Biomaterial Database

Characterization of the sulfonylurea-induced potentiation of the insulin response in cultured 3T3 adipocytes. 1986

J P van Putten, and H M Krans

Studies were carried out to determine the role of sulfonylureas in the regulation of insulin-sensitive hexose uptake in cultured 3T3 adipocytes. Exposure (0-72 hr) of cells to the sulfonylurea-derivative tolbutamide (0.05-0.3 mg/ml) induced a time- and concentration-dependent potentiation of the stimulatory effect of insulin on hexose uptake (500 vs 340%). The effect was maximal within 24 hr and completely reversible. It was strictly limited to the presence of insulin. Basal hexose uptake and insulin binding were not affected by the drug. High concentrations of the agent (greater than 0.3 mg/ml) induced a decrease in insulin response, suggesting a concentration optimum. Lineweaver-Burk analysis of uptake data revealed that the potentiating effect of tolbutamide was due to enhancement of the insulin-induced increase in apparent Vmax, i.e. in the number or activity of hexose transporters. This enhancement was inhibited by cycloheximide (1 microgram/ml), indicating involvement of protein synthesis in the induction of the effect. It is concluded that sulfonylureas act by influencing synthesis of protein(s) which potentiate the effect of insulin on hexose uptake.

UI	MeSH Term	Description	Entries
D007328	Insulin	A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).	Iletin,Insulin A Chain,Insulin B Chain,Insulin, Regular,Novolin,Sodium Insulin,Soluble Insulin,Chain, Insulin B,Insulin, Sodium,Insulin, Soluble,Regular Insulin
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D002460	Cell Line	Established cell cultures that have the potential to propagate indefinitely.	Cell Lines,Line, Cell,Lines, Cell
D004305	Dose-Response Relationship, Drug	The relationship between the dose of an administered drug and the response of the organism to the drug.	Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004357	Drug Synergism	The action of a drug in promoting or enhancing the effectiveness of another drug.	Drug Potentiation,Drug Augmentation,Augmentation, Drug,Augmentations, Drug,Drug Augmentations,Drug Potentiations,Drug Synergisms,Potentiation, Drug,Potentiations, Drug,Synergism, Drug,Synergisms, Drug
D006601	Hexoses	MONOSACCHARIDES whose molecules contain six carbon atoms, such as GLUCOSE and FRUCTOSE. They generally have the chemical formula C6H12O6.	Hexose
D000273	Adipose Tissue	Specialized connective tissue composed of fat cells (ADIPOCYTES). It is the site of stored FATS, usually in the form of TRIGLYCERIDES. In mammals, there are two types of adipose tissue, the WHITE FAT and the BROWN FAT. Their relative distributions vary in different species with most adipose tissue being white.	Fatty Tissue,Body Fat,Fat Pad,Fat Pads,Pad, Fat,Pads, Fat,Tissue, Adipose,Tissue, Fatty
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D013997	Time Factors	Elements of limited time intervals, contributing to particular results or situations.	Time Series,Factor, Time,Time Factor
D014044	Tolbutamide	A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)	Apo-Tolbutamide,Artosin,Diabetol,Diaval,Dolipol,Orabet,Orinase,Rastinon,Tolbutamid R.A.N.