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opioid receptor ligands

Opioid Peptides Derived from Food Proteins: The Exorphins

Abstract

"Peptides with opioid activity are found in pepsin hydrolysates of wheat gluten and alpha-casein. The opioid activity of these peptides was demonstrated by use of the following bioassays: 1) naloxone-reversible inhibition of adenylate cyclase in homogenates of neuroblastoma X-glioma hybrid cells; 2) naloxone-reversible inhibition of electrically stimulated contractions of the mouse vas deferens; 3) displacement of [3H]dihydromorphine and [3H-Tyr, dAla2]met-enkephalin amide from rat brain membranes. Substances which stimulate adenylate cyclase and increase the contractions of the mouse vas deferens but do not bind to opiate receptors are also isolated from gluten hydrolysates. It is suggested that peptides derived from some food proteins may be of physiological importance."

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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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