Abstract
Cyclic depsipeptide Cereulide toxin it is a very well know potassium electrogenic ionophore particularly sensitive to pancreatic beta cells. The mechanistic details of specific activity are unknown. Here, we describe a series of synthetic substituted cereulide potassium ionophores that cause an impressive selective activation of glucose-induced insulin secretion in a constitutive manner in rat insulinoma INS1E cells. Our study demonstrates that a different electroneutral K+transport mechanism by the anionic mutant depsipeptides when compared with classical electrogenic Cereulides can have an important impact of pharmacological value on gluco-sestimulated insulin secretion.