Description
Hyperforin is a natural activator of the steroid X receptor (active at 0.1 to 0.5 μg/ml) and inhibitor of several cytochrome P450 (CYP) isoforms (IC
50 = 10 μg/ml for CYP2D6). It can also inhibit microsomal prostaglandin E
2 synthase-1 (mPGES-1; IC
50 = 1 μM), 5-lipoxygenase activating protein, and sirtuins.
Uses
Hyperforin Dicyclohexylammonium Salt is an inhibitor of monoamine uptake and TRPC6 agonist.
General Description
This substance is a primary reference substance with assigned absolute purity (considering chromatographic purity, water, residual solvents, inorganic impurities). The exact value can be found on the certificate. Produced by PhytoLab GmbH & Co. KG
Biochem/physiol Actions
Stable salt of hyperforin. Hyperforin is believed to be the primary active constituent responsible for the antidepressant and anxiolytic properties of the extracts of St. John′s wort. It acts as a reuptake inhibitor of monoamines, including serotonin, norepinephrine, dopamine, and of GABA and glutamate by activating the transient receptor potential ion channel TRPC6. Activation of TRPC6 induces the entry of sodium and calcium into the cell which causes inhibition of monoamine reuptake. It also is an activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Recent studies have found other neurological effects, effects on inflammation, as well as antibacterial, antitumoral and antiangiogenic effects.
