• Chunqiu Chen, Meiling Lu, Qiuhui Pan, Jakub Fichna, Lijun Zheng, Kesheng Wang, Zhen Yu, Yongyu Li, Kun Li, Aihong Song, Zhongchen Liu, Zhenshun Song, and Martin Kreis.
• Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai, China.
• Plos One. 2015 Jan 1; 10 (12): e0145556.

Background And AimsBerberine and its derivatives display potent analgesic, anti-inflammatory and anticancer activity. Here we aimed at characterizing the mechanism of action of berberine in the gastrointestinal (GI) tract and cortical neurons using animal models and in vitro tests.MethodsThe effect of berberine was characterized in murine models mimicking diarrhea-predominant irritable bowel syndrome (IBS-D) symptoms. Then the opioid antagonists were used to identify the receptors involved. Furthermore, the effect of berberineon opioid receptors expression was established in the mouse intestine and rat fetal cortical neurons.ResultsIn mouse models, berberine prolonged GI transit and time to diarrhea in a dose-dependent manner, and significantly reduced visceral pain. In physiological conditions the effects of berberine were mediated by mu- (MOR) and delta- (DOR) opioid receptors; hypermotility, excessive secretion and nociception were reversed by berberine through MOR and DOR-dependent action. We also found that berberine increased the expression of MOR and DOR in the mouse bowel and rat fetal cortical neurons.ConclusionBerberine significantly improved IBS-D symptoms in animal models, possibly through mu- and delta- opioid receptors. Berberine may become a new drug candidate for the successful treatment of IBS-D in clinical conditions.

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