Comparison of the in vitro effect of biguanides and sulfonylureas on insulin binding of its receptors in target cells

The Journal of Clinical Endocrinology and Metabolism
R VigneriI D Goldfine

Abstract

The in vitro effects of two biguanides (phenformin and metformin) and four sulfonylureas (tolbutamide, glyburide, gliclazide, and glisolamide) on insulin binding to its receptors were studied in four cultured cell lines: human skin fibroblasts, IM-9 lymphoblasts, MCF-7 human mammary carcinoma, and H35 rat hepatoma. After a 24-h preincubation with maximal stimulatory concentrations of phenformin, specific [125I] insulin binding to its receptors in the four different cell lines were increased over control by 67.2 +/ 17.0%, 101.3 +/- 11.5%, 65.1 +/- 8.0%, and 44.0 +/- 12.1%, respectively (mean +/- SE). Phenformin was effective in IM-9 cells that were down-regulated by unlabeled insulin, and the effect of phenformin on insulin binding was not affected by inhibition of protein synthesis with cycloheximide. In concert with this observation. Scatchard plots indicated that phenformin increased the insulin receptor's affinity rather than the number of insulin-binding sites on IM-9 cells. Metformin was also effective in significantly enhancing insulin binding in both IM-9 and MCF-7 cells. In contrast to the effects of biguanides, none of the four sulfonylureas tested had any significant influence on insulin binding to any of the four cel...Continue Reading

Citations

Sep 1, 1995·Diabetes/metabolism Reviews·S Del PratoA Tiengo
Jun 1, 1988·Diabetologia·F PurrelloI D Goldfine
Oct 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·K M TordjmanM M Mueckler
Aug 20, 1990·The American Journal of Medicine·J F Caro
Oct 1, 1985·Metabolism: Clinical and Experimental·H GinJ Aubertin
Oct 1, 1987·Metabolism: Clinical and Experimental·M B Davidson, G Sladen
Aug 1, 1987·Metabolism: Clinical and Experimental·F PurrelloR Vigneri
Mar 1, 1983·Clinics in Endocrinology and Metabolism·G GrunbergerP Gorden
Jul 1, 1993·Scandinavian Journal of Clinical and Laboratory Investigation·E Widén
Sep 1, 1985·Diabetic Medicine : a Journal of the British Diabetic Association·S A OlczakC N Hales
Apr 7, 2007·Biopharmaceutics & Drug Disposition·V StetinováM Prazáková
Oct 1, 1988·Diabetic Medicine : a Journal of the British Diabetic Association·H Beck-NielsenO Pedersen
Feb 1, 1993·The Annals of Pharmacotherapy·C E RaeD D Cook
Mar 8, 2003·International Journal of Immunopathology and Pharmacology·M T GuagnanoS Sensi
May 23, 2006·Molecular and Cellular Biochemistry·S Satyanarayana, Eswar K Kilari
Dec 1, 1987·Journal of Endocrinological Investigation·K G MountjoyI M Holdaway
Jan 17, 1983·The American Journal of Medicine·D H LockwoodM L McCaleb
May 1, 1986·Pharmacological Research Communications·R I Hoich, F M Ng
Sep 20, 1985·The American Journal of Medicine·J R Gavin
Sep 20, 1985·The American Journal of Medicine·H J FrankW L Morris

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