Berberine is a cationic alkaloid that was first isolated in 1917 from goldenseal (Hydrastis canadensis), a North American herb of the buttercup family. It is found in the roots, rhizomes, stems, and bark of many other plants, including Berberisspp. (worldwide), yellowroot (Southwestern United States), and the Amur cork tree (East Asia). It usually exists as the chloride, but T. Kametani and co-workers reported the total synthesis as the iodide in 1969.
Berberine’s strong yellow color and yellow fluorescence made it a widely used dye in early days of the industry. It is still used in India as a wool dye, and its fluorescence makes it useful as a histology stain.
But berberine’s main use is as an herbal dietary supplement. It has antibiotic, anti-inflammatory, and antineoplastic properties, and it is being investigated as a treatment for diabetes, cancer, hyperlipidemia, congestive heart failure, and HIV. The US Food and Drug Administration has not yet approved berberine for any prescription or over-the-counter drug use, and it has sent notices of violation to companies that have made drug claims on their Web sites. Clinical trials show that berberine is generally safe, but it has shown drug interactions and is contraindicated for pregnant and breast-feeding women.
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