title: Inhibition of insulin release by alpha- and beta-D-galactose pentaacetate.
abstract: Several monosaccharide polyacetate esters display higher biological efficiency than the corresponding unesterified carbohydrates, this being attributable to their capacity to cross the plasma membrane without requiring the intervention of a specific carrier system and to their subsequent intracellular esterase-catalyzed hydrolysis. Some of these esters, however, also exert a direct effect upon a receptor system apparently displaying analogies with that involved in the identification of bitter compounds by taste buds. For instance, under suitable experimental conditions, esters of non-nutrient monosaccharides, such as L-glucose, D-mannoheptulose or 2-deoxy-D-glucose, unexpectedly stimulate insulin release. The present work reveals that alpha-D-galactose pentaacetate and, to a lesser extent, beta-D-galactose pentaacetate both inhibit leucine-induced insulin release in rat pancreatic islets. This indicates that the postulated receptor system displays anomeric specificity and may participate in a negative modulation of insulin secretion. It is proposed that advantage could be taken of the negative insulinotropic action of D-galactose pentaacetate esters to prevent excessive insulin release in pathological situations.
authors.affiliation: Laboratory of Experimental Medicine, Brussels Free University, Brussels, Belgium.
authors.forename: W J
authors.initials: WJ
authors.lastname: Malaisse
authors.forename: M M
authors.initials: MM
authors.lastname: Kadiata
mesh_terms: D000818:Animals; D005260:Female; D005690:Galactose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D066298:In Vitro Techniques; D007328:Insulin / Q000378:metabolism*; D007329:Insulin Antagonists / Q000494:pharmacology*; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000187:drug effects* / Q000378:metabolism; D007930:Leucine / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D007328:Insulin; D007329:Insulin Antagonists; C026877:galactose peracetate; D007930:Leucine; D005690:Galactose