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 hydroxypinoresinal.

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

Therapeutic Actions:

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.

References
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

HISTORY

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 Sesquiterpenes.

TECHNICAL DATA

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.

LAB MARKERS

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’ authenticity.

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 nervous tension.*

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