Metabolism of hyperforin, the active constituent of St. John's wort, in human liver microsomes.

Article Details

Citation

Hokkanen J, Tolonen A, Mattila S, Turpeinen M

Metabolism of hyperforin, the active constituent of St. John's wort, in human liver microsomes.

Eur J Pharm Sci. 2011 Feb 14;42(3):273-84. doi: 10.1016/j.ejps.2010.12.002. Epub 2010 Dec 17.

PubMed ID
21168483 [ View in PubMed
]
Abstract

The metabolism of hyperforin, one of the pharmacologically most active components of St. John's wort (Hypericum perforatum), was characterized in vitro using human liver microsomes and recombinant heterologously expressed P450 enzymes. A total of 57 hyperforin metabolites were detected. Of those, six were identified as monohydroxylations (M1-M6), while the others were formed via two or more hydroxylation reactions, via dehydrogenation, or by combinations of these reactions. A combined approach of cDNA-expressed recombinant CYPs, CYP-selective chemical inhibitors and correlation with CYP-specific marker activities indicated a central role of the CYP2C and CYP3A families in the metabolism of hyperforin. In addition, hyperforin was found to inhibit CYP2D6 and CYP3A4 model activities quite potently.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
St. John's WortCytochrome P450 2C19ProteinHumans
No
Substrate
Inducer
Details
St. John's WortCytochrome P450 2D6ProteinHumans
No
Inhibitor
Details
St. John's WortCytochrome P450 3A4ProteinHumans
Unknown
Substrate
Inducer
Activator
Details