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Acta Pharmacol Sin. 2017 Feb;38(2):157-167. doi: 10.1038/aps.2016.125. Epub 2016 Dec 5.

Advances in the study of berberine and its derivatives: a focus on anti-inflammatory and anti-tumor effects in the digestive system.

Zou K1,2, Li Z1,2, Zhang Y2, Zhang HY1,2, Li B2, Zhu WL2, Shi JY3,4, Jia Q1, Li YM1.

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School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.
CAS Key Laboratory of Receptor Research, Drug Discovery and Design Centre, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
UCB Biopharma SPRL, Chemin du Foriest, Braine-l'Alleud, Belgium.
Kellogg College, University of Oxford, Oxford, OX2 6PN, United Kingdom.


It has been widely recognized that inflammation, particularly chronic inflammation, can increase the risk of cancer and that the simultaneous treatment of inflammation and cancer may produce excellent therapeutic effects. Berberine, an alkaloid isolated from Rhizoma coptidis, has broad applications, particularly as an antibacterial agent in the clinic with a long history. Over the past decade, many reports have demonstrated that this natural product and its derivatives have high activity against both cancer and inflammation. In this review, we summarize the advances in studing berberine and its derivatives as anti-inflammatory and anti-tumor agents in the digestive system; we also discuss their structure-activity relationship. These data should be useful for the development of this natural product as novel anticancer drugs with anti-inflammation activity.

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