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Pharmacopsychiatry 2001; 34(Suppl1): 137-142
DOI: 10.1055/s-2001-15475
Original Paper
Georg Thieme Verlag Stuttgart · New York

Neurochemical Studies with St. John's Wort In Vitro

U. Simmen1 , J. Higelin2 , K. Berger-Büter1 , W. Schaffner1 , K. Lundstrom2
  • 1Institute of Pharmaceutical Biology, University of Basel, Witterswil, Switzerland
  • 2F. Hoffmann-La Roche, Research Laboratories, Basel, Switzerland
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Publication History

Publication Date:
31 December 2001 (online)

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The effect of extracts and constituents of St. John's wort, Hypericum perforatum, at various CNS receptors were studied by radioligand binding techniques in order to determine a profile of pharmacological activity in vitro. Binding inhibition was examined for the G-protein coupled opioid, serotonin (5-HT), histamine, neurokinin and corticotropin releasing factor (CRF) receptors, for the steroid estrogen-α receptor and for the ligand-gated ionchannel GABAA receptor. Hypericin showed the most potent binding inhibiton of all tested constituents to human CRF1 receptor with an IC50 value of 300 nM. Preliminary GTPγ35S binding studies to CRF1 coupled G-protein indicated an antagonistic action for hypericin. The acylphloroglucinole hyperforin failed to inhibit 125I-astressin binding to hCRF1 receptor up to 10 µM. Hyperforin inhibited binding to opioid and serotonin (5-HT) receptors at IC50 values between 0.4 and 3 µM, while hypericin and pseudohypericin inhibited with weaker potency. The biflavonoid I3,II8-biapigenin inhibited 3H-estradiol binding to the estrogen-α receptor with an IC50 value of 1 µM. The inhibition of 3H-muscimol binding to the GABAA receptor is likely to be exclusively due to GABA present in the extract. We therefore hypothesize that additive or synergistic actions of several ditsinct compounds may be responsible for the beneficial antidepressant effect of St. John's wort.

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Dr. Urs Simmen

Institute of Pharmaceutical Biology
University of Basel


Benkenstraße 254
4108 Witterswil
Switzerland