Research update of Valerian Root:

  seminal trace...Valerian Extract.Valerian root extract.Valerienic acid 0.2%0.4%,0.6%,0.8%.CAS.NO:109-52-4.M.F.C5H10O2.Pentanoic acid;Valeric acid;n-Valeric acid...

 


   Phytochemical info of Valerian Root:

 Product Name:
 Synonym:
 Definition: Valerian Root extract are majorly composed of
 Chemical information disclosed as following table:


   Valerian,Nardostachys and Patrinia:

 Almost everyone is familiar with the herb valerian, used for its calming and antispasmodic properties. It is taken in the form of tea, tincture, capsules, or tablets to treat nervousness and insomnia, muscle spasms, and pain. Valerian is one of the principal herbs of the Western tradition, rated among the top 10 herbs in America and Europe (along with garlic, ginkgo, St. John's wort, and echinacea). While valerian is used in the Far East to only a limited extent, an "Oriental valerian" is more commonly used there: it is a close relative called nardostachys. Nardostachys was known in ancient times as "nard" and, later, as spikenard (though other plants have also been given this name, so nardostachys is referred to as "true" spikenard).
 Valerian and nardostachys belong to the Valerianaceae family, one which gives rise to relatively few herbal medicines, these two herbs being the main ones (a third herb, patrinia, is used in Chinese medicine). They share a group of active constituents and the herbs are each characterized by an unusual fragrance, derived from the essential oil component. Below is an overview of their constituents, pharmacology, and medicinal actions.
 


   Valerian:

 There are numerous species of Valerian that have been utilized by herbalists (of approximately 150 species found worldwide, about 20% have been recorded as used for medicinal purposes), but the most common one has been named the official species: Valeriana officinalis. Other species of Valeriana may lack sufficient active constituents to make them as desirable. This herb is believed to be the one recorded by Dioscorides as phu, which refers to the peculiar strong odor of the root that combines pleasant and unpleasant fragrances. The herb may have been later named valerian after the Roman Emperor Valerian (Publius Licinius Valerianus; 253-260 A.D.), or both the herb and Emperor may have been named for their qualities (in Latin, valere means to be in health; valero means to be strong).

 The herb was found to be valuable in the treatment of epilepsy in the Middle Ages, which may be considered the origin of its current use as an antispasmodic. In the modern era, valerian became known as a nervine, a term that implies that it could calm the nervous system while also acting as a tonic (something that strengthens the body; in this case, it would nourish and improve the function of the nervous system). A typical example of the application of nervines is for treatment of nervousness and insomnia that result from stress and overwork. The British herb specialist M. Grieve, in her 1931 publication, A Modern Herbal, relayed the use of valerian during the First World War: "When air-raids were a serious strain on the overwrought nerves of civilian men and women, valerian, prescribed with other simple ingredients, taken in a single dose, or repeated according to the need, proved wonderfully efficacious, preventing or minimizing serious results." The herb was used even more often during the next World War for the same purpose, and valerian has become the principal remedy for nervousness in European herbal medicine.

 Although valerian is also known as an analgesic, more powerful pain-relieving medications have long been available (such as the morphine derivatives and the non-steroidal antiinflammatory drugs), so that it hasn't had much use for this purpose recently. While valerian's antispasmodic action was originally relied upon to treat convulsions and other serious disease symptoms, it is now applied to milder disorders, such as cases of gastro-intestinal spasms and minor peripheral muscular spasms. The majority of valerian research today is aimed at evaluating its potential to treat insomnia and anxiety. As a sleep aid, valerian is sometimes evaluated in combination with hops (Humulus lupulus) and/or lemon balm (Melissa officinalis) In the book Herbal Medicine, a number of double-blind, placebo-controlled studies of valerian's effect (alone or with hops; sometimes in larger formulas, containing lemon balm or other herbs) on sleep have been reviewed; a daily dose of about 400 mg of valerian extract (typically a 4:1 preparation) appears to be effective.
 

  The major active constituents of valerian appear to fall into two broad groups:

 the valepotriates (the main ones are called valtrates), that are non-volatile monoterpenes; and a group of essential oils (volatile compounds), with monoterpenes (mainly bornyl acetate, a type of borneol, with camphene, a type of camphor) and sesquiterpenes (mainly valeric acid) being dominant.

 The valepotriates are a type of iridoid (these are in the triester form; the iridoids in glycoside form are found in rehmannia, scrophularia, gardenia, and vitex, among other Chinese herbs used for clearing heat). These iridoids are thought to confer the primary sedative effect, though the essential oils, especially the sesquiterpenes, are also active. Typically, there is less than 1% of valepotriates and less than 1% of essential oils in the dried valerian roots. The mechanism of action of these compounds has not been fully elucidated, and the speculation about mechanisms will not be relayed here other than to indicate that changes in the levels of neurotransmitters appear to occur as a result of using the herb or its active components. Valerian is collected and cultivated world-wide as a medicinal plant, including Europe, Turkey, India, and China. It is manufactured into widely used medicinal formulations in Europe, particularly in Germany. A German text points out that valerian tincture, a commonly used dosage form, needs to be taken in amounts of one to two teaspoons, rather than a few drops, to attain good results.
 


   Nardostachys:

 The famous aromatic root, nard, was known in ancient times as an ingredient in ointments, and is believed to be the same as the Indian nardostachys, N. jatamansi which has been renamed Nardostachys grandiflora. There is also a Valeriana jatamansi that is similar to nardostachys and used as a substitute. The species name jatamansi is adopted directly from the original Sanskrit name of the herb. The biblical nard was a costly aromatic ointment, preserved in alabaster boxes. Unlike valerian, which has an odor that is often described as unpleasant (sometimes likened to dirty socks), the nardostachys fragrance is considered attractive and similar to expensive musk. Its oil is used in perfumery (especially to fragrance women's hair); the herb is also used in bathwater and it is a major ingredient in incense. In India, it is used in making many massage oils and is said to be useful for many diseases, especially beneficial as a sedative and to treat disorders of the digestive and respiratory systems. In Pakistan it is included in several remedies for hemiplegia, Bell's palsy, and Parkinson's disease.

 Nardostachys, which is native to the Himalayan foothills at high altitude, is used extensively in the TCM tradition. In fact, this herb may have been adopted into the India tradition from China, with plants growing in india being the same species as the variety of Western China provinces of Yunnan and Sichuan (in the mountain regions). Nardostachys was recommended in the TCM tradition for nervous and spasmodic symptoms, such as heart palpitations, headache, shaking, and convulsions. The active constituents of nardostachys are similar to those found in valerian. In China, modern research with the herb has been aimed at examining new uses rather than the traditional ones: it is being examined for its liver protective effects, ability to increase nerve growth factor, and lipid lowering effects. In China, some interest in this herb as an alternative to valerian has been shown, in that preliminary experiments (in laboratory animals) show that it has an even lower toxicity than valerian (which already has low toxicity).

 In China, Nardostachys chinensis, as well as N. jatamansi, is widely used as an analgesic herb. Its Chinese name is gansong or gansongxiang (gan = dry; song refers to the location where it was originally collected, Songban in Sichuan Province; xiang = fragrant); presumably, the fresh herb was used in folk medicine, and it is the dried herb (gan) that is incorporated into the Materia Medica as an item on the herb markets. According to Oriental Materia Medica, it is traditionally used for treating pain in the chest and abdomen that results from qi stagnation associated with internal cold. The herb is warm and regulates qi, having a quality similar to some other fragrant herbs, such as cyperus (xiangfu), saussurea (muxiang), sandalwood (tanxiang), and aquilaria (chenxiang), which have similar applications in treating pain.
  


   Patrina:

 Patrinia is an herb that was not widely used in Chinese herbology (except as a folk remedy) until recently, when interest in its antibacterial action was stimulated by the search for effective compounds to fight infections. It has become particularly well-known for treating appendicitis, with adaptation of an ancient formula from the Jing¨¹i Yaolue (ca. 220 A.D.) in which it is combined with aconite and coix. There is reference to an herb by the same name, baijiangcao, in the Shennong Bencao Jing (ca. 100 A.D.), but several unrelated herbs are now collected under this name, including Thlaspi arvensis (Cruciferae Family) and Sonchus barchyotus (Asteraceae Family); thus the identity of the original plant used is in doubt. The Chinese name refers to the smell of the root (bai = spoiled; jiang = a soy product; referring to the plant's smell like that of spoiled tofu; cao = weed). Traditionally, the herbs collected as baijiangcao have been used to remove toxic heat, resolve phlegm mass, vitalize blood, and resolve swellings. It is used for abscesses and other infectious conditions that are localized. According to the Bencao Gangmu, patrinia is good for discharging pus and removing blood stasis. The herb has been used as a folk remedy for postpartum abdominal pain due to blood stasis.

 Two species of Patrinia are currently in common use in China: P. scabiosaefolia and P. villosa, though other species of this herb are also collected. According to Pharmacology and Applications of Chinese Materia Medica, the sedative action of patrinia is twice as strong as that of valerian. According to clinical trials, the herb is reported to successfully treat neurasthenia symptoms of dizziness, heaviness of the heat, palpitations, hypersensitivity to light and sound, emotional instability, and anorexia. It was also reported effective, usually in combination formulas, for treating infections with swelling, such as mumps, suppurative tonsillitis, appendicitis, and acute pancreatitis, as well as other infections without swellings. Pharmacology experiments reveal a weak antibacterial action, so the herb may function via immune system regulation rather than direct antiseptic action.

 It is reported that side effects of patrinia are rarely seen (mainly dry mouth and gastric discomfort). The active ingredients are still under investigation, but include triterpene saponin glycosides (patrinosides), iridoids (as lactones), and volatile oils. As with nardostachys, research aimed at evaluating its ability to protect and regenerate liver cells is one of the areas of modern interest. Although the root of patrinia was traditionally the part used (as with valerian and nardostachys), now the whole plant of patrinia is collected for medicinal use, with the upper portion being the largest part.


   Research update of Valerian Root.

  Effect of valerian extract preparation (BIM) on the sleep-wake cycle in rats.:Biol Pharm Bull. 2007 Feb;30(2):363-6.[PMID: 17268081]

 In the present study, we studied the effect of valerian extract preparation (BIM) containing valerian extract, golden root (Rhodiola rosea L.) extract and L-theanine (gamma-glutamylethylamide) on the sleep-wake cycle using sleep-disturbed model rats in comparison with that of valerian extract. A significant shortening in sleep latency was observed with valerian extract and the BIM at a dose of 1000 mg/kg. On the other hand, valerian extract and the BIM caused no significant effects on total times of wakefulness, non-rapid eye movement (non-REM) sleep and REM sleep. Valerian extract and the BIM at a dose of 1000 mg/kg also had no significant effect on delta activity. In conclusion, it became clear that the BIM could be useful as a herbal medicine having a sleep-inducing effect without causing an alteration of the sleep-wakefulness cycle.

  Valerian for sleep: a systematic review and meta-analysis.:Am J Med. 2006 Dec;119(12):1005-12.Bent S, Padula A, Moore D, Patterson M, Mehling W.Osher Center for Integrative Medicine, University of California, San Francisco, CA 94121, USA. stephen.bent@ucsf.edu[PMID: 17145239]

 Insomnia affects approximately one-third of the adult population and contributes to increased rates of absenteeism, health care use, and social disability. Extracts of the roots of valerian (Valeriana officinalis) are widely used for inducing sleep and improving sleep quality. A systematic review of randomized, placebo-controlled trials of valerian for improving sleep quality is presented. An extensive literature search identified 16 eligible studies examining a total of 1093 patients. Most studies had significant methodologic problems, and the valerian doses, preparations, and length of treatment varied considerably. A dichotomous outcome of sleep quality (improved or not) was reported by 6 studies and showed a statistically significant benefit (relative risk of improved sleep = 1.8, 95% confidence interval, 1.2-2.9), but there was evidence of publication bias in this summary measure. The available evidence suggests that valerian might improve sleep quality without producing side effects. Future studies should assess a range of doses of standardized preparations of valerian and include standard measures of sleep quality and safety.

   Effects of aqueous, methanolic and chloroform extracts of rhizome and aerial parts of Valeriana officinalis L. on naloxone-induced jumping in morphine-dependent mice.:Addict Biol. 2006 Jun;11(2):145-51.Sharifzadeh M, Hadjiakhoondi A, Khanavi M, Susanabadi M. Department of Toxicology and Pharmacology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran. msharifzadeh@sina.tums.ac.ir[PMID: 16800827]

 In the present study, the effects of rhizomes and aerial parts extracts of Valeriana officinalis L. on morphine dependence in mice have been investigated. Animals were treated subcutaneously with morphine (50, 50 and 75 mg/kg) three times daily (10 am, 1 pm and 4 pm) for 3 days, and a last dose of morphine (50 mg/kg) was administered on the fourth day. Withdrawal syndrome (jumping) was precipitated by naloxone (5 mg/kg) which was administered intraperitoneally 2 hours after the last dose of morphine. To study the effects of the aqueous, methanolic and chloroform extracts of both aerial parts and rhizome of the V. officinalis L. on naloxone-induced jumping in morphine-dependent animals, 10 injections of morphine (three administrations each day) for dependence and a dose of 5 mg/kg of naloxone for withdrawal induction were employed. Intraperitoneal injection of different doses (1, 5, 25 and 50 mg/kg) of aqueous, methanolic and chloroform extracts of the rhizome of V. officinalis L. 60 minutes before naloxone injection decreased the jumping response dose-dependently. Pre-treatment of animals with different doses (1, 5, 25, 50 and 100 mg/kg) of aqueous and methanolic extracts of aerial parts of V. officinalis L. 60 minutes before naloxone injection caused a significant decrease on naloxone-induced jumping. The chloroform extract of the aerial parts of V. officinalis L. did not show any significant changes on jumping response in morphine-dependent animals. It is concluded that the extracts of V. officinalis L. could affect morphine withdrawal syndrome via possible interactions with inhibitory neurotransmitters in nervous system.

   Chemical fingerprinting of valeriana species: simultaneous determination of valerenic acids, flavonoids, and phenylpropanoids using liquid chromatography with ultraviolet detection.:J AOAC Int. 2006 Jan-Feb;89(1):8-15.Navarrete A, Avula B, Choi YW, Khan IA.National Center for Natural Products Research, Research Institute of Pharmaceutical Sciences, The University of Mississippi, MS 38677, USA. anavarrt@servidor.unam.mx[PMID: 16512222]

 The roots and rhizomes of various valeriana species are currently used as a sleeping aid or mild sedative. A liquid chromatography method has been developed that permits the analysis of chlorogenic acid, lignans, flavonoids, valerenic acids, and valpotrates in various valerian samples. The best results were obtained with a Phenomenex Luna C18(2) column using gradient elution with a mobile phase consisting of water and 0.05% phosphoric acid and 2-100% acetonitrile-methanol (1 + 1) with 0.05% phosphoric acid. The flow rate was 0.8 mL/min and ultraviolet detection was at 207, 225, 254, 280, and 325 nm. Different valerian species and commercial products showed remarkable quantitative variations. Chlorogenic acid (0.2-1.2%), 3 lignans, linarin (0.002-0.24%), and valepotriates were detected in all the valeriana species analyzed. Highest amounts of valerenic acids were detected in V. officinalis L., trace amounts in V. sitchensis, and none in the other species analyzed.

   A combination of valerian and lemon balm is effective in the treatment of restlessness and dyssomnia in children.:Phytomedicine. 2006 Jun;13(6):383-7. Epub 2006 Feb 17.Muller SF, Klement S.Dr. Willmar Schwabe Pharmaceuticals, Karlsruhe, Germany.[PMID: 16487692]

 Efficacy and tolerability of a combined valerian/lemon balm preparation were investigated in an open, multicentre study in children less than 12 years suffering from restlessness and nervous dyskoimesis. Patients were dosed individually by the investigators. In total, 918 children were evaluated for therapeutic efficacy and tolerability. A distinct and convincing reduction in severity was found for all symptoms in the investigators' and parents' ratings. The core symptoms dyssomnia and restlessness were reduced from "moderate/severe" to "mild" or "absent" in most of the patients. In total, 80.9% of the patients who suffered from dyssomnia experienced an improvement for this symptom and 70.4% of the patients with restlessness improved clearly. For the other listed symptoms the total improvement was 37.8% on average. Both, parents and investigators assessed efficacy as to be "very good" or "good" (60.5% and 67.7%, respectively). The tolerability of Euvegal forte was considered as "good" (in 96.7% of the patients it was judged to be "very good" or "good"). No study medication-related adverse events occurred. In conclusion, Euvegal forte was effective in the treatment of younger children with restlessness and dyssomnia and it was very well tolerated.


  Herbal products: behaviors and beliefs among Italian women.:Pharmacoepidemiol Drug Saf. 2006 May;15(5):354-9.Zaffani S, Cuzzolin L, Benoni G.Department of Medicine & Public Health, Section of Pharmacology, University of Verona, Verona, Italy. zaffani@yahoo.it[PMID: 16329162]

 PURPOSE: The use of phytotherapy is growing worldwide, but the popular perception is that this kind of approach is natural and therefore safer than traditional medicine; for this reason the use is frequently not communicated to the doctor. Instead, even if many herbal remedies are benign in nature, some of these therapies have potentially harmful side effects or adverse interactions with other medications. So, the purpose of our study was to analyze the behavior patterns and decision-making modalities about herbal remedy use among a sample of Italian women. METHODS: During a 5-month period, interviews to women attending the outpatient ambulatory of an urban university general hospital were made on the basis of a pre-structured 25-item questionnaire. RESULTS: Among a random study population of 1,044 subsequent patients, 491 women (47.03%) reported to have been taking one or more herbal products in the last year, sometimes used during pregnancy or given to their children (35.23%). The 10 most frequently used herbal products reported were propolis, aloe, valerian root, blueberry, fennel, dandelion, mallow, arnica, thyme, and Echinacea. The major purposes for using these products were to stimulate the immune system and to cure respiratory problems. 47/491 (9.57%) women reported side effects, but only 36% referred to the doctor. In most of the cases, herbal products were taken in combination with drugs (44.61%) or homeopathic treatments (11.81%). The majority of our women did not obtain information about this kind of therapy from a health care provider (72.71%). CONCLUSIONS: The present survey highlights the general use of phytomedicines by a sample of Italian women, the potential risk of their confidence with the 'natural world,' and the lack of discussion on this argument with doctors and pharmacists. This suggests the importance of training for health care providers and the need of informational programs for consumers.

  Pharmacokinetics of valerenic acid after administration of valerian in healthy subjects.:Phytother Res. 2005 Sep;19(9):801-3.Anderson GD, Elmer GW, Kantor ED, Templeton IE, Vitiello MV.Department of Pharmacy, University of Washington, Seattle, 98195, USA. gaila@u.washington.edu[PMID: 16220575]

 OBJECTIVES: To describe the pharmacokinetics of valerenic acid in a group of healthy adults after a single oral dose of valerian using a newly developed sensitive assay for serum concentrations of valerenic acid, a commonly used marker for qualitative and quantitative analysis of valerian root and valerian products. STUDY DESIGN: Six healthy adults (22-61 years, five men, one female) received a single 600 mg dose of valerian at 08:00. Blood samples were collected for 8 h after administration. Valerenic acid was extracted from serum and measured using a LC/MS/MS method developed in our laboratory. RESULTS: The maximum serum concentration of valerenic acid for five of the six subjects occurred between 1 and 2 h ranging from 0.9 to 2.3 ng/mL. Valerenic acid serum concentrations were measurable for at least 5 h after the valerian dose. One subject showed a peak plasma value at 1 h and a second peak at 5 h. The elimination half-life (T(1/2)) for valerenic acid was 1.1 +/- 0.6 h. The area under the concentration time curve (AUC) as a measure of valerenic acid exposure was variable (4.80 +/- 2.96 microg/mL. h) and not correlated with subject's age or weight. CONCLUSIONS: Assuming that valerenic acid serum concentrations correlate with the pharmacological activity of valerian, the timing of the valerenic acid peak concentration is consistent with the standard dosage recommendation to take valerian 30 min to 2 h before bedtime. Ongoing studies are evaluating the relationship between valerenic acid serum concentrations and objective measures of sleep in patients.

   Preserved pharmacological activity of hepatocytes-treated extracts of valerian and St. John's wort.:Planta Med. 2005 Jul;71(7):592-8.Simmen U, Saladin C, Kaufmann P, Poddar M, Wallimann C, Schaffner W.Institute of Pharmaceutical Biology, University of Basel, Basel, Switzerland. usimmen@dtc.ch.[PMID: 16041642]

 The two herbal extracts valerian (Valeriana officinalis L.) and St. John's wort (Hypericum perforatum L.) were studied for their metabolic changes upon incubation with freshly prepared rat hepatocytes and subsequently analysed phytochemically as well as pharmacologically in vitro. Quantitative HPLC analysis of valerian extracts revealed considerable metabolic activities with regard to sesquiterpenes and iridoids. The amount of acetoxyvalerenic acid decreased 9-fold, while that of hydroxyvalerenic acid correspondingly increased 9-fold due to O-deacetylation. The valepotriates didrovaltrate, isovaltrate and valtrate decreased 2-, 18- and 16-fold, respectively. However, the binding affinities of the incubated extracts to the benzodiazepine and picrotoxin binding site of the GABA (A) receptor were quite similar to those of the non-incubated extracts. Neither valerenic acids nor valepotriates exhibited any significant effect on the two binding sites when tested as single compounds. Therefore, either other constituents represent the active ones or multiple compounds are necessary for the observed inhibitory and allosteric effects at the GABA (A) receptor. Extracts of St. John's wort were less potently metabolised than valerian. The amount of pseudohypericin and the main flavonoids (hyperoside, rutin, isoquercitrin, quercitrin, quercetin and I3,II8-biapigenin) slightly decreased during the 4-h incubation period. Both the antagonist effect at the corticotropin-releasing factor (CRF) type 1 receptor and the binding inhibition at the 5-HT transporter were attenuated during the metabolic treatment. The reduced antagonist effect correlates with the decreasing amount of pseudohypericin known to be a CRF (1) receptor antagonist. In conclusion, the incubation of plant extracts with freshly prepared rat hepatocytes represents a useful approach to study the pharmacological action of metabolised plant extracts. The consistent pharmacological activity of both valerian and St. John's wort is concordant with the known clinical efficacy of pharmacological activities.

   Management of insomnia: a place for traditional herbal remedies.:Prescrire Int. 2005 Jun;14(77):104-7.[PMID: 15984105 ]

 (1) Insomnia should be treated first with non drug measures; this has traditionally involved the use of herbal remedies. (2) About 20 plants are approved in France in the production of medications 'traditionally used' for minor sleep disturbances. Virtually nothing is known of their efficacy or potential dangers. (3) Most of these plants are suspected of toxicity and should therefore be avoided, especially in view of their unproven efficacy. (4) Littleleaf linden, vervain, melissa and orange flower have no demonstrated efficacy but are safe and can therefore be used. Similarly, there are no scientific grounds for rejecting preparations based on hawthorn or passiflora. (5) Available data suggest that valerian extracts have a modest impact on subjective sleep quality; they are nevertheless more effective than a placebo. Valerian products that do not contain valepotriates have no apparent adverse effects. It is best to avoid high-titre alcoholic extracts and powdered valerian root, and to select aqueous extracts and low-titre hydro-alcoholic preparations.

   Isobolographic analysis of the sedative interaction between six central nervous system depressant drugs and Valeriana edulis hydroalcoholic extract in mice.:J Pharm Pharmacol. 2005 May;57(5):631-9.Ugalde M, Reza V, Gonzalez-Trujano ME, Avula B, Khan IA, Navarrete A.Facultad de Quimica, Departamento de Farmacia, Universidad Nacional Autonoma de Mexico, Ciudad Universitaria Coyoacan 04510, Mexico D.F., Mexico.[PMID: 15901352]

 It has been declared frequently that valerian may potentiate the effect of other central nervous system (CNS) depressant drugs, however there has been a lack of experimental data. We have evaluated the profile of the interactions between the ethanol extract of Valeriana edulis spp procera and six CNS depressant drugs using an exploratory model to test the sedative effect in mice. All the compounds tested showed a dose-dependent sedative effect with the following ED50 values: valerian 181.62, diazepam 1.21, ethanol 1938, pentobarbital 11.86, buspirone 1.04, haloperidol 0.41 and diphenhydramine 17.06 mg kg-1. An isobolographic analysis was used to evaluate the sedative interaction of the intraperitoneal co-administration of 1:1 fixed-ratio combination of equi-effective doses of valerian extract with each CNS depressant drug. The ED50 theoretical (Zadd) and experimental (Zexp) for each combination were: valerian+diazepam,Zadd=91.41 mg kg-1, Zexp=81.64 mg kg-1; valerian+ethanol, Zadd=1060.22 mg kg-1, Zexp=687.89 mg kg-1; valerian+pentobarbital, Zadd=96.74 mg kg-1, Zexp=151.83 mg kg-1; valerian+buspirone, Zadd=91.33 mg kg-1, Zexp=112.73 mg kg-1; valerian+haloperidol, Zadd=91.01 mg kg-1, Zexp=91.52 mg kg-1; valerian+diphenhydramine, Zadd=99.34 mg kg-1, Zexp=123.52 mg kg-1. Neither synergistic nor attenuate effects were found in any of the combinations evaluated. We concluded that the valerian extract did not potentiate the sedative effect of commonly prescribed CNS depressant drugs as was expected. The additive effect found through the isobolographic analysis suggested that the sedative effect of V. edulis resulted from the activation of common mechanisms of haloperidol, diazepam, buspirone, pentobarbital, diphenhydramine and ethanol.


  Studies on HPLC fingerprint of the hydrophilic constituents of Valeriana medicinal plants.:Zhongguo Zhong Yao Za Zhi. 2005 Mar;30(6):426-9.Shi JL, Liu Y, Xiao PG.School of Chinese Pharmacology, Beijing University of Chinese Medicine, Beijing 100102, China. shijl@vip.sina.com[PMID: 15810445]

 OBJECTIVE: To establish the fingerprint of the hydrophilic constituents of Valeriana medicinal plants. METHOD: The HPLC-UV assay was used to establish the fingerprint of the hydrophilic constituents of Valeriana medicinal plants. RESULT: The HPLC fingerprint profiles of the hydrophilic constituents of Valeriana medicinal plants contains 12 common peaks. The relative retention time and the ranges of relative area of the common peaks were determined. CONCLUSION: The fingerprint profile can be used for the identification and quality control of Valeriana medicinal plants.

  Determination of metal content in valerian root phytopharmaceutical derivatives by atomic spectrometry.:J AOAC Int. 2005 Jan-Feb;88(1):221-5.Arce S, Cerutti S, Olsina R, Gomez MR, Martinez LD.Area de Farmacotecnia, Universidad Nacional de San Luis, Facultad de Quimica, Bioquimica y Farmacia, Chacabuco y Pedernera, San Luis, Argentina.[PMID: 15759744]

 Phytopharmaceuticals containing Valerian are used as mild sleep-inducing agents. The elemental composition of 3 different marks of Valeriana officinalis roots commercially available in the Argentinian market, their teas, and a commercial tincture have been studied. The content of Al, Ca, Cd, Co, Cr, Cu, Fe, Li, Mn, Ni, Pb, V, and Zn was determined in phytopharmaceuticals by flame atomic emission/absorption spectrometry, electrothermal atomic absorption spectrometry, and ultrasonic nebulization coupled to inductively coupled plasma-optical emission spectrometry. Prior to analyses of the samples, a digestion procedure was optimized. The analytical results obtained for Fe, Al, Ca, and V in the solid sample study were within the range 100-1000 mg/kg, and for Mn, Zn, and Pb within the range 10-100 mg/kg. Cadmium was found at levels up to 0.0125 mg/kg.

   Could valerian have been the first anticonvulsant?:Epilepsia. 2004 Nov;45(11):1338-43.Eadie MJ.Department of Medicine, University of Queensland, Royal Brisbane Hospital, Brisbane, Australia. M.Eadie@mailbox.uq.edu.au[PMID: 15509234]

 PURPOSE: To assess the available evidence for the belief that valerian, highly recommended in the past for treating epilepsy, possessed real anticonvulsant effectiveness. METHODS: Review of available literature. RESULTS: In 1592, Fabio Colonna, in his botanical classic Phytobasanos, reported that taking powdered valerian root cured his own epilepsy. Subsequent reports of valerian's anticonvulsant effectiveness appeared. By the late 18th and early 19th centuries, it was often regarded as the best available treatment for the disorder. Valerian preparations yield isovaleric acid, a substance analogous to valproic acid and likely to possess anticonvulsant properties, as isovaleramide does. In favorable circumstances, high valerian doses can be calculated to have sometimes provided potentially effective amounts of anticonvulsant substance for epilepsy patients. CONCLUSIONS: Valerian probably did possess the potential for an anticonvulsant effect, but the uncertain chemical composition and content of valerian preparations, and their odor and taste, made it unlikely that they could ever prove satisfactory in widespread use.

   Extraction of valerenic acids from valerian (Valeriana officinalis L.) rhizomes.:Pharmazie. 2004 Sep;59(9):727-8.Boyadzhiev L, Kancheva D, Gourdon C, Metcheva D.Institute of Chemical Engineering, Bulgarian Academy of Sciences, Sofia, Bulgaria. lboyadz@bas.bg[PMID: 15497760]

 Extraction of valerenic acids (valerenic, acetoxyvalerenic and hydroxyvalerenic) from dry ground rhizomes of valerian (Valeriana officinalis L.) was studied. The effect of ethanol concentration in the solvent, extraction temperature and drug particle size on extraction kinetics were investigated and the optimum values of these process parameters were determined for the case of intensively stirred two-phase dispersion. It was found that increased processing temperature favors extraction kinetics, but provokes moderate degradation of valerenic acids.

   Neuroprotective properties of Valeriana officinalis extracts.:Neurotox Res. 2004;6(2):131-40.Malva JO, Santos S, Macedo T.Institute of Biochemistry, Faculty of Medicine and Center for Neuroscience and Cell Biology, University of Coimbra, 3004-504 Coimbra, Portugal. jomalva@cnc.cj.uc.pt[PMID: 15325965]

 Valeriana officinalis have been used in traditional medicine for its sedative, hypnotic, and anticonvulsant effects. There are several reports in the literature supporting a GABAergic mechanism of action for valerian. The rationale of the present work is based on the concept that by decreasing neuronal network excitability valerian consumption may contribute to neuroprotection. The aim of our investigation was to evaluate the neuroprotective effects of V. officinalis against the toxicity induced by amyloid beta peptide 25-35 Abeta(25-35). Cultured rat hippocampal neurons were exposed to Abeta(25-35) (25 microM) for 24-48 h, after which morphological and biochemical properties were evaluated. The neuronal injury evoked by Abeta, which includes a decrease in cell reducing capacity and associated neuronal degeneration, was prevented by valerian extract. Analysis of intracellular free calcium (Ca(2+)i) indicated that the neuroprotective mechanisms may involve the inhibition of excess influx of Ca2+ following neuronal injury. Moreover, membrane peroxidation in rat hippocampal synaptosomes was evaluated, and our data indicate that valerian extract partially inhibited ascorbate/iron-induced peroxidation. In conclusion we show evidence that the signalling pathways involving Ca(2+)i and the redox state of the cells may play a central role in the neuroprotective properties of V. officinalis extract against Abeta toxicity. The novelty of the findings of the present work, indicating neuroprotective properties of valerian against Abeta toxicity may, at the long-term, contribute to introduction of a new relevant use of valerian alcoholic extract to prevent neuronal degeneration in aging or neurodegenerative disorders.


  The fixed combination of valerian and hops (Ze91019) acts via a central adenosine mechanism.:Planta Med. 2004 Jul;70(7):594-7.Schellenberg R, Sauer S, Abourashed EA, Koetter U, Brattstrom A.Institut fur Ganzheitliche Medizin und Wissenschaft, Huttenberg, Germany.[PMID: 15254851]

 The aim of the study was to demonstrate competition between caffeine and a fixed valerian/hop extract combination (Ze91019) by the central adenosine mechanism. EEG was used to describe the action of caffeine on the central nervous system after oral administration (200 mg) in healthy volunteers. In addition to caffeine, the volunteers (16 in each group) received either placebo or verum (2 and 6 tablets containing the valerian/hop extract). The EEG responses were recorded every 30 min thereafter. The verum medication was capable of reducing (2 tablets) or inhibiting (6 tablets) the arousal induced by caffeine. This pharmacodynamic action was observed 60 minutes after oral administration, indicating not only competition between the antagonist caffeine and the partial agonist, i. e., the valerian/hop extract but also bio-availability of the compound(s) responsible for the agonistic action. In conclusion, the valerian/hop extract acts via a central adenosine mechanism which is possibly the reason for its sleep-inducing and -maintaining activity.

  Stability control of valerian ground material and extracts: a new HPLC-method for the routine quantification of valerenic acids and lignans.:Pharmazie. 2004 Jun;59(6):446-52.Goppel M, Franz G. Department of Pharmaceutical Biology, Institute of Pharmacy, University of Regensburg, Germany.[PMID: 15248459]

 A new HPLC-method for the separation of medium polar and nonpolar compounds in preparations of Valeriana officinalis was established for stability control. Powdered valerian root and a commercial ethanolic valerian extract were investigated for apparent differences in stability behaviour. Storage conditions were chosen according to the ICH-guidelines. Changes in composition of valerenic acids and lignans were observed depending on storage conditions and packaging materials. Hydroxyvalerenic acid, pinoresinol and hydroxypinoresinol were identified as degradation products in Valerian root, especially during accelerated testing. Ethanolic extracts appeared not to be as sensitive for chemical degradation under climatic influences compared to the crude plant material, and showed no increase in the amounts of lignan-aglyka. In comparison, extracts showed high sensitivity on changes of physical properties like loss on drying and viscosity.

   Valerian does not appear to reduce symptoms for patients with chronic insomnia in general practice using a series of randomised n-of-1 trials.:Complement Ther Med. 2003 Dec;11(4):215-22.Coxeter PD, Schluter PJ, Eastwood HL, Nikles CJ, Glasziou PP. Herbal Medicines Research and Education Center, University of Sydney, Sydney, NSW, Australia.[PMID: 15022653]

 OBJECTIVE: To investigate the effectiveness of valerian for the management of chronic insomnia in general practice. DESIGN: Valerian versus placebo in a series of n-of-1 trials, in Queensland, Australia. RESULTS: Of 42 enrolled patients, 24 (57%) had sufficient data for inclusion into the n-of-1 analysis. Response to valerian was fair for 23 (96%) participants evaluating their "energy level in the previous day" but poor or modest for all 24 (100%) participants' response to "total sleep time" and for 23 (96%) participants' response to "number of night awakenings" and "morning refreshment". As a group, the proportion of treatment successes ranged from 0.35 (95% CI 0.23, 0.47) to 0.55 (95% CI 0.43, 0.67) for the six elicited outcome sleep variables. There was no significant difference in the number (P=0.06), distribution (P=1.00) or severity (P=0.46) of side effects between valerian and placebo treatments. CONCLUSIONS: Valerian was not shown to be appreciably better than placebo in promoting sleep or sleep-related factors for any individual patient or for all patients as a group.

   Comparative cognitive and psychomotor effects of single doses of Valeriana officianalis and triazolam in healthy volunteers.:Hum Psychopharmacol. 2003 Dec;18(8):619-25.Hallam KT, Olver JS, McGrath C, Norman TR.Department of Psychiatry, The University of Melbourne, Austin and Repatriation Medical Centre, Heidelberg, Vic 3084, Australia.[PMID: 14696021]

 OBJECTIVES: To assess the cognitive and psychomotor effects of single oral doses of valerian in healthy volunteers in comparison with a placebo and the hypnotic agent triazolam. METHODS: In a double-blind, placebo-controlled, four-way crossover study nine healthy subjects (5 males, 4 females) received in random order valerian 500 mg, valerian 1000 mg, triazolam 0.25 mg and placebo. Doses were separated by a wash-out period of at least 1 week. Subjects were tested before each dose and at 2, 4 and 8 h after the dose of each compound using the critical flicker fusion (CFF), choice reaction time (CRT), digit symbol substitution test (DSST), symbol search test (SST), digit span test (DST) and visual analogue scales of mood. RESULTS: Repeated measures ANOVA was used to examine the changes in performance on tests over time and significant effects were further analysed using simple main effects analysis with least significant difference corrections. Statistically significant differences were only noted for the cognitive tests: SST (F(3, 8)=3.182, p<0.05) and DSST (F(3, 8)=9.688, p<0.005). In both cases the differences between groups were due to the effects of triazolam. CONCLUSION: These data confirm that at recommended therapeutic doses, triazolam has detrimental effects on cognitive processes in healthy volunteers as found in previous studies. Valerian was without effect on either cognitive or psychomotor performance in healthy volunteers at the doses used in this study. Should the hypnotic activity of valerian be confirmed in randomized double-blind trials it may be a less troublesome alternative to benzodiazepines in the treatment of insomnia.

   In vitro release of valerenic and hydroxyvalerenic acids from valerian tablets.:Pharmazie. 2003 Sep;58(9):636-8.Torrado JJ.Dpto. Farmacia y Tecnologia Farmaceutica, Facultad de Farmacia (UCM) Madrid, Spain. torrado1@farm.ucm.es[PMID: 14531459 ]

 Although most commercial valerian formulations are coated tablets not any comparison study of their drug release profiles has been published so far. The main objective of this work is to establish a drug release test suitable for studying and comparing different valerian tablets. Thus, hydroxyvalerenic and valerenic acid concentrations were assayed by HPLC using a C18 Kromasil (200 x 4.6 mm, 5 microm) column and a mobile phase containing methanol and an orthophosphoric acid solution 0.5% v/v in water at a ratio of 75:25 at a constant flow rate of 1 ml/min. Saturation solubilities for hydroxyvalerenic and valerenic acid at pH 6.8 were 26 +/- 5.1 and 1 +/- 0.6 microg/ml, respectively. Usually for drugs with such low solubility values, their oral absorption and hence bioavailability are limited by their dissolution characteristics. A dissolution test was conducted according to the general method 2 (paddles) of USP 24 using 500 ml buffer medium (pH 6.8) at 50 rpm. Five different formulations were studied and compared: one uncoated tablet formulation and four marketed coated tablets. The uncoated tablet formulation had the fastest release profile, whereas the coated tablets manifested very different release patterns, depending on the type of formulation. Because of these differences in drug release pattern not every tablet formulation may be appropriate for the same clinical indications. Clinical data are required to confirm the correlation between drug release pattern and the therapeutically value of each formulation.


  Iridoids from the rhizomes and roots of Valeriana jatamansi.:J Nat Prod. 2002 Dec;65(12):1949-52.Tang Y, Liu X, Yu B. State Key Laboratory of Bio-organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, People's Republic of China. ytang6@imap2.asu.edu.[PMID: 12502349]

 Five new iridoids, 1-homoacevaltrate (1), 1-homoisoacevaltrate (2), 11-homohydroxyldihydrovaltrate (3), 10-acetoxy-1-homovaltrate hydrin (4), and 10-acetoxy-1-acevaltrate hydrin (5), along with 10 known analogues, were isolated from the rhizomes and roots of Valeriana jatamansi. Structural elucidation was based on spectroscopic data interpretation.

  (-)-3 beta,4 beta-epoxyvalerenic acid from Valeriana officinalis.:Planta Med. 2002 Jul;68(7):661-2.Dharmaratne HR, Nanayakkara NP, Khan IA.[PMID: 12143008]

 Chemical investigation of the root extract of Valeriana officinalis afforded a new bicyclic sesquiterpene acid, (-)-3 beta,4 beta-epoxyvalerenic acid together with valerenic acid and hexadecanoic acid. The structure of the new compound was elucidated by spectroscopic data and confirmed by partial synthesis of its methyl ester from valerenic acid. Methyl (-)-3 alpha,4 alpha-epoxyvalerenate was obtained as a minor product from the above reaction.

   Effect of valerian, Valeriana edulis, on sleep difficulties in children with intellectual deficits: randomised trial.:Phytomedicine. 2002 May;9(4):273-9.Francis AJ, Dempster RJ.Department of Psychology and Disability Studies, Royal Melbourne Institute of Technology University, Victoria, Australia. andrew.francis@rmit.edu.au[PMID: 12120807]

 Serious sleep problems are common in children with an intellectual deficit (ID), and are often the source of much distress for both the child and caregivers. As yet, no satisfactory long-term treatment exists for intransigent sleep difficulties in children with an ID. Valerian, Valeriana spp., has been used for thousands of years to induce relaxation and sleep. Scientific investigation of valerian's sleep promoting ability in humans, whilst limited, has yielded promising findings. This initial study aimed to explore valerian's potential for assisting in the treatment of sleep problems in children with an ID. Five children with varying intellectual deficits and different primary sleep problems underwent eight continuous weeks of monitoring via sleep diaries, adhering to a double blind, placebo controlled and randomised design. Compared to baseline and placebo, valerian treatment led to significant reductions in sleep latencies and nocturnal time awake, lengthened total sleep time and improved sleep quality. The treatment was apparently most effective in children with deficits that involved hyperactivity. Although the findings are preliminary and in need of replication, there is evidence to suggest that valerian may be useful in the safe and effective long-term treatment of intransigent sleep difficulties in children with ID's, and therefore warrants further investigation.

   The safety of herbal medicines in the psychiatric practice.:Harefuah. 2001 Aug;140(8):780-3, 805.Boniel T, Dannon P. Pharmaceutical Service, Sheba Medical Center, Tel-Hashomer, Ramat-Gan.[PMID: 11547487 ]

 The use of alternative medicines is increasing world-wide and in Israel. These drugs, considered by the Ministry of Health as food supplements, are to be obtained at pharmacies and health stores and are being sold freely, without any professional advice. Many of the herbs are used by patients to treat psychiatric disorders. These herbs have a pharmacological activity, adverse effects and interactions with conventional drugs, which can produce changes in mood, cognition, and behavior. We present the most commonly used herbal drugs, and discuss their safety and efficacy in psychiatric practice. Hypericum--used as an antidepressant and as an antiviral medicine, was reported in 23 randomized clinical trials reviewed from the MEDLINE. It was found to be significantly more effective than placebo and had a similar level of effectiveness as standard antidepressants. Recent studies almost clearly prove that this herb, like most of the conventional antidepressants, can induce mania. Valerian--is used as an anti-anxiety drug, and reported to have sedative as well as antidepressant properties. In contrast to the significant improvement in sleep that was found with the use of valerian, compared to placebo, there are several reports on the valerian root toxicity. This includes nephrotoxicity, headaches, chest tightness, mydriasis, abdominal pain, and tremor of the hands and feet. Ginseng--another plant that is widely used as an aphrodisiac and a stimulant. It has been associated with the occurrence of vaginal bleeding, mastalgia, mental status changes and Stevens-Johnson syndrome after it's chronic administration. It has interactions with digoxin, phenelzine and warfarin. Ginkgo--in clinical trials the ginkgo extract has shown a significant improvement in symptoms such as memory loss, difficulties in concentration, fatigue, anxiety, and depressed mood. Long-term use has been associated with increased bleeding time and spontaneous hemorrhage. Ginkgo should be used cautiously in patients receiving aspirin, NSAIDs, anticoagulants or other platelet inhibitors. Health care professionals can no longer ignore the widespread use of alternative medicines and cannot continue with the "don't ask, don't tell" policy. Clinicians should ask the patients about their use of herbs in a non-judgmental way, and should document the patient's use of these drugs. Finally, we must be more aware of the side effects and the potential drug interactions of these herbs, and advise our patients to avoid long term use of these drugs due to lack of information regarding the safety of these medicines.

   Valerian as a hypnotic for Hispanic patients.:Cultur Divers Ethnic Minor Psychol. 2000 Feb;6(1):84-92.Dominguez RA, Bravo-Valverde RL, Kaplowitz BR, Cott JM.Department of Psychiatry and Behavioral Sciences, University of Miami School of Medicine, Florida 33136, USA.[PMID: 10975170]

 Valerian is a botanical used for its sedative effects whose central nervous system activity is ascribed to multiple constituents. Twenty-three established outpatient symptomatic Hispanic volunteers receiving mental health services at a large urban hospital participated in this case study. All complained of insufficient sleep. They were asked to try a popular national brand of valerian ("Nature's Way", 470 mg valerian root) and completed sleep questionnaires at baseline and at the end of Weeks 1 and 2. They were instructed to take 1 capsule each night before retiring and were allowed to increase their dose to a maximum of 3 capsules after Week 1. Twenty patients completed the trial. On an ordinal scale of 1 (no effect), 3 (moderately helpful), and 5 (extremely helpful), 16 patients rated their insomnia as at least "moderately improved" at the end of Week 1. By Week 2, 16 still rated themselves at least "moderately improved," but 15 of them now described their response as either a 4 or a 5. Global improvement at Week 2 was significantly better than at Week 1 (Wilcoxon ranks test p = .005), perhaps reflecting a time-dependent or dose-response relationship. This case study suggests that valerian can be a supplement for improving insomnia in a symptomatic population.


  The influence of valerian treatment on "reaction time, alertness and concentration" in volunteers.:Pharmacopsychiatry. 1999 Nov;32(6):235-41.Kuhlmann J, Berger W, Podzuweit H, Schmidt U.Lichtwer Pharma AG, Berlin, Germany. jkuhlmann@csi.com[PMID: 10599933]

 A randomised, controlled, double-blind trial was performed on 102 male and female volunteers to determine whether reaction time, alertness and concentration might be impaired by treatment with a native valerian root extract (VRE). The effect was first examined the morning after a single evening dose of VRE (600 mg LI 156) vs. flunitrazepam (FNZ) (1 mg) and placebo (PL) (trial section A), and then after two weeks of evening administration of VRE (600 mg LI 156) vs. PL (trial section B). 99 volunteers were analysed in section A and 91 in section B. The primary criterion was the median of reaction time (MRT) measured with the Vienna Determination Test. Secondary criteria were cognitrones (alertness test), tracking test (two-handed co-ordination), sleep quality (VIS-A, Vis-M), further VDT parameters, and safety criteria. The single administration of LI 156 did not impair the reaction abilities, concentration and co-ordination. After 14 days of treatment, the equivalence of VRE and PL was proven by confirmative analysis concerning the improvement of MRT (p = 0.4481). Evaluation of the secondary criteria were consistent with the results of the primary criterion. It is concluded that neither single nor repeated evening administrations of 600 mg of VRE have a relevant negative impact on reaction time, alertness and concentration the morning after intake.

  Synaptosomal GABA release as influenced by valerian root extract--involvement of the GABA carrier.:Arch Int Pharmacodyn Ther. 1994 Mar-Apr;327(2):220-31.Santos MS, Ferreira F, Cunha AP, Carvalho AP, Ribeiro CF, Macedo T.Department of Zoology, Faculty of Medicine, University of Coimbra, Portugal.[PMID: 7979830]

 The effect of an aqueous extract obtained from the roots of Valeriana officinalis was investigated on the uptake and release of GABA in synaptosomes isolated from rat brain cortex. Aqueous extract of valerian inhibited the uptake and stimulated the release of [3H]GABA, either in the absence or in the presence of K+ depolarization. The release was Na(+)-dependent and independent of the presence of Ca2+ in the external medium. It is concluded that valerian extract releases [3H]GABA by reversal of the GABA carrier, which is Na(+)-dependent and Ca(2+)-independent. This increase in [3H]GABA release appears to be independent from Na(+)-K(+)-ATPase activity and the membrane potential.

   Effect of valerian on human sleep.:Psychopharmacology (Berl). 1985;87(4):406-9.Balderer G, Borbely AA. [PMID: 3936097]

 The effect of an aqueous extract of valerian root on sleep was studied in two groups of healthy, young subjects. One group (N = 10) slept at home, the other (N = 8) in the sleep laboratory. Sleep was evaluated on the basis of questionnaires, self-rating scales and night-time motor activity. In addition, polygraphic sleep recordings and spectral analysis of the sleep EEG was performed in the laboratory group. Under home conditions, both doses of valerian extract (450 and 900 mg) reduced perceived sleep latency and wake time after sleep onset. Night-time motor activity was enhanced in the middle third of the night and reduced in the last third. The data suggest a dose-dependent effect. In the sleep laboratory, where only the higher dose of valerian was tested, no significant differences from placebo were obtained. However, the direction of the changes in the subjective and objective measures of sleep latency and wake time after sleep onset, as well as in night-time motor activity, corresponded to that observed under home conditions. There was no evidence for a change in sleep stages and EEG spectra. The results indicate that the aqueous valerian extract exerts a mild hypnotic action.

   Aqueous extract of valerian root (Valeriana officinalis L.) improves sleep quality in man.:Pharmacol Biochem Behav. 1982 Jul;17(1):65-71.Leathwood PD, Chauffard F, Heck E, Munoz-Box R. [PMID: 7122669 ]

 The effect of an aqueous extract of valerian (Valeriana officinalis L.) root on subjectively rated sleep measures was studied on 128 people. Each person received 9 samples to test (3 containing placebo, 3 containing 400 mg valerian extract and 3 containing a proprietary over-the-counter valerian preparation). The samples, identified only by a code number, and presented in random order, were taken on non-consecutive nights. Valerian produced a significant decrease in subjectively evaluated sleep latency scores and a significant improvement in sleep quality: the latter was most notable among people who considered themselves poor or irregular sleepers, smokers, and people who thought they normally had long sleep latencies. Night awakenings, dream recall and somnolence the next morning were relatively unaffected by valerian. With the proprietary valerian-containing preparation, the only change was a significant increase in reports of feeling more sleepy than normal the next morning. Thus the questionnaire, simple to use and non-invasive, provides a sensitive means for detecting the effects of mild sedatives on different aspects of sleep in man. It also allows identification within the test population of the subgroups most affected.

   Preserved pharmacological activity of hepatocytes-treated extracts of valerian and St. John's wort.:Planta Med. 2005 Jul;71(7):592-8.Simmen U, Saladin C, Kaufmann P, Poddar M, Wallimann C, Schaffner W. Institute of Pharmaceutical Biology, University of Basel, Basel, Switzerland. usimmen@dtc.ch[PMID: 16041642]

 The two herbal extracts valerian (Valeriana officinalis L.) and St. John's wort (Hypericum perforatum L.) were studied for their metabolic changes upon incubation with freshly prepared rat hepatocytes and subsequently analysed phytochemically as well as pharmacologically in vitro. Quantitative HPLC analysis of valerian extracts revealed considerable metabolic activities with regard to sesquiterpenes and iridoids. The amount of acetoxyvalerenic acid decreased 9-fold, while that of hydroxyvalerenic acid correspondingly increased 9-fold due to O-deacetylation. The valepotriates didrovaltrate, isovaltrate and valtrate decreased 2-, 18- and 16-fold, respectively. However, the binding affinities of the incubated extracts to the benzodiazepine and picrotoxin binding site of the GABA (A) receptor were quite similar to those of the non-incubated extracts. Neither valerenic acids nor valepotriates exhibited any significant effect on the two binding sites when tested as single compounds. Therefore, either other constituents represent the active ones or multiple compounds are necessary for the observed inhibitory and allosteric effects at the GABA (A) receptor. Extracts of St. John's wort were less potently metabolised than valerian. The amount of pseudohypericin and the main flavonoids (hyperoside, rutin, isoquercitrin, quercitrin, quercetin and I3,II8-biapigenin) slightly decreased during the 4-h incubation period. Both the antagonist effect at the corticotropin-releasing factor (CRF) type 1 receptor and the binding inhibition at the 5-HT transporter were attenuated during the metabolic treatment. The reduced antagonist effect correlates with the decreasing amount of pseudohypericin known to be a CRF (1) receptor antagonist. In conclusion, the incubation of plant extracts with freshly prepared rat hepatocytes represents a useful approach to study the pharmacological action of metabolised plant extracts. The consistent pharmacological activity of both valerian and St. John's wort is concordant with the known clinical efficacy of pharmacological activities.


  Interspecific and intraspecific comparison of valepotrates contents in three Valeriana plants.:Zhong Yao Cai. 2002 Apr;25(4):237-8.Chen L, Qin L, Zheng H, Nian H, Guo C, Zhang C.School of Pharmacy, Second Military Medical University, Shanghai 200433.[PMID: 12583171]

 OBJECTIVE: To compare the contents of three valepotrates intraspecifically and intraspecifically in three medicinal Valeriana plants grown in different areas in China. METHODS: The method of RE-HPLC was adopted. RESULTS: The results showed that the contents of three valepotriates in Valeriana jatamansi Jones, V. officinalis L. and V. officinalis var. latifolia Miq. were different. Among them, that of Valeriana jatamansi Jones was the highest. The contents of three valepotrates in Valeriana jatamansi Jones varied significantly from different areas, samples collected from Longli of Guizhou province ranking the highest. The contents of three valepotriates in V. officnalis L. also varied significantly from different areas, samples from Liuba of Shaanxi province showing the highest. The results also showed that the contents of three valepotriates in underground part are all higher than that in aerial part. CONCLUSION: The interspecific and intraspecific differences of valepotriates in three Valeriana plans were obvious.

  Effect of valepotriates (valerian extract) in generalized anxiety disorder: a randomized placebo-controlled pilot study.:Phytother Res. 2002 Nov;16(7):650-4.Andreatini R, Sartori VA, Seabra ML, Leite JR. Departamento de Farmacologia, Laboratorio de Fsisiologia e Farmacologia do Sistema Nervoso Central, Universidade Federal do Parana, CP 19031, Curitiba, PR, Brazil, 81540-970. andreat@bio.ufpr.br[PMID: 12410546]

 The aim of the present study was to carry out a controlled pilot study on the putative anxiolytic effect of valepotriates. Thirty-six outpatients with generalized anxiety disorder (DSM III-R), after a 2-week wash-out, were randomized to one of the following three treatments for 4 weeks (n = 12 per group): valepotriates (mean daily dose: 81.3 mg), diazepam (mean daily dose: 6.5 mg), or placebo. A parallel, double-blind, flexible-dose, placebo-controlled design was employed. No significant difference was observed among the three groups at baseline or in the change from baseline on the Hamilton anxiety scale (HAM-A) or in the trait part of the state-trait anxiety inventory (STAI-trait). Moreover, the three groups presented a significant reduction in the total HAM-A scores. On the other hand, only the diazepam and valepotriates groups showed a significant reduction in the psychic factor of HAM-A. The diazepam group also presented a significant reduction of the STAI-trait. Although the principal analysis (HAM-A between group comparison) found negative results (probably due to the small sample size in each group), the preliminary data obtained in the present study suggest that the valepotriates may have a potential anxiolytic effect on the psychic symptoms of anxiety. However, since the number of subjects per group was very small, the present results must be viewed as preliminary. Thus, further studies addressing this issue are warranted.

   Quantitative determination of valepotriates from Valeriana native to South Brazil.:Planta Med. 2002 Jun;68(6):570-2.Silva AL, Rech SB, von Poser GL. [PMID: 12094311]

 Valtrate, DIA-valtrate, acevaltrate, 1-beta-acevaltrate and didrovaltrate have been quantitatively estimated by reversed-phase HPLC in the leaves, flowers, stems and roots of Valeriana glechomifolia Meyer, V. catharinensis Graebn., V. chamaedryfolia Cham. & Schltdl., V. eichleriana (C.A.Mull.) Graebn., V. polysthachya Smith, V. scandens L., V. eupatoria Sobral, V. salicariifolia Vahl and V. tajuvensis Sobral. All plants presented valepotriates being V. glechomifolia the richest one, followed by V. eupatoria, V. eichleriana and V. tajuvensis.


  Scientific References:

  1.Valeriana officinalis.Valerian and Medical Attributes.
  2.Research update of Valerian Root