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目的:探讨radicamine B对大鼠体外小肠葡萄糖吸收的影响。方法:采用α-葡萄糖苷酶抑制实验及酶抑制动力学实验和离体大鼠小肠葡萄糖吸收模型来研究radicamine B的抑制作用。结果:radicamine B对α-葡萄糖苷酶和大鼠体外小肠葡萄糖的吸收均呈剂量依赖性抑制作用,其IC50分别为2.19,0.094 g.L--1,与拜糖平相比较无显著性差异。而且radicamineB对α-葡萄糖苷酶活性属于竞争性抑制,Ki=6.3×10-7 mol.L-1。结论:radicamine B能显著抑制小肠葡萄糖的吸收,有望成为一种治疗糖尿病的药物。
Objective: To investigate the effect of radicamine B on rat intestinal glucose absorption. METHODS: The inhibitory effect of radicamine B was studied by α-glucosidase inhibition assay, enzyme inhibition kinetics assay, and rat intestine glucose absorption model. RESULTS: Radacamine B showed a dose-dependent inhibitory effect on α-glucosidase and glucose uptake in rat intestine in vitro. The IC50 values were 2.19 and 0.094 g.L-1, respectively, and there was no significant difference when compared with glycoside. Moreover, radicamine B is competitively inhibited by α-glucosidase activity, Ki = 6.3 × 10-7 mol.L-1. CONCLUSION: Radacamine B can significantly inhibit the absorption of glucose in the small intestine and is expected to become a drug for the treatment of diabetes.