Polysaccharide and flavones were extracted, isolated, and partially purified from mulberry leaves. The results from studies by using enzymatic kinetics showed that, mulberry leave polysaccharide was an excellent competitive inhibitor of α- glucosidase for glucose releasing. Its inhibitory rate increased with increasing concentration. The optimum acting time for polysaccharide inhibition was 5min. Mulberry leave flavone was found as an activator of α-glucosidase, a potential functional factor for increasing blood sugar. Glycerol monostearicate, as an emulsifier, was introduced into the enzymatic reaction solvent system to enhance the homogeneity of flavones in water.