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Review | Regular issue | Vol 91, No. 12, 2015, pp.2233-2270
Published online, 1st December, 2015
DOI: 10.3987/REV-15-825
Berberine Analogues: Progress towards Versatile Applications

Jing Wang, Jie Tang, Li-Fang Yu, Jia Li, Jing-Ya Li, and Fan Yang*

*Shanghai Engineering Research Center of Molecular Theraputics and New Drug Development, East China Normal University, North Zhongshan Road, Shanghai 200062, China


The promising activities shown by analogues of natural product berberine in numerous categories such as anti-hyperglycaemic, anti-cancer, anti-inflammatory, anti-alzheimer’s disease and anti-microbials, have made it an indispensable structure for development of new therapeutic agents. The compounds bearing various substituents on the berberine skeleton have exhibited a wide spectrum of biological activities. Short reviews on biological importance of this core structure have been showcased in literature. However, systematic review on the research advances of structure-activity relationship of berberine and its analogues seems lacking. In the present review, various analogues of berberine with different pharmacological activities were summarized and their SAR were discussed as well. The current review would provide useful information for further studies on structural modifications on berberine for discovering new drug leads.