Valepotriate

The thermo- and chemolabilc genuine valepotriates arc not present in the usual therapeutically used formulations (infusion, extract, fluid extract, tincture),... 

Valepotriates are detected by placing the chromatogram 0.3 mm from a TLC plate sprayed with cone, ammonia solution (sandwich configuration layer to layer), fastening with clips and heating to 110°C in a drying cupboard for 10 min [12]. 

Reagent for Epoxides e.g. trichothecene-mycotoxins [1 — 6] valepotriates [7,17] Olefins, acetylene derivatives [8] 4-Hydroxycumarin, anthraquinone [8] Alkylating agents [9-12] NOz... 

Note Trichothecenes and valepotriates only react when there is an epoxy group present in the molecule their detection limits are in the range 25—200 ng substance per chromatogram zone [1]. The detection limits for acetylene derivatives are 100— 800 ng substance per chromatogram zone, but not all give a positive reaction [8]. 

The content of valepotriates and sesquiterpenes varies across species of the Valeriana genus. For example, Valeriana officinalis has relatively high content of sesquiterpenes and low content of valepotriates, while Valeriana edulis has a high proportion of valepotriates and low content of sesquiterpenes (Lindahl and Lindwall 1989). 

For some time it was thought to be the valepotriates, but this was later discredited due to their unstable nature. 

Valerian extracts show sedative and anxiolytic effects. Whereas passionflower and chamomile have relatively specific anxiolytic effects, valerian shows more general sedative effects, but all effects occur in a dose-dependent manner (Della Logia et al. 1981 Leuschner et al. 1993). The sedative effects of valerian extract are moderate when compared to diazepam and the neuroleptic chlorpromazine (Leuschner et al. 1993). However, valepotriates reverse the anxiogenic effects of diazepam withdrawal in rats in the elevated plus maze. This effect is dose dependent, effective at 12 mg/kg but not 6 mg/kg. Interestingly, the fragrant valerian compound bornyl acetate has sedative effects in mice, but only when inhaled (Buchbauer et al. 1992). 

The active agent for this effect is uncertain, but catnip has in it several terpenes, including nepetalactone. One terpene, c/s-trans-nepetalactone was hypothesized to be responsib e for the sedative effect based on its structural similarity to valepotriates, the depressant principles from valerian. 

Chavadej S, Becker H, Weberling F. (1985). Further investigations of valepotriates in the Valerianaceae. Pharm Weekbl Sci. 7(4) 167-8. 

Dunaev W, Trzhetsinskii SD, Tishkin VS, Fursa NS, Linenko VI. (1987). [Biological activity of the sum of the valepotriates isolated from Valeriana alliariifolia]. Farmakol Tol ikol. 50(6) 33-37. 

This herb has been part of folk medicine since pre-Christian times (247). It has been primarily used as a sedative and for the treatment of epilepsy. Consistent with this use, this herb reportedly can increase synaptic concentrations of GABA (248). GABA has also been isolated from Valeria and extracts of Valeria have been reported to bind to GABA receptors in rat brain. Although Valeria has been reported to be active in rodent models of depression, there have been no efficacy trials in humans. The potential adverse effects of Valeria include the sensation of strangeness ( 247) and several cases of liver damage (e.g., central lobular necrosis) (249). Mutagenicity in bacteria has been reported and attributed to unstable, water-insoluble valepotriates ( 238). As a result of these reports, many, but not all, commercial preparations of Valeria use water-soluble extracts standardized for their content of valeric acid. 

N.A. Galium aparine L. Iridoid valepotriates, polyphenolic acids, anthraquinones, tannins.99107 For vitamin C deficiency. 

N.A. Valeriana officinalis L. Essential oil, valtrate, valepotriates, bomyl esters, alkaloids, isovaltrate.99-100 Sedative for nervous disorders, antispasmodic. 

Tropane alkaloids Turmerone Tyramine Tyrosine Umbelliferone Uric acid Ursolic acid Urushiol Valepotriates Valerianic acid Valeric acid Valtrate Vanillic acid... 

Main actives Valepotriates (0.5-2.0%), volatile oil (0.2-1.0%) and valeric acid (0.1-0.9%). Benefits Valerian has been used as a daytime sedative to reduce anxiety and stress and it has been demonstrated to reduce the time it takes to fall asleep. Valerian root extracts and volatile oils are used as components in the flavour industry, especially in alcoholic beverages such as beers and liqueurs and in soft drinks such as root beers. They have also been used in tobacco flavours. 

Valerian is used in the treatment of insomnia and stress and anxiety. The important active compounds of valerian are the valepotriates (iridoid molecules) and valeric acid. These compounds are found exclusively in valerian. Originally, it was thought that just the valepotriates were responsible for valerian s sedative effects but, recently, an aqueous extract of valerian has also been shown to have a sedative effect. As the valepotriates are not soluble in water, it was concluded that valeric acid also possesses sedative action and is the chemical factor responsible for the sedative effect noted in human clinical trials with aqueous extracts of valerian (Murray, 1995). Valerian inhibits the uptake of GABA and enhances the release of GABA. 

Note Valerian consists of the dried rhizome and roots of Valeriana officinalis Linne (Fam. Valerianaceae). It has been employed as an antianxiety agent and sleep aid for more than 1000 years. The drug contains from 0.3 to 0.7% of an unpleasant-smelling volatile oil containing bornyl acetate and the sesquiterpenoids, valerenic acid, and acetoxyvalerenolic acid. Also present is a mixture of lipophilic iridoid principles known as valepotriates. These bicyclic monoterpenoids are quite unstable and occur only in the fresh plant or in material dried at temperatures under 40°C. Although the specific active principals of valerian have not been determined, it is possible that a combination of the sesquiterpenoids and the valepotriates may be involved. The drug may be administered as a tea prepared from 2 to 3 g of the dried herb or equivalent amounts of a tincture or extract may be employed. 

The structure for valerosidate is incorrect in the previous Report (Vol. 5, p. 17). A new valepotriate has been isolated from Valeriana officinalis and shown spectroscopically to be 7-epideacetylisovaltrate (103) 193 it is also shown to be related to didrovaltrate (104) stereochemically, but in view of the recently reported absolute configuration of didrovaltrate (104)192 this assignment must be questioned. The occurrence of iridoids in the Argentine ant Iridomyrmex humilis has been re-investigated.194... 

The full paper concerning galiridoside, isolated from Galeopsis tetrahit (see Vol. 1, p. 18), has appeared. A thorough study of ca. 40 species of various Valerianaceae has shown that the valepotriates, the main component of which is... 

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