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]

1. Katsunori Yamaura, Maki Shimada, Noriyuki Nakayama, Koichi Ueno;
Protective effects of goldenseal (Hydrastis canadensis L.) on acetaminophen-induced hepatotoxicity through inhibition of CYP2E1 in rats; PubMed PMID: 22224048
2. Clin Pharmacol Ther. 2005 May;77(5):415-26;
In vivo effects of goldenseal, kava kava, black cohosh, and valerian on human cytochrome P450 1A2, 2D6, 2E1, and 3A4/5 phenotypes; Gurley BJ, Gardner SF, Hubbard MA, Williams DK, Gentry WB, Khan IA, Shah A; Department of Pharmaceutical Sciences, College of Pharmacy, University of Arkansas for Medical Sciences, 4301 W Markham St, Slot 522, Little Rock, AR 72205, USA; PubMed PMID: 15900287
3. An in vitro evaluation of cytochrome P450 inhibition and P-glycoprotein interaction with goldenseal, Ginkgo biloba, grape seed, milk thistle, and ginseng extracts and their constituents.
Etheridge AS, Black SR, Patel PR, So J, Mathews JM. PubMed PMID: 17611934
4. Clinical assessment of CYP2D6-mediated herb-drug interactions in humans: effects of milk thistle, black cohosh, goldenseal, kava kava, St. John's wort, and Echinacea.
Gurley BJ, Swain A, Hubbard MA, Williams DK, Barone G, Hartsfield F, Tong Y, Carrier DJ, Cheboyina S, Battu SK; PMID: 18214849; PMCID: 2562884;
5. Repeated administration of berberine inhibits cytochromes P450 in humans
Ying Guo, Yao Chen, Zhi-rong Tan, Curtis D. Klaassen, Hong-hao Zhou; Published online 2011 Aug 26.; Eur J Clin Pharmacol. 2012 Feb; 68(2): 213–217.; doi: 10.1007/s00228-011-1108-2; NIHMSID: NIHMS583946; PMCID: PMC4898966

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