined as a positive response to either of two questions:...
.
The precise mechanism of this action has not been established. It is likely that several different components of the plant contribute to the effect. Valerenic acid is thought to be at least partly responsible for the sedative effects.
A study in 2004 found valerenic acid to act as a subtype-selective GABAA receptor agonist
Agonist
An agonist is a chemical that binds to a receptor of a cell and triggers a response by that cell. Agonists often mimic the action of a naturally occurring substance...
in neonatal rat brainstem preparations. The mechanism of this action could not be elucidated in this study.
A study in 2007 on GABA receptors of various composition, expressed in Xenopus
Xenopus
Xenopus is a genus of highly aquatic frogs native to Sub-Saharan Africa. There are 19 species in the Xenopus genus...
oocytes (frog eggs), found valerenic acid to act mainly at α1β2 and α1β3 subtypes of these receptors. Only channels incorporating β2 or β3 subunits were stimulated by valerenic acid. Modulation of ion channel action was not significantly dependent on incorporation of α1, α2, α3 or α5 subunits.
A study in 2005, in vitro (receptor material not specified in abstract), found valerian extract as well as valerenic acid to be 5HT5A receptor (serotonin receptor) partial agonists.
Part of the binding studies focused on the 5HT5A receptor, which is distributed in the suprachiasmatic nucleus
Suprachiasmatic nucleus
The suprachiasmatic nucleus or nuclei, abbreviated SCN, is a tiny region on the brain's midline, situated directly above the optic chiasm. It is responsible for controlling circadian rhythms...
. This is a tiny region of the brain, which is implicated in the sleep-wake cycle.
A study in 2006 found valerian extract as well as valerenic acid to inhibit NF-κB, a protein complex that controls the transcription
Transcription
Transcription may refer to:*Transcription , a business which converts speech into a written or electronic text document*Transcription , software which helps convert speech into text transcript...
of DNA
DNA
Deoxyribonucleic acid is a nucleic acid that contains the genetic instructions used in the development and functioning of all known living organisms . The DNA segments that carry this genetic information are called genes, but other DNA sequences have structural purposes, or are involved in...
, in HeLa
HeLa
A HeLa cell is a cell type in an immortal cell line used in scientific research. It is the oldest and most commonly used human cell line. The line was derived from cervical cancer cells taken on February 8, 1951 from Henrietta Lacks, a patient who eventually died of her cancer on October 4, 1951...
(cultured human cancer) cells. This was measured with the IL-6 / Luc (Interleukin-6 luciferase
Luciferase
Luciferase is a generic term for the class of oxidative enzymes used in bioluminescence and is distinct from a photoprotein. One famous example is the firefly luciferase from the firefly Photinus pyralis. "Firefly luciferase" as a laboratory reagent usually refers to P...
) assay as a measurement tool. The study mentioned that such inhibition may be connected to the reported anti-inflammatory
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....
action of the valerian plant.