People from just about every culture on earth have occasionally faced
restless, sleepless nights. Fortunately, natural relief is available in
just about every corner of the globe, from Valerian root. In addition,
the majority of Valerian users report feeling refreshed upon waking –
free of drowsiness, and ready to face the day!
Pharmacology and Mechanisms of Action:
Valerian has an affinity for GABAA receptors, likely due to the relatively
high GABA content in valerian itself. The amount of GABA present in
valerian extract is sufficient to induce the release of GABA in
synaptosomes and may also inhibit GABA reuptake.
Other believed mechanisms of action in valerian include inhibition of the
catabolism of GABA by valerenolic acid and acetylvalerenolic acid and
affinity for the 5-HTA receptor by another constituent of valerian called
Due to the herb’s historical use as an anti-convulsant, sedative, migraine
treatment and pain reliever, most basic research has been focused on the
interaction of valerian constituents with the GABA neurotransmitter. The
findings of these studies remain inconclusive. Thus, the true mechanism of
action of valerian remains unknown.
History and Composition:
Valerian Officinalis is native to Europe, North America, and the northern
part of Asia. Altogether, the genus contains about 150 different species.
These are widely distributed throughout the temperate zones. Both the root
and the rhizome are highly prized for their healing properties. The major
healing components found in the valerian root are valepotrits, valeranic
acid, valeranone, valereal. These are all volatile oils that are found only
in valerian. Other volatile oils in the root such as pineole, borneol,
cineole, carophilene, and azulene are also commonly found in other herbs
with healing properties. All of these oils exert anti-inflammatory,
antispasmodic, and nerve-calming effects on the body. In addition, the root
contains alkaloids that are known to relieve pain and relax the body. Other
ingredients found in the root include rutin, beta-sitosterol, salicylic
acid, and choline.1
Valerian can be classified into many different therapeutic categories. It is
one of the best nervine herbs for its efficacy in treating disorders of the
nervous system and in calming the entire body. Other categories include
anodyne (pain reliever), anti-inflammatory, antispasmodic, antiemetic,
carminative (tones, soothes, and stimulates the digestive and elimination
systems), sedative, hypnotic, antihypertensive, and antibacterial.
The herb valerian is most effective in treating a wide range of stress
conditions such as irritability, depression, fear, anxiety, nervous
exhaustion, hysteria, delusions, and nervous tension. It is also indicated
for patients who suffer from insomnia. Valerian not only eases the trouble
of falling asleep but also improves the quality of sleep during the night. After taking valerian, a patient will wake up very rested and alert without
the grogginess seen with some over-the-counter sleeping pills. As a pain
reliever, the herb is useful for treating tension headaches, migraine
headaches, arthritis, and sore muscles.
Valerian has also been found to be effective in a number of nerve
disorders. The herb is useful for treating shingles, sciatica, neuralgia,
multiple sclerosis, and epilepsy. Symptoms suggestive of peripheral
neuropathy such as numbness, tingling sensation, pain, and muscle weakness
are effectively controlled with the use of valerian. It has also been used
to treat attention deficit disorder in adults.
The herb has also found a role in treating a variety of nervous disorders
in children. In one German study, an extract of valerian root was given to
120 children with a wide variety of behavioral disorders such as
restlessness, sleep disorders, hyperactivity, learning disorders, bedwetting, anxiety, headache, and the habits of thumb sucking and
nail-biting. After three weeks of using valerian extract daily, 75 percent
of the children showed marked improvement in their conditions without any
toxicity or negative side effects.3
In ancient Rome, valerian was used to treat certain heart conditions.
Through its positive action on the autonomic nervous system, the herb is
effective in treating tachycardia by slowing down the heart at the same
time gently increasing its force. It also is effective in regulating
arrhythmias. Along with a stabilizing effect on blood pressure,
valerian is an anti-thrombotic that can be used to prevent the formation
of blood clots.4
This stabilizing effect is also seen in the gastrointestinal and
respiratory tracts. Valerian calms the stomach while encouraging the
release of digestive enzymes and reducing the pain and discomfort of
ulcers. In the colon, the herb alleviates cramps, gas, and diarrhea, and
has a soothing effect on the bowel with colitis. Valerian has also proved
helpful in the treatment of asthma.
Unlike other sedatives and drugs, valerian has none of the side effects or
dependency risk that these have. In addition, there is no synergistic
effect when the herb is taken with alcohol. It can also be taken safely
along with other prescription drugs. Valerian is used extensively in Europe
where it is accepted by orthodox medicine. It is found in many
over-the-counter preparations used to treat a variety of nervous disorders.
As more practitioners discover the benefits of valerian, its use will
increase in The United States as well.
1. Pedersen, M. Nutritional Herbology. Bountiful, UT: Pedersen
Publishing,1987, p. 248.
2. Leathwood, P.D., Chauffard, F. Aqueous extract of valerian improves
sleep quality in a man. Pharmacol Biochem Behavior 17:65-71, 1982.
3. Klich, R, Gladbach, B. Verhaltensstoerungen im kindesalter und deren
therapie. MedizinischeWelt 26(25):1252-1254, 1975.
4. Mowrey, D.B. Herbal Tonic Therapies. New Canaan, CT: Keats
Publishing, 1993, pp154-155
Marker Compounds in Herbal Extracts: Valerian (Valeriana Officinalis)
By Ted Waszkuc
Valerian, Valeriana officinalis L. (Valerianacea) has a long history of use
in temperate regions of Europe as a mild sedative due to its documented
central nervous system (CNS) depressant activity.1 It has been used
therapeutically since the Greek and Roman periods and currently is a
top-ranking herb worldwide as a remedy for anxiety and insomnia.
Native to Europe and most often used by Western herbalists, V. officinalis
is a hardy and adaptable perennial plant. It was transported to the New
World by early settlers and now grows in much of the northern United States
and southern Canada. The medicinally valued material consists of
underground parts; i.e. roots and rhizomes. Nowadays, for medicinal use, it
is largely cultivated in Northern and Central Europe.
Investigations of this plant have focused on finding and isolating the
active constituents.2-6 During the last 30 years the identity of substances
believed to be responsible for Valerian’s tranquilizing effect has
frequently changed and still remains controversial.7 Two major groups of
constituents can be distinguished, both terpenoid in nature: Iridoids and
Iridoids found in Valerian root consist of monoterpenic epoxy-triesters
derivatives are collectively known as a Valepotriates, (Valeriana
epoxy-triesters). Different acid substituents, mainly Isovaleric acid, and
its derivatives, can be esterified to the hydroxyl groups present in
Valepotriates. They were isolated from the plant and found to demonstrate
sedative activity. Valepotriates are unstable and hydrolyze rapidly in a
presence of moisture, or acidity (pH < 3) and even moderate heat (>
40°C); hence they have a short life in liquid preparations. Due to this
fact, phytomedicines containing Valepotriates are usually formulated as
solid dosage products like tablets or powder-filled capsules. The
noticeably unpleasant smell associated with Valerian is due to the odor of
Isovaleric acid formed upon hydrolysis of Isovaleric Valepotriate esters.
Since liquid preparations of Valerian, such as alcoholic tinctures and
teas, are still pharmacologically active, constituents other than iridoids
must be responsible for their sedative effect.
Sesquiterpenic carboxylic acids, namely Valerenic, Acetoxyvalerenic, and
Hydroxyvalerenic acid, represent the other class of compounds2,3,6 thought
to be responsible for Valerian preparations’ activity. Valerenic acid is a
spasmolitic and muscle relaxant and inhibits the breakdown of
g-Aminobutyric acid (GABA) at nerve endings.8 The presence of Valerenic
acids (usually about 0.3%) distinguishes V. officinalis from other
Valerinacea, which comprises about 200 known species. Only a few other than
V. officinalis have medicinal uses, with Mexican valerian (Valeriana
edulis) and Indian valerian (Valeriana wallichii) as the most common
examples. Mexican and Indian plant material mainly contain valepotriates
(about 7% w/w and up to 3% w/w, respectively). On the contrary,
Valepotriates level in European Valerian ranges from 0.5% to 1.2%, with
most commercial products averaging at 0.6%.9 None of the Valerenic acids
could be detected in V. edulis or V. wallichii.
The synergistic effect of all the plant’s constituents is now believed to
account for valerian’s pharmacological action. Due to considerable
variation in Valerian preparations’ composition and content - as well as
the instability of some of its constituents - standardization of Valerian
products requires choosing stable, analytically reliable active or marker
compounds characteristic of the plant material. Standardization of
Valeriana officinalis preparations on Valerenic acids content is an
illustrative example when the marker compounds utilized to confirm sample
authenticity and potency may/or may not be active ingredients. Valerenic
acids are stable, non-volatile substances, unique to Valeriana species,
quantifiable by HPLC technique, and commercially available as reference
standards with a moderate cost. Although both Valepotriates and Valerenic
acids are still considered to contribute to Valerian’s sedative action, it
is widely acknowledged that standardization of Valerian-containing
phytomedicines (Valeriana officinalis), using Valerenic acids as identity
markers measured by HPLC technique should be preferred.
To assure the quality of our LifeSource Valerian-containing products we
developed the HPLC method based on the validated USP assay for Valerenic
acid content. The method is modified to quantify all three Valerenic acids
and is specific for V. Officinalis products in both solid and liquid forms.
It can also serve as a reliable check for all Valerian products’
LifeSource Vitamins Valerian Root 500 mg 100 Caps - is most effective in
treating a wide range of stress conditions such as irritability,
depression, fear, anxiety, nervous exhaustion, hysteria, delusions, and
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