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Titolo:
INTESTINAL-ABSORPTION OF FLUORESCENCE-DERIVATIZED CATIONIC PEPTIDE 001-C8-NBD VIA ADSORPTIVE-MEDIATED TRANSCYTOSIS
Autore:
SAI Y; KAJITA M; TAMAI I; KAMATA M; WAKAMA J; WAKAMIYA T; TSUJI A;
Indirizzi:
KANAZAWA UNIV,FAC PHARMACEUT SCI,DEPT PHARMACEUT,TAKARA MACHI KANAZAWA ISHIKAWA 920 JAPAN KANAZAWA UNIV,FAC PHARMACEUT SCI,DEPT PHARMACEUT KANAZAWA ISHIKAWA 920 JAPAN OSAKA UNIV,FAC SCI,DEPT CHEM TOYONAKA OSAKA 560 JAPAN KINKI UNIV,FAC SCI & TECHNOL,DEPT CHEM HIGASHIOSAKA OSAKA 577 JAPAN
Titolo Testata:
Bioorganic & medicinal chemistry
fascicolo: 6, volume: 6, anno: 1998,
pagine: 841 - 848
SICI:
0968-0896(1998)6:6<841:IOFCP0>2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
BLOOD-BRAIN-BARRIER; RAT SMALL-INTESTINE; OLIGOPEPTIDE TRANSPORTER; ANALGESIC PEPTIDE; INVIVO; DRUG; MICRODIALYSIS; ENDOCYTOSIS; PERMEATION; EBIRATIDE;
Keywords:
INTESTINAL ABSORPTION; ADSORPTIVE-MEDIATED TRANSCYTOSIS; DRUG DELIVERY; CATIONIC PEPTIDE; FLUORESCENT-LABELED PEPTIDE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
21
Recensione:
Indirizzi per estratti:
Citazione:
Y. Sai et al., "INTESTINAL-ABSORPTION OF FLUORESCENCE-DERIVATIZED CATIONIC PEPTIDE 001-C8-NBD VIA ADSORPTIVE-MEDIATED TRANSCYTOSIS", Bioorganic & medicinal chemistry, 6(6), 1998, pp. 841-848

Abstract

The intestinal absorption of an intact oligopeptide was investigated in rats using a synthetic cationic peptide, 001-C8 (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)(8)NH2). The peptide was coupled with 4-nitrobenzo-2-oxa-1,3-diazole (NBD) to prepare a fluorescence-labeled derivative 001-C8-NBD (H-MeTyr-Arg-MeArg-D-Leu-NH(CH2)(8)NH-NBD) for the purpose of quantification, The degradation half-life of 001-C8-NBD in jejunal homogenate (1 mg/mL) was 99.5 min, which was significantly longer than that of natural leucine enkephalin (1.14 min). The absorption of 001-C8-NBD was evaluated by the vascular-perfusion method. Intact 001-C8-NBD appeared in the blood time-dependently and the absorption volume at 30 min(2.75 +/- 0.14 mu L/cm intestine) was significantly larger than that of [H-3]PEG 900 (0.88 +/- 0.13 mu L/cm intestine), of which membrane permeability is very low. The absorption of 001-C8-NBD was greatly reduced by an adsorptive-mediated endocytosis inhibitor, protamine (10 mM). No inhibition of the absorption of [H-3]PEG 900 by protamine was observed. The intestinal absorption was also measured by an in vivo loop method. The absorption clearance of 001-C8-NBD measured by this method(0.083 +/- 0.008 mu L/min/cm intestine) was comparable to that obtained by the vascular perfusion method (0.092 +/- 0.005 mu L/min/cm intestine). All of these data suggested that 001-C8-NBD was absorbed as theintact oligopeptide in the intestine in vivo. Adsorptive-mediated transcytosis is suggested to have enormous potential as an oral delivery system for peptide and/or protein drugs. (C) 1998 Elsevier Science Ltd. All rights reserved.

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Documento generato il 04/07/20 alle ore 20:53:33