小檗碱对葡萄糖吸收的抑制作用

目的研究小檗碱的吸收特性和对肠道葡萄糖吸收的影响,探索小檗碱抗糖尿病作用机制。方法采用在体肠灌流模型观察小檗碱的吸收特性;用Caco-2细胞模型研究小檗碱对肠上皮细胞二糖酶(麦芽糖酶)活力的影响和对葡萄糖转运蛋白的作用。结果小檗碱在肠道内几乎不吸收(2.5 h吸收量小于5%),但能有效抑制小肠上皮细胞上二糖酶活力,其抑制蔗糖酶的ID50为1.830 mg·L^-1;对麦芽糖酶也有抑制作用,但无明显的剂量关系。小檗碱对于葡萄糖在Caco-2细胞上的摄取也有一定抑制作用。结论小檗碱抗糖尿病作用可能主要通过抑制蔗糖酶、麦芽糖酶等二糖酶活力,作为一种α-葡糖苷酶抑制剂发挥其抗糖尿病作用。

Inhibitory action of berberine on glucose absorption

AIM: To study the absorption characteristics of berberine and its influence on glucose absorption. METHODS: Rat recirculating perfusion model was used to study berberine absorption characteristics and Caco-2 cell model was used to explore the influence of berberine on disaccharidase, using HPLC to assay the appearance of glucose to indicate enzyme activities. RESULTS: Berberine was found to be hardly absorbed in the intestine (less than 5% in 2.5 h). However, sucrase and maltase activities were found to be inhibited by berberine, its ID50 to sucrase is 1.830 mg.L-1, and showed no dose dependent influence on maltase activity. Berberine also showed influence on glucose absorption. However, this effect is not significant. CONCLUSION: Berberine may act as an alpha-glucosidase inhibitor, which is its main mechanism in diabetes treatment.