title: Hyperforin: To Be or Not to Be an Activator of TRPC(6).
abstract: Meantime, it is well accepted that hyperforin, the chemical instable phloroglucinol derivative of Hypericum perforatum, St. John's wort, is the pharmacophore of St. John's wort extracts. With the decline of this scientific discussion, another controversial aspect has been arisen, the question regarding the underlying mechanism leading to the pharmacological profile of the plant extract used in therapy of depression. We will summarize the different concepts described for hyperforin's antidepressive activity. Starting with unspecific protein-independent mechanisms due to changes in pH, we will summarize data of protein-based concepts beginning with concepts based on involvement of a variety of proteins and will finally present concepts based on the modulation of a single protein.
authors.affiliation: Department of Molecular and Clinical Pharmacy, Friedrich-Alexander University Erlangen/Nuremberg, Cauerstr. 4, 91058, Erlangen, Germany. kristina.leuner@fau.de.
authors.forename: Kristina
authors.initials: K
authors.lastname: Friedland
authors.affiliation: Institute of Pharmacology and Toxicology and Interfaculty Centre for Pharmacogenomics and Drug Research, Eberhard Karls Universität, Wilhelmstr. 56, 72074, Tübingen, Germany. christian.harteneck@uni-tuebingen.de.
authors.forename: Christian
authors.initials: C
authors.lastname: Harteneck
mesh_terms: D000818:Animals; D065693:Cytochrome P-450 Enzyme Inducers / Q000494:pharmacology; D004355:Drug Stability; D006801:Humans; D010696:Phloroglucinol / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D050052:TRPC Cation Channels / Q000187:drug effects* / Q000502:physiology; D000074287:TRPC6 Cation Channel; D013729:Terpenes / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D065693:Cytochrome P-450 Enzyme Inducers; D050052:TRPC Cation Channels; D000074287:TRPC6 Cation Channel; C117032:TRPC6 protein, human; D013729:Terpenes; D010696:Phloroglucinol; C001654:hyperforin
keywords: Calcium homeostasis; Depression; Hyperforin; Ion channel; Protonophore; St. John's wort; TRP channel