Role of hyperforin in the antidepressant-like activity of Hypericum perforatum extracts

Abstract

These results support the view that hyperforin plays a key role in the antidepressant-like activity of Hypericum p. However, brain concentrations after effective doses are probably far from those active in vitro on the neurotransmitter mechanisms so far investigated.

Hyperforin-Containing Extracts of St John's Wort Fail to Alter Gene Transcription in Brain Areas Involved in HPA Axis Control in a Long-Term Treatment Regimen in Rats

“…Furthermore, the dosage used in the present study proved to be active when tested in the forced swimming test (see Materials and methods). However, recently Cervo et al (2002) showed that hyperforinFused as a hyperforindicyclohexylammonium saltFwas active in several behavioral models, but that the ester as well as the free drug could not be detected in the brain probably because of its poor passage through the blood-brain barrier. The authors speculate that the antidepressant-like effect of hyperforin might be mediated by a still unknown metabolite of this compound.…”

Hyperforin Inhibits Cancer Invasion and Metastasis

“…injection, when the hematic peak is reached (25), and was always lower than the in vitro cytotoxic threshold for the injected cells (C-26), with concentrations Ͻ1.2 …”

“…After electrophoresis, the gels were washed twice for 15 minutes with 2.5% Triton X-100, incubated overnight at 37°C in Tris buffer [50 mmol/L Tris-HCl, 200 mmol/L NaCl, and 10 mmol/L CaCl 2 (pH 7.4)], stained 30 minutes with 30% For gelatinase inhibition assays, Hyp-DCHA was freshly solubilized in methanol and diluted (1, 10, and 100 mol/L) in the Tris buffer used for developing separate slices of gelatinase zymograms, which were incubated as above. (25), and five animals received injections of vehicle only; three untreated mice were used as control. After 15 days, the mice were weighed, anesthetized, heparinized, and exsanguinated via the femoral artery; the heart and lungs were removed en bloc, the lungs were dissected away from the external vasculature and bronchi, weighed, sectioned parasaggitally superior to inferior, and the specimens were fixed in buffered 4% paraformaldehyde for morphological studies.…”

“…25), and the plasma was mixed with 2 volumes of ethanol and centrifuged; the supernatant was then vacuum-dried and solubilized in methanol. Hyp was identified and quantified by high-performance liquid chromatography, using a Chromquest P4000 pump (Thermoseparation, San Jose, CA) equipped with a photodiode array detector (UV6000), and a RP-18 column Vydac (5 m) eluted with a water-methanol-acetonitrile-phosphoric acid mobile-phase system, according to Brolis et al (31).…”

“…1; refs. 23,24) is a convenient storage form of the natural product already used in studies of antidepressant activity in rats (25) and, for this reason, was chosen for our investigation.…”