Correlation of hyperforin content of Hypericum perforatum (St John's Wort) extracts with their effects on alcohol...

Extracts of the herb St John's Wort have been shown to reduce alcohol intake in alcohol-preferring rats, but it is not known which of the constituent(s) are responsible for this effect. In this study, the effect of a crude methanolic extract of Hypericum perforatum (negligible hyperforin content) on alcohol drinking in C57BL/6J alcohol-preferring mice was compared with that of a hyperforin-rich extract (45% hyperforin) prepared by extracting the herb with supercritical carbon dioxide. The dose of the hyperforin-rich extract required to significantly reduce 10% ethanol intake (5 mg/kg) was 125-fold less than that required for the crude extract (625 mg/kg), and was comparable to the dose of fluoxetine (10 mg/kg) required to produce a similar effect. None of these agents significantly affected water intake. These results suggest that the effects of H. perforatum extracts on alcohol drinking behaviour are due to the hyperforin content of the herb rather than to other, more polar constituents. Hyperforin is an unstable compound and this study also highlights the effect of different methods of extract preparation on hyperforin content.