Isovaleramide, an anticonvulsant molecule isolated from Valeriana pavonii
Keywords:
valerian, medicine, traditional, valproic acid, anticonvulsants, epilepsy, tonic-clonic
Abstract
Introduction. Fractioning of an extract of Valeriana pavonii, a native species used in Colombian folk medicine as tranquilizer, led to the isolation and identification of isovaleramide, one of the active constituents responsible for its central nervous system activity as anticonvulsant.Objective. Description of the isolation and identification of isovaleramide, an active principle on central nervous system from Valeriana pavonii.
Materials and methods. The purification of isovaleramide was carried out by chromatographic techniques. Its structural elucidation was determined by nuclear magnetic resonance and mass spectrometry. Maximal electroshock seizure was used as in vivo pharmacological test, additionally in vitro GABA-A/BDZ-binding site studies were performed.
Results. Isovaleramide was isolated from the most active fraction of Valeriana pavonii. This compound, at 100 mg/Kg, p.o, evidenced a 90% index protection against the maximal electroshock seizure in mice (MES), comparable to the reference agent: sodium phenytoin (20 mg/kg, p.o, 100%). In the in vitro assay, isovaleramide (300 μM) exhibited a 42% of inhibition of the binding of 3H-FNZ to its sites.
Conclusion. Isovaleramide is one of the active anticonvulsant constituents of Valeriana pavonii, for the first time reported in this species. These results support the traditional use of Valeriana pavonii and its interest as a therapeutic source.
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References
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2. Houghton PJ. The scientific basis for the reputed activity of Valerian. J Pharm Pharmacol.1999;51:505-12.
3. Fernández S, Wasowski C, Paladini AC, Marder M. Sedative and sleep-enhancing properties of linarin, a flavonoid-isolated from Valeriana officinalis. Pharmacol Biochem Behav. 2004;77:399-04.
4. García H. Flora medicinal de Colombia, Botánica Médica. Instituto de Ciencias Naturales, Universidad Nacional de Colombia, Bogotá: Mundo Editores; 1992. Tomo 3. p. 254-62.
5. Arévalo D, Martínez C, Rincón J, Guerrero MF. Fracción alcaloidal obtenida de Valeriana pavonii Poepp con actividad anticonvulsivante. Rev Colomb Ciencias Quím Farm. 2006;35:168-76.
6. Célis CT, Rincón J, Guerrero MF. Actividad farmacológica sobre el sistema nervioso central del extracto etanólico y de la fracción alcaloidal de Valeriana pavonii. Rev Colomb Ciencias Quím Farm. 2007;36:11-22.
7. Pradilla G, Vesga B, León-Sarmiento F, Grupo Geneco. Estudio neuroepidemiológico nacional (EPINEURO) colombiano. Rev Panam Salud Pública. 2003;14:104-11.
8. Burneo J, Tellez-Zenteno J, Wiebe S. Understanding the burden of epilepsy in Latin America: a systematic review of its prevalence and incidence. Epilepsy Res. 2005; 66:63-74.
9. Löscher W. Current status and future directions in the pharmacotherapy of epilepsy. Trends Pharmacol Sci. 2002;23:113-8.
10. Schachter SC. Botanicals and herbs: a traditional approach to treating epilepsy. Neurotherapeutics. 2009;6:415-20.
11. Giardina WJ. Models of epilepsy: Electroshock and chemical induced convulsions in the mouse. En: Current Protocols in Pharmacology. New York: John Wiley & Sons; 2000. Volume 5. p. 1-22.
12. Wolf P. Basic principles of the ILAE syndrome classification. Epilepsy Res. 2006;70(Suppl.1):S20-6.
13. Swinyard EA, Woodhead JH. Experimental detection, quantification, and evaluation of anticonvulsants. En: Woodbury DM, Penry JK, Pippenger CE. Antiepileptic Drugs. 2nd edition. New York: Raven Press; 1982. p. 111-26.
14. Bialer M, Johannessenb SI, Kupferbergc HJ, Levyd RH, Perucca E, Tomson T. Progress report on new antiepileptic drugs: a summary of the seventh EILAT conference (EILAT VII). Epilepsy Res. 2004;61:1-48.
15. Pollard JR, French J. Antiepileptic drugs in development. Lancet Neurol. 2006;5:1064-7.
16. America´s Pharmaceutical Research Companies. Pharmaceutical companies researching and developing more than 500 medicines for neurological disorders. En: Report, medicines in development for neurological disorders. Washington, D.C.: Pharma, New Medicines, New Hope; 2008. p. 37.
17. Bialer M, Yagen B. Valproic acid: second generation. Neurotherapeutics. 2007;4:130-7.
18. Isoherranen N, Yagen B, Bialer M. New CNS-active drugs which are second-generation valproic acid: can they lead to the development of a magic bullet? Curr Opin Neurol. 2003;16:203-11.
19. Nau H, Siemens H. Differentiation between valproate-induced antiepileptic effect, teratogenicity and hepatotoxicity. Pharm Weekbl Sci. 1992;14:101-5.
20. Bucková A, Grznár K, Haladová M, Eisenreichová E. Active principles in Valeriana officinalis L. Cesk Farm. 1977;26:308-9.
How to Cite
1.
Giraldo SE, Rincón J, Puebla P, Marder M, Wasowski C, Vergel N, et al. Isovaleramide, an anticonvulsant molecule isolated from Valeriana pavonii. biomedica [Internet]. 2010 Aug. 4 [cited 2024 May 18];30(2):245-50. Available from: https://revistabiomedica.org/index.php/biomedica/article/view/187
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