Novel peptides derived from alpha(s1)-casein with opioid activity and mucin stimulatory effect on HT29-MTX cells

作者：Fernandez Tome S; Martinez Maqueda D; Giron R; Goicoechea C; Miralles B; Recio I^*

来源：Journal of Functional Foods, 2016, 25: 466-476.

DOI：10.1016/j.jff.2016.06.023

• Opioid peptide
• mu-Opioid receptor
• Molecular dynamics
• Mucin
• Goblet cells

The opioid effect of alpha(s1)-casein fragments related to (143)AYFYPEL(149) and (YFYPEL149)-Y-144, which had previously shown mucin-stimulatory activity in human goblet cells, was investigated. Peptides (YFYPEL149)-Y-144 and (YFYPE148)-Y-144 showed opioid agonistic activity in guinea pig ileum, and in mouse vas deferens but to a lower extent. Peptides were partly hydrolysed during the assay and several of the resulting fragments lost the N-terminal Tyr residue. Docking of peptides (YFYPEL149)-Y-144 (active) and (YFYP147)-Y-144 (inactive) into the active site of the opioid receptor model showed remarkable differences regarding the flexibility at the third intracellular loop of the receptor and the interaction with Pro at the peptide C-terminus that forced residues Arg(148) and Glu(166) from the receptor to move towards the interior of the binding pocket. The study on human cells HT29-MTX has shown that (YFYPEL149)-Y-144 is the minimum fragment able to stimulate MUC5AC expression.

• 出版日期2016-8