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Titolo:
IMPROVEMENT OF INTESTINAL-ABSORPTION OF LEUCINE-ENKEPHALIN BY SUGAR COUPLING AND PEPTIDASE INHIBITORS
Autore:
MIZUMA T; OHTA K; KOYANAGI A; AWAZU S;
Indirizzi:
TOKYO UNIV PHARM & LIFE SCI,SCH PHARM,DEPT BIOPHARMACEUT,1432-1 HORINOUCHI HACHIOJI TOKYO 19203 JAPAN TOKYO UNIV PHARM & LIFE SCI,SCH PHARM,DEPT BIOPHARMACEUT HACHIOJI TOKYO 19203 JAPAN
Titolo Testata:
Journal of pharmaceutical sciences
fascicolo: 8, volume: 85, anno: 1996,
pagine: 854 - 857
SICI:
0022-3549(1996)85:8<854:IOIOLB>2.0.ZU;2-2
Fonte:
ISI
Lingua:
ENG
Soggetto:
GUINEA-PIG ILEUM; AMINOPEPTIDASE; DEGRADATION; TRANSPORT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
9
Recensione:
Indirizzi per estratti:
Citazione:
T. Mizuma et al., "IMPROVEMENT OF INTESTINAL-ABSORPTION OF LEUCINE-ENKEPHALIN BY SUGAR COUPLING AND PEPTIDASE INHIBITORS", Journal of pharmaceutical sciences, 85(8), 1996, pp. 854-857

Abstract

Peptidase-degradable leucine enkephalin (LE) was coupled with cellobiose or gentiobiose. in the absorption experiments, cellobiose-coupled LE (CcpLE) was more stable than LE itself on the mucosal side, and CcpLE appeared on the serosal side. Destyrosyl LE coupled with cellobiosewas not formed, indicating that sugar coupling provided LE with aminopeptidase resistance. In the presence of inhibitors of angiotensin-converting enzyme and enkephalinase, the stability of CcpLE on the mucosal side was increased, and as a result more was absorbed. Furthermore, the absorption clearance was much higher than the Value expected from the mucosal concentration of CcpLE. Similar results were observed in the absorption of gentiobiose-coupled LE. In the LE absorption experiment, however, LE was not detected on the serosal side even in the presence of these peptidase inhibitors. Improvement of intestinal absorption by sugar coupling and peptidase inhibitors was evaluated kinetically, indicating the exclusive contribution of metabolic degradation of LEthrough intestinal tissues to the absorption process.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 20/09/20 alle ore 10:02:40