Transport of Val-Leu-Pro-Val-Pro in human intestinal epithelial (Caco-2) cell monolayers.
Angiotensin converting enzyme (ACE) inhibitory peptides are biologically active peptides that play a very important role in blood pressure regulation. In previous experiments, we obtained an ACE inhibitory peptide Val-Leu-Pro-Val-Pro (VLPVP) by DNA recombinant technology. The purpose of this study was to examine the bidirectional transport of VLPVP by using the human intestinal Caco-2 monolayers. The permeability coefficient ( P app) values of VLPVP over 4-8 mmol/L ranged from 7.44 x 10(-8) to 1.35 x 10(-6) cm/s for apical (AP) to basolateral (BL) transport, while the P app values for BL to AP flux were significantly lower than those for the AP to BL flux, with efflux ratio values of 0.74-0.13 over 4-8 mM. Preincubation of the paracellular transport enhancer (sodium deoxycholate), the inhibitor of multidrug resistant protein (MK-571), or sodium azide stimulated efflux of VLPVP significantly ( p < 0.01); these results indicate that the transport of VLPVP across Caco-2 monolayers was involved in paracellular diffusion and MRP2 transport.
Lei
Lin
L
Department of Applied Biotechnology, Shenzhen Polytechnic, Shenzhen, Guangdong, People's Republic of China.
Sun
Haiyan
H
Liu
Dong
D
Liu
Liegang
L
Li
Shimin
S
D000806:Angiotensin-Converting Enzyme Inhibitors / Q000378:metabolism*; D001692:Biological Transport; D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D002851:Chromatography, High Pressure Liquid; D004058:Diffusion; D006801:Humans; D007413:Intestinal Mucosa / Q000378:metabolism*; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins / Q000378:metabolism; D009842:Oligopeptides / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
D000806:Angiotensin-Converting Enzyme Inhibitors; D000089762:Multidrug Resistance-Associated Protein 2; D027425:ATP-Binding Cassette, Sub-Family C Proteins; D009842:Oligopeptides; D011994:Recombinant Proteins; C000715087:ABCC2 protein, human; C530287:valyl-leucyl-prolyl-valyl-proline