Sequential insulin degradation in cultured fetal hepatocytes in relation with chloroquine-dependent events . Zachayus, Jean-Luc, Shahid Khan, and Christiane Plas. Laboratoire de Biologie-Odontologie, Universit[acute]e Paris 7, Institut Biom[acute]edical des Cordeliers, 15 rue de l'Ecole de M[acute]edecine, 75006 Paris, France
APStracts 3:0089E, 1996.
- Insulin cellular degradation was studied in cultured 18-day old fetal rat hepatocytes in the presence and absence of insulin degradation inhibitors which decrease the glycogenic response to insulin. After cell incubation with 3 nM [125I](A14) or (B26)insulin, hormone degradation products associated with cells or present in the medium were analyzed by HPLC. Within cells, four components containing intact [125I](A14)insulin A-chain and part of B-chain (A1 to A4, according to increasing retention times) were found together with two [125I](B26)insulin B-chain C-terminal fragments (B1 and B2). Medium degradation intermediates comprised B1 and B2 but not A1 to A4. Cellular insulin fragments A3 and B2 exhibited a maximal transient accumulation after 2 min, whereas the others increased progressively to plateau after 10 min. Chloroquine inhibited the formation of A1, A2 and B1 by 70-80%, while that of A3, A4 and B2 was not significantly affected. N-ethylmaleimide (NEM) and bacitracin, two inhibitors of insulin degrading enzyme (IDE), decreased the formation of chloroquine-dependent cellular peptides. Thus, cell -associated insulin degradation implied primarily two cleavages in B -chain near C-terminus, the one sensitive to chloroquine and IDE inhibitors occurring after endosomal segregation of insulin and its receptor.

Received 3 January 1996; accepted in final form 5 April 1996.
APS Manuscript Number E2-6.
Article publication pending Am. J. Physiol. (Endocrinol. Metab.).
ISSN 1080-4757 Copyright 1996 The American Physiological Society.
Published in APStracts on 1 May 96