Skip to main content

Effects of Valeriana Officinalis Extracts on [3H]Flunitrazepam Binding, Synaptosomal [3H]GABA Uptake, and Hippocampal [3H]GABA Release

Neurochemical Research volume 24, pages 1373–1378 (1999)Cite this article

We’re sorry, something doesn't seem to be working properly.

Please try refreshing the page. If that doesn't work, please contact support so we can address the problem.

Abstract

Extracts of Valeriana officinalis have been used in folkloric medicine for its sedative, hypnotic, tranquilizer and anticonvulsant effects, and may interact with γ-aminobutyric acid (GABA) and/or benzodiazepine sites. At low concentrations, valerian extracts enhance [3H]flunitrazepam binding (EC50 4.13 × 10−10 mg/ml). However, this increased [3H]flunitrazepam binding is replaced by an inhibition at higher concentrations (IC50 of 4.82 × 10−1 mg/ml). These results are consistent with the presence of at least two different biological activities interacting with [3H]flunitrazepam binding sites. Valerian extracts also potentiate K+ or veratridine-stimulated release of radioactivity from hippocampal slices preloaded with [3H]GABA. Finally, inhibition of synaptosomal [3H]GABA uptake by valerian extracts also displays a biphasic interaction with guvacine. The results confirm that valerian extracts have effects on GABAA receptors, but can also interact at other presynaptic components of GABAergic neurons.

This is a preview of subscription content, access via your institution.

Access options

Buy single article

Instant access to the full article PDF.

USD 39.95

Price includes VAT (USA)
Tax calculation will be finalised during checkout.

REFERENCES

  1. Petkov, V., Manolov, P., Marekov, N.L., Popov, S.S., and Khandzhieva, N.B.1974. Pharmacological studies on a mixture of valepotriates isolated from Valeriana officinalis. Dokl. Bolg. Akad. Nauk. 27:1007–1010.

    Google Scholar 

  2. Cott, J.1995. Medicinal plants and dietary supplements: sources for innovative treatments of adjuncts. Psychopharmacol. Bull. 31:137–137

    Google Scholar 

  3. Granicher, F., Christen, P.,and Kapetanidis, I.1995. Essential oils from normal and hairy roots of Valeriana officinalis varsambucifolia. Phytochemistry 40:1421–1424.

    Google Scholar 

  4. Haas, L.F.1996. Neurological stamp Valeriana officinalis. J.Neurol. Neurosurg. Psychiatry 60:255.

    Google Scholar 

  5. Petkov, V.,and Manolov, P.1975.To the pharmacology of iridoids. Agressologie 16:25–30.

    Google Scholar 

  6. Leuschner, J., Muller, J.,and Rudmann, M.1993. Characterization of the central nervous depressant activity of a commercially available valerian root extract.Arzneim. Forsch./Drug. Res. 43:638–641.

    Google Scholar 

  7. Andreatini, R.,and Leite, J.R.1994. Effect of valepotriates on the behavior of rats in the elevated plus-maze during diazepanwithdrawal. Eur. J. Pharmacol. 260:233–235.

    Google Scholar 

  8. Hendriks, H., Bos, R., Allersma, D.P., Malingre, T.H.M., and Koster, A.S.J.1981. Pharmacological screening of valerenal and some other components of essential oil of Valerianaofficinalis. Planta Med. 42:62–68.

    Google Scholar 

  9. Hendriks, H., Bos, R., Woerdenbag, H.J., and A. Sj. Koster,1985. Central nervous depressant activity of valerenic acid in the mouse. Planta Med.1:28–31.

    Google Scholar 

  10. Leathwood, P.D.,and Chauffard, F.1985. Aqueous extract of valerian reduces latency to fall asleep in man. Planta Med. 2:144–148.

    Google Scholar 

  11. Santos, M.S., Ferreira, F., Cunha, A.P., Carvalho, A.P., and Macedo, T.1994. Aqueous extract of valerian influences the transport of GABA in synaptosomes. Planta Med. 60:278–279.

    Google Scholar 

  12. Santos, M.S., Ferreira, F., Cunha, A.P., Carvalho, A.P., Ribeiro, C.F.,and Macedo, T.1994. Synaptosomal GABA release as influenced by valerian root extract-involvement of theGABA carrier. Arch. Int. Pharmacodyn. 327:220–231

    Google Scholar 

  13. Santos, M.S., Ferreira, F., Faro, C., Pires, E., Carvalho, A.P.,and A.P.,Cunha,1994. The amount of GABA present in aqueous extracts of valerian is sufficient to account for [3 H ] GABA release in synaptosomes. Planta Med. 60:475–476.

    Google Scholar 

  14. Cavadas, C., Araujo, I., Cotrim, M.D., Amaral, T., Cunha, A.P., Macedo, T.,and Ribeiro, C.F.1995. In vitro study on the interaction of Valeriana Officinalis L.extracts and their amino acidson GABAA receptor in rat brain. Arzneim-Forsch /Drug Res. 45:753–755.

    Google Scholar 

  15. Rosenstein, J.M.1996. Permeability of the blood-brain barrier to protein and [3 H ]GABA in intraparenchymal fetal CNS tissuegrafts. Exp.Neurol. 142:66–79.

    Google Scholar 

  16. Chiu, T.M., Dryden, D.M., and H.C. Rosenberg.,1982. Kinetics of [3 H ]flunitrazepam binding to membrane bound benzo-diazepine receptors. Mol. Pharmacol. 21:57–65.

    Google Scholar 

  17. Ortiz, J.G., Negron, A., Thomas, A., Heimer, H., Moreira, J.A., Cordero, M.L., Aranda, J.,and Bruno, M.S.1991. GABAergic neurotransmission in the C57BL/10 sps/sps mouse mutant: a model of absence of seizures. Exp. Neurol. 113:338–343.

    Google Scholar 

  18. Cordero, M.L., Ortiz, J., Santiago, G., Negron, A.,and Moreira, J.A.1994. Altered GABAergic and glutamatergic transmission in audiogeitic seizure-susceptible mice. Mol. Neurobiol.9:253–258.

    Google Scholar 

  19. Bradford, M.M.1976. A rapid and sensitive method for the quantification of microgram quantities of protein utilizing the principle of protein-dye binding. Anal,Biochem.72:248–254.

    Google Scholar 

  20. Lindah, O.,and Lindwall, L.1989. Double blind study of a valerian preparation. Pharmacol. Biochem. Behavior 32:1065–1066.

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Department of Pharmacology and Toxicology, University of Puerto Rico School of Medicine, Puerto Rico

    José G. Ortiz & Jennifer Nieves-Natal

  2. Center for Molecular and Behavioral Neuroscience, Universidad Central del Caribe, Bayamón, Puerto Rico

    Pedro Chavez

  3. School of Pharmacy, PO Box 365067, San Juan, Puerto Rico, 00936-5067

    José G. Ortiz & Jennifer Nieves-Natal

  4. Dept. of Medicinal Chemistry and Pharmacognosy, Midwestern University-Glendale College of Pharmacy, 19555 Norh 59th Ave, Glendale, AZ, 85308

    Pedro Chavez

Authors
  1. José G. Ortiz
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Jennifer Nieves-Natal
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Pedro Chavez
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and Permissions

About this article

Cite this article

Ortiz, J.G., Nieves-Natal, J. & Chavez, P. Effects of Valeriana Officinalis Extracts on [3H]Flunitrazepam Binding, Synaptosomal [3H]GABA Uptake, and Hippocampal [3H]GABA Release. Neurochem Res 24, 1373–1378 (1999). https://doi.org/10.1023/A:1022576405534

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1022576405534

  • Valeriana
  • [3H]flunitrazepam
  • [3H]GABA uptake
  • [3H]GABA release