Compound Monograph
Hyperforin
A prenylated acylphloroglucinol from St. John's Wort regarded as a principal antidepressant constituent and a potent inducer of drug metabolism.
Classification
Hyperforin is a prenylated acylphloroglucinol, part of the other constituents class. Compounds outside the major chemical classes — nucleosides, simple amines, mixed volatile oils, and as-yet uncategorised constituents.
Where Does It Come From? (1)
Hyperforin is a naturally occurring prenylated acylphloroglucinol, found in St. John's Wort. It is flagged as moderately toxic.
Research & Evidence
Hyperforin is a prenylated acylphloroglucinol and one of the principal active constituents of St. John’s Wort (Hypericum perforatum). It is thought to contribute substantially to the herb’s antidepressant activity, acting in part by inhibiting the reuptake of several neurotransmitters through a mechanism distinct from conventional antidepressants. St. John’s Wort has reasonable clinical evidence for mild to moderate depression, and hyperforin is one of the constituents to which this is attributed.
Toxicity & Safety
Hyperforin is a potent activator of the pregnane X receptor, which strongly induces the drug-metabolising enzyme CYP3A4 and the transporter P-glycoprotein. This makes St. John’s Wort a clinically important cause of herb-drug interactions: it can reduce the effectiveness of many medicines, including oral contraceptives, certain anticoagulants, immunosuppressants, some HIV and cancer drugs, and others. Anyone taking prescription medication should treat St. John’s Wort as capable of serious interactions and seek professional advice before combining them.