Hyperforin represents the neurotransmitter reuptake inhibiting constituent of hypericum extract.
Hydroalcoholic hypericum extract inhibits the synaptosomal uptake of serotonin, norepinephrine, and dopamine with about similar affinities and leads to a significant down-regulation of cortical beta-adrenoceptors and 5-HT2-receptors after subchronic treatment of rats. While neither hypericine nor kaempferol did show any reuptake inhibiting properties, hyperforin was identified as the unspecific reuptake inhibitor of hypericum extracts with half-maximal inhibitory concentrations for the three synaptosomal uptake systems mentioned above between 80 and 200 nmol/l. Moreover, a hyperforin-enriched (38%) CO2 extract also leads to a significant beta-receptor down-regulation after subchronic treatment. The data suggest hyperforin as the active principle of hypericum extracts in biochemical models of antidepressant activity.
Department of Pharmacology, Biocenter University of Frankfurt, Germany.
W E
WE
Müller
A
A
Singer
M
M
Wonnemann
U
U
Hafner
M
M
Rolli
C
C
Schäfer
D000818:Animals; D001921:Brain / Q000187:drug effects* / Q000201:enzymology; D001643:Bridged Bicyclo Compounds; D004298:Dopamine / Q000378:metabolism; D005260:Female; D020902:Hypericum; D008297:Male; D051379:Mice; D008995:Monoamine Oxidase / Q000378:metabolism; D014179:Neurotransmitter Uptake Inhibitors / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism; D010569:Perylene / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D010696:Phloroglucinol / Q000031:analogs & derivatives; D010936:Plant Extracts / Q000737:chemistry / Q000494:pharmacology; D010946:Plants, Medicinal; D011794:Quercetin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D011943:Receptors, Adrenergic, beta / Q000378:metabolism; D011985:Receptors, Serotonin / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism; D013574:Synaptosomes / Q000187:drug effects* / Q000378:metabolism; D013729:Terpenes / Q000032:analysis / Q000494:pharmacology; D014966:Xanthenes / Q000737:chemistry* / Q000494:pharmacology*
D001643:Bridged Bicyclo Compounds; D014179:Neurotransmitter Uptake Inhibitors; D010936:Plant Extracts; D011943:Receptors, Adrenergic, beta; D011985:Receptors, Serotonin; D013729:Terpenes; D014966:Xanthenes; D012701:Serotonin; D010569:Perylene; D011794:Quercetin; D010696:Phloroglucinol; D008995:Monoamine Oxidase; C001654:hyperforin; D004298:Dopamine; D009638:Norepinephrine