[Analysis of the essential oils of brilliant valerian and tall valerian by gas-liquid chromatography].
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The psychotropic effects of "Hokkai-Kisso", i.e. roots of Japanese valerian, were compared with those of diazepam and imipramine. Both 30% EtOH extract of valerian root (11.2 g/kg) and diazepam (3 mg/kg) significantly prolonged hexobarbital-induced sleep in mice. Spontaneous ambulation and rearing during an open field test were significantly decreased by valerian extract (11.2 g/kg), but kessyl glycol diacetate (KGD, 400 mg/kg) and diazepam (3 mg/kg) significantly increased ambulation. Diazepam (10 mg/kg) significantly decreased approach-avoidance conflict in mice in a water-lick conflict test, but valerian extract and KGD did not. By contrast, valerian extract (4.1 g/kg) and imipramine (20 mg/kg) significantly inhibited immobility induced by a forced swimming test in rats, but did not increase spontaneous motor activity during an open field test just before the forced swimming test. In addition, valerian extract and imipramine significantly reversed reserpine-induced hypothermia in mice. These results indicate that valerian extract acts on the central nervous system and may be an antidepressant.
Peripheral plasma from four postmenopausal women was analysed for oestrone (E1) and oestradiol (E2) during 48 hours after oral intake of a single tablet of 2 mg Progynon (oestradiol valerianate). Plasma levels of E1, E2 and d-norgestrel were analysed daily in five postmenopausal women during treatment with tablet Cyclabil (oestradiol valerianate in a biphasic preparation with dl-norgestrel) in 21 dyas. Radioimmunoassay (RIA) was utilized for the quantifications. Pretreatment plasma levels of E1 were about 20 pg/ml and E2 about 12 pg/ml. It is concluded that oestradiol valerianate is rapidly absorbed from the gastrointestinal tract and converted to E1. This is reflected by plasma levels of E1 considerably higher than those of E2. The E2 levels found were in the range of those in ovulatory women, while the oestrone levels were higher.
The aromatherapeutical use of commercial valerian root oil (Chinese origin) and of pure fragrance compounds--borneol, isoborneol, bornyl acetate (main constituent of the proved valerian root oil) and isobornyl acetate--as potentially drugs with sedative effects after inhalation was investigated in an animal experiment (mice). In additional analyses the mice were treated i.p. by caffeine and distinct sedative effects were observed only by inhalation of the cited substances.
Valerian root contains two substances of special pharmacological interest--valepotriates and sesquiterpenes. The former, which has been used for standardization of the drug, is cytotoxic. The latter has no such effect. Both have sedative effects. A double blind test has been carried out on a preparation (VALERINA NATT) containing primarily sesquiterpenes. When compared with placebo it showed a good and significant effect on poor sleep (p less than 0.001). Forty-four percent reported perfect sleep and 89% reported improved sleep from the preparation. No side effects were observed.
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A comprehensive review of the constituents of the Valerianaceae is presented with particular reference to the sedative activity of extracts from various constituent species. The sedative activity can be ascribed to the valepotriates present and to a lesser extent to the sesquiterpene constituents of the volatile oils. Recent research into the toxicology of the valepotriates is also considered.
The valepotriates, a group of chemically unstable iridoid triesters possessing sedative activity, contain various ester groups at the C-1, C-7, and C-11 positions. Using the selective INEPT NMR technique and employing a suitable polarization delay for long-range coupling, it was possible to achieve the assignment and location of the ester groups directly, without ambiguity, and without chemical modification. Six valepotriates isolated from Valmane tablets served as examples to demonstrate the utility of this NMR technique. During the course of this work, the "acevaltrate" fraction was shown to be a mixture of 1-alpha-acevaltrate (3) and 7-beta-acevaltrate (4), the structures of valtrate (1) and didrovaltrate (2) were confirmed directly, and two new valepotriates, 5a and 5b, were obtained as an inseparable mixture and characterized.
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