Hyperforin modifies neuronal membrane properties in vivo.
Hyperforin, the major active constituent of St. John Wort (SJW) extract, affects several neurotransmitter systems in the brain putatively by modulation of the physical state of neuronal membranes. Accordingly, we tested the effects of SJW extract and of hyperforin on the properties of murine brain membrane fluidity. Oral administration of SJW extract and of hyperforin sodium salt results in significant hyperforin brain levels. Treatment of mice with hyperforin leads to decreased annular- and bulk fluidity and increased acyl-chain flexibility of brain membranes. All hyperforin related changes of membrane properties were significantly correlated with the corresponding hyperforin brain levels. Our data emphasises a membrane interaction of hyperforin that possibly contributes to its pharmacological effects.
Eckert
Gunter P
GP
Institute of Pharmacology, J.W. Goethe-University, Biocenter N260, Marie-Curie-Strasse 9, 60439 Frankfurt, Germany. g.p.eckert@em.uni-frankfurt.de
Keller
Jan-Henning
JH
Jourdan
Claudia
C
Karas
Michael
M
Volmer
Dietrich A
DA
Schubert-Zsilavecz
Manfred
M
Müller
Walter E
WE
D000284:Administration, Oral; D000818:Animals; D016880:Anisotropy; D001921:Brain / Q000166:cytology / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D001643:Bridged Bicyclo Compounds; D002462:Cell Membrane / Q000187:drug effects* / Q000378:metabolism; D002853:Chromatography, Liquid / Q000379:methods; D004161:Diphenylhexatriene; D004305:Dose-Response Relationship, Drug; D005260:Female; D020902:Hypericum / Q000737:chemistry*; D008560:Membrane Fluidity / Q000187:drug effects; D051379:Mice; D009474:Neurons / Q000166:cytology / Q000187:drug effects*; D010696:Phloroglucinol / Q000031:analogs & derivatives; D010936:Plant Extracts / Q000494:pharmacology; D011721:Pyrenes; D013729:Terpenes / Q000378:metabolism / Q000494:pharmacology*
D001643:Bridged Bicyclo Compounds; D010936:Plant Extracts; D011721:Pyrenes; D013729:Terpenes; D004161:Diphenylhexatriene; C030984:pyrene; D010696:Phloroglucinol; C001654:hyperforin