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opioid peptides

Effect of gluten exorphins A5 and B5 on the postprandial plasma insulin level in conscious rats.

Abstract

"The effect of exogenous opioid peptides, gluten exorphins A5 and B5, which were isolated from the enzymatic digest of wheat gluten, on thepostprandial insulin level were examined in rats. The oral administration of gluten exorphin A5 at a dose of 30 mg/kg w. potentiated the postprandialplasma insulin level and the effect was reversed by naloxone. The administration of gluten exorphin B5 showed a similar effect at a higher dose (300 mg/kg w). Furthermore, intravenous administration of gluten exorphin A5 at a dose of 30 mg/kg w. also stimulated the postprandial insulin release. The fact that orally and intravenously administered gluten exorphin A5 stimulates insulin release suggests that it modulates pancreatic endocrine function by the action after the absorption rather than within the the gastrointestinal tract."

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Opioid Receptor Ligands Derived from Food Proteins

Abstract:

"During the last two decades a variety of food protein fragments has been demonstrated to elicit biological effects in various in vitro or in vivo test systems. A considerable part of these bioactive peptides are opioid receptor ligands , which may be regarded as exogenous supplements to the endogenous opioidergic systems of the human organism. Most of these foodderived opioid receptor ligands are fragments of the milk proteins alpha-, beta- or kappa-casein, alpha-lactalbumin, beta-lactoglobulin or lactotransferrin; however, also wheat gluten, rice albumin, bovine serum albumin or hemoglobin, i.e. possible constituents of meat, and even a protein from spinach could be demonstrated to contain fragments behaving like opioid receptor ligands. Practically all of these compounds display opioid agonist activity; only very few of them behave like opioid antagonists. Bioactive food protein derivatives have been termed “ food hormones”, which implies that these compounds display their bioactivities when released from food constituents, i.e. from their precursor molecules due to the action of gastrointestinal enzymes. The critical point in case of food protein-derived opioid receptor ligands is that only a minority of their bioactive effects demonstrated as yet has been observed upon oral or intragastric administration of these peptides or their precursor proteins and that most of these studies have been performed in animals. Thus, in terms of “evidence-based dietary supplementation” more studies are needed to prove effects of food protein-derived opioid receptor ligands or their precursors after oral administration in humans and, moreover, to prove a benefit for the consumers organism."

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Gluten exorphin B5 stimulates prolactin secretion through opioid receptors located outside the blood-brain barrier.

Abstract

"Gluten exorphin B5 (GE-B5) is a food-derived opioid peptide identified in digests of wheat gluten. We have recently shown that GE-B5 stimulates prolactin (PRL) secretion in rats; this effect is abolished by preadministration of the opioid receptor antagonist naloxone. However, since the structure of naloxone allows it to cross the blood-brain barrier (BBB) and antagonize opioid effects centrally as well as peripherally, it could not established, on the basis of those data, if GE-B5-induced PRL release is exerted through sites located inside or outside the BBB. In this study, we sought to determine the site of action of GE-B5 on PRL secretion, by pretreating male rats with naloxone methobromide (NMB), an opioid antagonist that does not cross the BBB. Four groups of rats were given the following treatments: 1) intravenous vehicle; 2) intravenous GE-B5 (3 mg kg(-1) body weight); 3) intraperitoneal NMB (5 mg kg(-1) body weight), followed by vehicle; 4) NMB, followed by GE-B5. Blood samples for PRL were taken at intervals for 40 minutes after vehicle or GE-B5 administration. GE-B5 stimulated PRL secretion; the effect was statistically significant at time 20. NMB preadministration completely abolished PRL response. Our experiment indicates that GE-B5 stimulates PRL secretion through opioid receptors located outside the BBB. Since opioid peptides do not exert their effect on PRL secretion directly, but via a reduced dopaminergic tone, our data suggest that GE-B5 can modify brain neurotransmitter release without crossing the BBB."

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