REGULATION OF INTRACELLULAR GLUCOCORTICOID CONCENTRATIONS

摘要

The interconversion of inactive 11-keto steroids with their active 11beta-hydroxy equivalents can be controlled by the use of inhibitors of the 11beta-reductase enzyme, such as carbenoxolone (3beta-(3-carboxypropionyloxy)-11-oxo-olean-2-en30-oic acid). Such inhibitors may be put to a number of therapeutic uses in humans and animals, for instance to inhibit hepatic gluconeogenesis, to lower intracellular cortisol concentration, to increase insulin sensitivity in adipose tissue and muscle, and to prevent or reduce neuronal loss/cognitive impaiment due to glucocorticoid potentiated neurotoxicity or neural dysfunction or damage.