Target intelligence / Profile preview

Hypericum perforatum extract

Molecular classification
Other (complex plant extract), Not a specific molecular target
01

Overview

Hypericum perforatum extract is a complex herbal preparation derived from the aerial parts of the Hypericum perforatum plant (St. John’s wort). It contains a wide variety of bioactive compounds—including naphthodianthrones (hypericin, pseudohypericin), phloroglucinols (hyperforin), flavonoids, essential oils, and others[1][3][2]. The main use for standardized extracts is the treatment of mild to moderate depression, with efficacy linked mainly to the content of hyperforin and, to a lesser extent, hypericin[3][4]. The extract works primarily through inhibition of monoamine neurotransmitter reuptake, induction of drug-metabolizing enzymes, and other neurochemical effects. Importantly, "Hypericum perforatum extract" does not refer to a single molecular target, but to a plant extract with variable composition and pharmacology. The intake of this extract poses clinically significant risks, especially via potentially dangerous drug interactions[3].

Other names
St. John’s wort extractHypericum extractHyperici herba (herb of Hypericum perforatum)Johanniskraut (German)
02

Mechanism of action

Hyperforin, one of the main constituents, is a reuptake inhibitor of serotonin, norepinephrine, dopamine, GABA, and glutamate, likely through indirect mechanisms such as activation of TRPC6[4]. Induction of hepatic and intestinal cytochrome P450 enzymes (notably CYP3A4, CYP2C9) and P-glycoprotein via activation of pregnane X receptor (PXR)[3][4], which alters the pharmacokinetics of many co-administered drugs. Additional phytochemicals (hypericin, flavonoids, etc.) contribute to a range of poorly-defined mechanisms[1][3].

03

Biological functions

Other (combination of multiple phytochemical activities)
04

Disease associations

Other (used in mild to moderate depression)Evidence for other disease areas is lacking or not supported by clinical evidence[3]
05

Safety considerations

Serious drug interactions due to induction of CYP3A4, CYP2C9, and P-glycoprotein: can cause loss of efficacy of many prescription drugs[3]Adverse CNS effects (e.g., serotonin syndrome when combined with other serotonergic drugs)Photosensitivity reactionsVariability in composition and content of active ingredients between products[3]
06

Interacting drugs

Oral contraceptives

5 more in the full profile.

07

Biomarkers

None known for patient selection or efficacy monitoring

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