Goldenseal (Hydrastis canadensis), also known as orangeroot or yellow puccoon, is an herb in the buttercup family Ranunculaceae, native to southeastern Canada and the northeastern United States.
Goldenseal is reputed to be an alterative, anti-catarrhal, anti-inflammatory, antiseptic, astringent, bitter tonic, laxative, anti-diabetic and muscular stimulant.
Goldenseal's main active compounds are believed to be the isoquinoline alkaloids berberine and hydrastine. It also contains the alkaloids canadaline, canadine (tetrahydroberberine), 1-α-hydrastine and 5-hydroxytetrahydroberberine. In addition to these alkaloids goldenseal also contains feruloyl quinic acid glucoside esers, C-methyl flavonoids (methylluteolin methyl ethers), chlorogenic acid, meconin, β-sitosterol glucoside, resin, starch, sugar, volatile oils, etc.
Effects On Cytochrome P450 Enzymes
Goldenseal has been shown to inhibit several cytochrome P450 enzymes in humans.
Goldenseal Extract P450 Enzyme Interaction
Goldenseal extract has been shown to be a moderate inhibitor of CYP2D6 and CYP3A4. The berberine content differs among extracts from different manufacturers. For optimal and reliable inhibition, it's recommended to use pure berberine rather than an extract.
Enzyme | Effect | Dosage | Verified In Humans |
---|---|---|---|
CYP1A2 | Ne effect [2] | 900 mg1, 3 times daily for 28 days[2] | Yes[2] |
CYP2A6 | ? | ? | ? |
CYP2C9 | No effects in vitro[3] | ? | ? |
CYP2D6 | 50% Inhibition[4] | 208.8 mg of alkaloids2 daily[4] | Yes[4] |
CYP2D6 | 40% inhibition[2] | 900 mg3, 3 times daily for 28 days[2] | Yes[2] |
CYP2E1 | No effect[2]4 | 900 mg5, 3 times daily for 28 days[2] | Yes[2] |
CYP3A4 | 40% Inhibition[2] | 900 mg6, 3 times daily for 28 days[2] | Yes[2] |
Isolated Berberine P450 Enzyme Interaction
Berberine has been shown to be a very potent CYP2D6 inhibitor. It also strongly inhibits CYP2C9 and weakly inhibits CYP3A4.
Enzyme | Effect | Dosage | Verified In Humans |
---|---|---|---|
CYP1A2 | ? | ? | ? |
CYP2A6 | ? | ? | ? |
CYP2C9 | ? | ? | ? |
CYP2C9 | inhibition (200% increase in substrates)[5] | 300 mg for 2 weeks[5] | Yes[5] |
CYP2D6 | inhibition (900% increase in substrates)[5] | 300 mg for 2 weeks[5] | Yes[5] |
CYP2E1 | ? | ? | ? |
CYP3A4 | inhibition (40% increase in substrates)[5] | 300 mg for 2 weeks[5] | Yes[5] |
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