Lee Hoi-Seon
Research Center for Industrial Development of Biofood Materials and Institute of Agricultural Science & Technology, College of Agriculture, Chonbuk National University, Chonju 561-756, Korea. hoiseon@ moak.chonbuk.ac.kr
J Agric Food Chem. 2002 Nov 20;50(24):7013-6. doi: 10.1021/jf020674o.
The inhibitory activity of Coptis japonica root-derived materials was evaluated against lens aldose reductase isolated from male Sprague-Dawley rats and compared to that of three commercially available isoquinoline alkaloids (berberine sulfate, berberine iodide, and palmatine chloride), as well as quercitrin as aldose reductase inhibitor. The biologically active constituents of C. japonica extract were characterized as the isoquinoline alkaloids, berberine chloride and palmatine iodide, by spectral analysis. The inhibitory effects varied with both chemical and concentration used. The IC(50) values of berberine chloride and palmatine iodide are 13.98 and 13.45 nM, respectively. Among three berberines and two palmatines, the inhibitory activity was much greater for the choridated and sulfated analogues than for those with iodide. Quercitrin was a much more potent inhibitor than berberines and palmatines. Nonetheless, berberines and palmatines may be useful as lead compounds and new agents for aldose reductase inhibition.
评估了黄连根提取物对从雄性Sprague-Dawley大鼠分离的晶状体醛糖还原酶的抑制活性，并将其与三种市售异喹啉生物碱（硫酸小檗碱、碘化小檗碱和氯化巴马汀）以及作为醛糖还原酶抑制剂的槲皮苷的抑制活性进行了比较。通过光谱分析，将黄连提取物的生物活性成分鉴定为异喹啉生物碱氯化小檗碱和碘化巴马汀。抑制作用随所用化学物质和浓度的不同而变化。氯化小檗碱和碘化巴马汀的IC50值分别为13.98 nM和13.45 nM。在三种小檗碱和两种巴马汀中，氯化和硫酸化类似物的抑制活性远高于碘化类似物。槲皮苷是一种比小檗碱和巴马汀更有效的抑制剂。尽管如此，小檗碱和巴马汀可能作为醛糖还原酶抑制的先导化合物和新药物。
