Department of Pathophysiology, Institute of Digestive Disease, Tongji University School of Medicine, Shanghai, 200092, China.
Phytother Res. 2013 Oct;27(10):1564-71. doi: 10.1002/ptr.4926. Epub 2013 Jan 21.
Although Berberine (BER) is popular in treating gastrointestinal (GI) disorders, its mechanisms are not clear yet. In order to investigate the effects and possible mechanism of BER on GI motility in rodents, we first explored GI motility by recording the myoelectrical activity of jejunum and colon in rats, and upper GI transit with a charcoal marker in mice. Then, the plasma levels of gastrin, motilin, somatostatin and glucagon-like-peptide-1 (Glp-1) were measured by ELISA or radioimmunoassay (RIA). Furthermore, endogenous opioid-peptides (β-endorphin, dynorphin-A, met-enkephalin) were detected by RIA after treatment with BER. Our results showed that BER concentration-dependently inhibited myoelectrical activity and GI transit, which can be antagonized by opioid-receptor antagonists to different extents. The elevated somatostatin and Glp-1, and decreased gastrin and motilin in plasma, which were caused by BER application, also could be antagonized by the opioid-receptor antagonists. Additionally, plasma level of β-endorphin, but not dynorphin-A and met-enkephalin, was increased by applying BER. Taken together, these studies show that BER plays inhibiting roles on GI motility and up-regulating roles on somatostatin, Glp-1 and down-regulating roles on gastrin, motilin. The pharmacological mechanisms of BER on GI motility and plasma levels of GI hormones were discovered to be closely related to endogenous opioid system.
尽管小檗碱（BER）在治疗胃肠道（GI）疾病方面很受欢迎，但它的作用机制尚不清楚。为了研究 BER 对啮齿动物 GI 运动的影响及其可能的机制，我们首先通过记录大鼠空肠和结肠的肌电活动以及小鼠上 GI 转运的木炭标记来探索 GI 运动。然后，通过 ELISA 或放射免疫测定法（RIA）测量血浆胃泌素、胃动素、生长抑素和胰高血糖素样肽-1（Glp-1）的水平。此外，在用 BER 处理后，通过 RIA 检测内源性阿片肽（β-内啡肽、强啡肽-A、甲硫氨酸脑啡肽）。我们的结果表明，BER 浓度依赖性地抑制肌电活动和 GI 转运，阿片受体拮抗剂可以不同程度地拮抗这种作用。BER 引起的血浆生长抑素和 Glp-1 升高，胃泌素和胃动素降低，也可被阿片受体拮抗剂拮抗。此外，BER 应用后血浆β-内啡肽水平升高，但强啡肽-A 和甲硫氨酸脑啡肽水平没有升高。综上所述，这些研究表明，BER 对 GI 运动具有抑制作用，对生长抑素、Glp-1 具有上调作用，对胃泌素、胃动素有下调作用。BER 对 GI 运动和胃肠激素血浆水平的药理作用机制与内源性阿片系统密切相关。
