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目的:建立醛糖还原酶(A ldose Reductase,AR)抑制剂的体外筛选模型,考察黄芩苷、小檗碱及黄芪多糖对AR的体外抑制作用及三者配伍的合并效应。方法:测定不同质量浓度的黄芩苷、小檗碱、黄芪多糖以及阳性对照药(依帕司他)对AR的抑制率;结合正交t值法评价3种药物配伍后对AR作用的合并效应。结果:300μg/mL的黄芩苷和小檗碱对AR的抑制率分别为(88.4±7.4)%、(69.0±9.4)%,二者合用时对AR的抑制作用表现为拮抗;黄芪多糖则无AR抑制活性。结论:黄芩苷、小檗碱体外能显著抑制AR的活性,是良好的醛糖还原酶抑制剂。
Objective: To establish an in vitro screening model for aldose reductase (AR) inhibitors and investigate the inhibitory effects of baicalin, berberine and astragalus polysaccharides on AR in vitro and the combined effect of the three drugs. METHODS: The inhibition rates of AR by different concentrations of baicalin, berberine, astragalus polysaccharides, and positive control (Epalrestat) were determined; the combined effects of three drugs on AR were evaluated by orthogonal t value method. . RESULTS: The inhibition rates of AR by baicalin and berberine at 300 μg/mL were (88.4±7.4)% and (69.0±9.4)%, respectively. When the two were combined, the inhibitory effect on AR was antagonistic; the APS was not. AR inhibitory activity. Conclusion: Baicalin and berberine can significantly inhibit the activity of AR in vitro and is a good inhibitor of aldose reductase.