Study On The Inhibition Of Glycosidases By Cyclitol Compounds

Cyclitol compounds can be found in the configurations of many products of microbial metabolizability. As cyclitol compounds have strong inhibition on hydrolases, especially glycosidases, the studies on cyclitol compounds have gained more and more attention. In our lab, validamycins were used as raw material, cyclitol compounds such as vaienamine, validamine, and validoxylamine A were obtained by microbial catalysis.In this paper, the inhibition of valienamine and validamine on porcine intestinal sucrase@maltase and yeast sucrase was researched in detail. The results of experiments indicated that valienamine and validamine had inhibition effects on various glycosidases incoordinately. The inhibition of valienamine and validamine was competitive and the inhibitors were thermostable within 30~100$. The interaction of the inhibitor valienamine or validamine and glycosidases is a fast binding process in the experiments. The results showed that approximately five minutes was required to reach inhibition equilibrium.Validoxylamine A, the core of jinggangmycins, is composed of two unique aminocyclitol units, and its structure is very similar to that of trehalose. Validoxylamine A could control some bad insect and fungus via inhibiting the activity of trehalase. In this dissertation , the inhibition of silkworm and porcine kidney trehalase by validoxylamine A was studied. Results showed that validoxylamine A had strong inhibition on trehalase.In addition, the configuration of jinggangmycins comprises of validoxylamine A and glucose. Validoxylamine A and glucose are linked with glycosidic bond. So various glycosidases were tried to decomposejinggangmycins to validoxylamine A. After trials, it was found that the enzymolysis rate was low. There are many works to be done for finding a suitable glycosidase.All of studies in this dissertation offer references to research and development of glycosidase inhibitor medicine and bio-pesticide.