Rat lens aldose reductase inhibitory activities of Coptis japonica root-derived isoquinoline alkaloids

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 IC50 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 a's lead compounds and new agents for aldose reductase inhibition.