HYPERFORIN

Uses

St. John’s wort is a widely consumed herbal preparation which has been claimed to have a number of medicinal properties. It contains a number of known lipid signalling mediators, including chlorogenic acid, hypericin, hyperforin, and I3,II8-biapigenin. Hyperforin exhibits two activities which may alter the action of other concurrent medications. It inhibits the activity of several CYP450 enzymes, with CYP2D6 being the most sensitive with an IC50 of about 10 μg/ml. Hyperforin is also a ligand for the steroid X receptor (SXR). Since one activity of this receptor is the induction of CYP450 expression, the exact nature of hyperforin’s drug-drug interactions must be evaluated on a case-by-case basis. However, these interactions certainly complicate its use as a human therapeutic.[Cayman Chemical]

Uses

Hyperforin may be used:

• as a reference standard for calibration curve generation in high-perfornamce liquid chromatography (HPLC) analysis
• to test its cytotoxic effect and apoptosis induction in mouse embryonic cells
• as a pregnane X receptor (PXR) in porcine brain capillary endothelial cells for transport assay

Definition

ChEBI: A cyclic terpene ketone that is a prenylated carbobicyclic acylphloroglucinol derivative produced by St. John's Wort, Hypericum perforatum.

General Description

Hyperforin is a phloroglucinol component of St. John′s wort and a pregnane X receptor ligand.

Biochem/physiol Actions

Hyperforin is an active antidepressant and an inhibitor of cytochrome P450 3A4 (CYP3A). It elicits antioxidant and antibacterial activity. Hyperforin is also embryotoxic and inhibits tumor proliferation. It effectively inhibits dopamine, serotonin and norepinephrine.

Synthesis

Low temperature ultrasonic extraction process: weigh 10g of crushed Hypericum perforatum powder, placed in a 500mL beaker, add 10 times the amount of 75% ethanol and mix according to the volume ratio, add the appropriate amount of antioxidants, according to a variety of set conditions of ultrasound time of 10min each time, extraction for 3 times, combined extracts, with nitrogen blowing instrument to volatilize the ethanol, the use of freeze-drying technology for drying, the temperature of -60 . Pre-freezing for 4h, and then drying under the conditions of the program heating curve for 27h, that is, to obtain the extract of Hypericum perforatum. Guanlianin is unstable to light and heat, therefore, the temperature should always be controlled below 60C at each step of the whole process such as extraction and guanlianin should be stored in brown bottles protected from light.

in vivo