Potentiation by its esterification of the inhibitory action of 2-deoxy-D-glucose on D-glucose metabolism and insulinotropic action.

It was recently reported that selected esters of D-glucose are more efficiently metabolized and display a greater insulinotropic action in pancreatic islets than the unesterified hexose. Likewise, in the present study, the inhibitory action of 2-deoxy-D-glucose tetraacetate upon D-glucose metabolism in rat erythrocytes and pancreatic islets was found to be more pronounced than that of unesterified 2-deoxy-D-glucose. At a concentration of 10 mM, the ester also inhibited more severely than unesterified 2-deoxy-D-glucose the release of insulin evoked by D-glucose in isolated islets. It is proposed that 2-deoxy-D-glucose tetraacetate represents a useful tool to facilitate the intracellular delivery of the glucose analog and to increase its efficiency as a potential therapeutic agent.