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Pharmacopsychiatry 2001; 34(Suppl1): 74-82
DOI: 10.1055/s-2001-15510
Original Paper
© Georg Thieme Verlag Stuttgart · New York

Modulation of Ion Channels in Rat Neurons by the Constituents of Hypericum Perforatum

O. Krishtal1 , N. Lozovaya1 , A. Fisunov1 , T. Tsintsadze1 , Y. Pankratov1 , M. Kopanitsa1 , S. S. Chatterjee2
  • 1Bogomoletz Institute of Physiology, Kiev, Ukraine
  • 2Dr. Willmar Schwabe GmbH & Co., Karlsruhe, Germany
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Publication History

Publication Date:
31 December 2001 (online)

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Despite almost forty years of widespread use of antidepressant drugs, their mode of action is still unknown. Hyperforin, a phloroglucinol derivative, is a major pharmacologically and therapeutically active constituent of Hypericum perforatum extract that is widely used as an herbal antidepressant drug. However, the mechanism or mechanisms of action of these naturally abundant, non-toxic extracts remain unclear. Enzymatically isolated patch-clamped rat central and peripheral neurons exposed to rapid changes in the composition of external medium (concentration clamp) were used in our experiments to investigate the modulation of the various voltage- and ligand-gated channels by hyperforin, as well as by other constituents of Hypericum perforatum. At nanomolar concentrations, hyperforin induced significant inhibition of various ion channels. In the case of P-type Ca2+ channels, we established that hyperforin acts via interaction with calmodulin or through calmodulin-activated pathways involving at least one second messenger. The results presented here indicate that multiple mechanisms and extract constituents may be involved in the antidepressant action of Hypericum extracts, and that they could also possess neuroprotective and analgesic effects.

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Dr. O. Krishtal,MD 

Department of Cellular Membranology
Bogomoletz Institute of Physiology

4 Bogomoletz Street

Kiev 01024

Ukraine

Fax: +380 44 2562590

Email: krishtal@serv.biph.kiev.ua