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The metabolism of berberine and its contribution to the pharmacological effects

Wang, Kun, Feng, Xinchi, Chai, Liwei, Cao, Shijie, Qiu, Feng·2017·Drug Metabolism Reviews

Abstract

Berberine, a bioactive alkaloid isolated from several herbal substances, possesses multiple pharmacological effects, including antimicrobial, antidiabetic, anticancer activities. Meanwhile, berberine undergoes extensive metabolism after oral administration which results in its extremely low plasma exposure. Therefore, it is believed that the metabolites of berberine also contribute a lot to its pharmacological effects. Along these lines, this review covers the metabolism studies of berberine in terms of its metabolic pathways and metabolic organs based on the identified metabolites, and it also covers the pharmacological activities of its active metabolites. In brief, the predominant metabolic pathways of berberine are demethylation, demethylenation, reduction, hydroxylation and subsequent conjugation in vivo. Active metabolites such as columbamine, berberrubine and demethyleneberberine also exhibit similar pharmacological effects by comparison with berberine, such as antioxidant, anti-inflammatory, antitumor, antimicrobial, hepatoprotective, neuroprotective, hypolipidemic and hypoglycemic effects. Overall, berberine together with its metabolites formed the material basis of berberine in vivo.

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Metadata

Authors
Wang, K., Feng, X., Chai, L., Cao, S., & Qiu, F.
Venue
Drug Metabolism Reviews
Published
2017-04-03
Volume
49
Issue
2
Pages
139-157
ISSN
  • 0360-2532 (ISSN-L)
  • 1097-9883
OpenAlex
W2604636580
Cited by
502
References
7
FWCI
12.26
Type
journal article
Language
en
Open access
closed

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CoChat. (2026). Citation check: The metabolism of berberine and its contribution to the pharmacological effects. https://app.cochat.ai/papers/10.1080/03602532.2017.1306544
The paper
Wang, K., Feng, X., Chai, L., Cao, S., & Qiu, F. (2017). The metabolism of berberine and its contribution to the pharmacological effects. Drug Metabolism Reviews. https://doi.org/10.1080/03602532.2017.1306544

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.