Aldose Reductase Inhibitor Screening Model To Establish And Traditional Chinese Medicine Screening Applications

Aldose reductase(AR),the key enzyme of the polyol pathway associated with the conversion of glucose to sorbitol,is known to play important roles in diabetic complications(DC).Experiments in diabetic animals have implicated that sorbitol accumulation in the cells lead to the development of DC.The use of ARIs in animal studies has demonstrated that DC can be ameliorated.Interpretation of results obtained with ARIs therapy in human subjects suggests that these inhibitors are effective at early stages of DC.Chinese traditional medicine has long-terms experiment in prevention and treatment of the DC at clinical trial,expecially to prolong life-time and improve the quality of living.The enzyme is inhibited by quercetin such as extracts from Salvia miltiorrhiza and Radix Scutellariae,et al.To evaluate the inhibitory potential of aldose reductase from Chinese traditional medicine,the screening model of ARIs has been established with the help of the modern pharmaceutical technology and using the advanced methods and aquipments.After homogenization,centrifugation,(NH₄)₂SO₄ fractionation(40%, 50%,75%) and dialysis,AR has been purified to homogeneity from SD rat lenses. DL-glyceraldehyde is the preferred substrate(Km=72 mM;kcat/Km=17,250) with concomitant conversion of NADPH into NADP⁺.During our research of new ARIs,ZY0095 showing potent inhibitory activity against AR was reseached its active ingredients.The acetal part of ZY0095 separated by D101 column chromatography with 50%ethanol,whose inhibitory activity of AR reaches to 96.5%.We study on the primary activities of ZY0095 and identify these compounds to be consisted of flavone and saponins etc.