Hydrastis canadensis (Goldenseal) and Lawsonia inermis (Henna)
Azamal Husen in Herbs, Shrubs, and Trees of Potential Medicinal Benefits, 2022
Hydrastis canadensis (Figure 8.1) is an herbaceous plant that is annually growing from a horizontal, yellowish rhizome, Plantae kingdom and Ranunculaceae family. Fine hairy, erect, unbranched, stalks are 15–50 cm long (www.efloras.org. Retrieved January 1, 2021). Goldenseal is a small, long-lived herb with two large leaves (Gentry et al., 1998). It has one small white flower and a single fruit that is similar in shape, and its color is raspberry (Lloyd and Lloyd, 1884).Different parts of Hydrastis canadensis.
Catalog of Herbs
James A. Duke in Handbook of Medicinal Herbs, 2018
Alkaloids isolated from hydrastis include hydrastine (1.5 to 4%), berberastine (2 to 3%), berberine (0.5 to 6%), canadine, candaline, hydrastinine, 5-hydroxytetrahydroberberine, meconine, reticuline, and xanthopucine. Volatile oils, chlorogenic acid, phytosterins, and resins are also recorded. Leung states that goldenseal is used for inflammation of mucous membranes (uteral and vaginal), hemorrhoids, nasal congestion, sore eyes, sore gums, acne, dandruff, etc.29
Bioactivation of herbal constituents: mechanisms and toxicological relevance
Published in Drug Metabolism Reviews, 2019
Goldenseal extracts (Hydrastis canadensis) is a popular dietary supplement in the United States for gastrointestinal disorders. The primary bioactive constituents are the MDP-containing isoquinoline alkaloids including hydrastine and berberine. Concomitant administration of goldenseal extract inhibited the metabolism of CYP2D6 and CYP3A4 index substrate drugs in healthy subjects (Gurley et al. 2008a, 2008b). Ingestion of a goldenseal supplement (1.3 g root extract containing 132 mg hydrastine and 77 mg berberine) for 2 weeks led to 62% and 41% increase in AUC and Cmax of midazolam respectively (Gurley et al. 2008b). Hydrastine was shown to be a mechanism-based inhibitor of CYP3A4, with inactivation parameters KI = 110 µM and kinact = 0.23 min−1 (Chatterjee and Franklin 2003). The quasi-irreversible inhibition was evidenced by time- and NADPH-dependent formation of the 455 nm absorbing species, with no dissociation of the MI complex in the presence of selective CYP substrates. Mechanism-based inactivation of CYP3A4 and CYP2D6 by berberine was also demonstrated (Zhao et al. 2015). While a carbene may be involved in the MI complex formation, the catechol formed via oxidative demethylenation of the MDP moiety was identified in healthy subjects after oral administration of a goldenseal supplement (Gupta et al. 2015).
Cancer Related to Herbs and Dietary Supplements: Online Table of Case Reports. Part 5 of 5
Published in Journal of Dietary Supplements, 2018
Native Americans used goldenseal (Hydrastis Canadensis L.) as a medicinal remedy and yellow coloring agent (IARC, 2016). It is used to treat gastric infections causing diarrhea and as a topical ointment on skin infections. Oral preparations range from 100 to 470 mg daily. Rat studies suggest an increased risk of liver cancer. After their review, the International Agency for Research on Cancer (IARC, 2016) concluded: “There is sufficient evidence in experimental animals for the carcinogenicity of goldenseal root powder” (Goldenseal, p. 86).“There is inadequate evidence in humans for the carcinogenicity of goldenseal” (Goldenseal, p. 86).“Goldenseal root powder is possibly carcinogenic to humans (Group 2B)” (Goldenseal, p. 86).
Mechanism-based inactivation of cytochrome P450 enzymes by natural products based on metabolic activation
Published in Drug Metabolism Reviews, 2020
Tingting Zhang, Jinqiu Rao, Wei Li, Kai Wang, Feng Qiu
Another isoquinoline alkaloid, hydrastine (Table 5), which was extracted from Goldenseal, has two isomers, (+)- and (–)-hydrastine. Only (–)-hydrastine has been proven to be a mechanism-based inhibitor of CYP3A4. The reason for the irreversible inhibition may be due to MIC generation (Chatterjee and Franklin 2003).
Related Knowledge Centers
- Berberine
- Canadine
- Coptis Chinensis
- Efflux
- In Vitro
- Cytochrome P450
- Hydrastine
- Hydrastinine
- Herbal Medicine
- Berberis Aquifolium