Transport of μ-opioid receptor agonists and antagonist peptides across Caco-2 monolayer

Release of Endogenous Opioids From Duodenal Enteroendocrine Cells Requires Trpm5

“…It is unknown at this point what may be the major target of the opioids in the gut, however there are cells and nerve endings with opioid receptors in the vicinity that can be reached by opioids. Small peptides, either produced by gut or resulting from food breakdown have been shown to cross the gut barrier,50 and were also shown experimentally to cross a monolayer of Caco cells 51. Peptide hormones from 5–166 amino acids (including Leu-enkephalin LHRH, insulin, calcitonin, and interferon beta), introduced into the intestinal lumen were effective in crossing the intestinal epithelium and entering the bloodstream.…”

Dairy Chemistry and Biochemistry

“…BCMs have been detected in bovine milk ), milk products (Jarmolowska et al 1999), human milk (Jarmolowska et al 2007a, b) and infant formulae (Sturner and Chang 1988). However, Iwan et al (2008) demonstrated the transport of opioid peptides across human intestinal mucosa, specifically the transport of μ-opioid receptor agonists, human BCMs 5 and 7 (BCM5, BCM7) and the antagonist lactoferroxin A (LCF A). However, Iwan et al (2008) demonstrated the transport of opioid peptides across human intestinal mucosa, specifically the transport of μ-opioid receptor agonists, human BCMs 5 and 7 (BCM5, BCM7) and the antagonist lactoferroxin A (LCF A).…”

Casein-derived bioactive peptides: Biological effects, industrial uses, safety aspects and regulatory status

“…In addition, oligopeptides can be transported by transcytosis (vesicle-mediated transcellular transport) (Shen, Wan, & Ekrami, 1992). Much research has been carried out on the transport of bioactive peptides in Caco-2 cells (Foltz et al, 2007;Iwan et al, 2008). Opioid peptides (Iwan et al, 2008;SienkiewiczSz1apka et al, 2009a), ACE inhibitors (Chua, Jois, Sim, & Go, 2004;Foltz et al, 2008;Zhu et al, 2008) and anti-hypertensive peptides (Quiró s, Dá valos, Lasunció n, Ramos, & Recio, 2008;Sun, Liu, Li, & Qin, 2009) have been shown to cross the epithelial cell monolayer.…”

“…Much research has been carried out on the transport of bioactive peptides in Caco-2 cells (Foltz et al, 2007;Iwan et al, 2008). Opioid peptides (Iwan et al, 2008;SienkiewiczSz1apka et al, 2009a), ACE inhibitors (Chua, Jois, Sim, & Go, 2004;Foltz et al, 2008;Zhu et al, 2008) and anti-hypertensive peptides (Quiró s, Dá valos, Lasunció n, Ramos, & Recio, 2008;Sun, Liu, Li, & Qin, 2009) have been shown to cross the epithelial cell monolayer. These studies found that the method of transport was not only dependent on the size of the peptide but also on charge, molecular weight, hydrogen bonding and hydrophobicity (Iwan et al, 2008;Pauletti, Okumu, & Burchardt, 1997;SienkiewiczSz1apka et al, 2009a).…”