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Drug Metab Rev. 2017 May;49(2):139-157. doi: 10.1080/03602532.2017.1306544. Epub 2017 Apr 3.

The metabolism of berberine and its contribution to the pharmacological effects.

Wang K1,2, Feng X1, Chai L1,2, Cao S1,2, Qiu F1,2.

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a School of Chinese Materia Medica , Tianjin University of Traditional Chinese Medicine , Tianjin , P.R. China.
b Tianjin State Key Laboratory of Modern Chinese Medicine , Tianjin University of Traditional Chinese Medicine , Tianjin , P.R. China.


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.


Berberine; active metabolites; metabolism; oral bioavailability; pharmacological effects

[Indexed for MEDLINE]

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