Abstract

This study aimed to understand the role of the mucus layer (a biological hydrogel) in the transport mechanisms of peptides. Using established in vitro models, the mucin-binding activity and mucus-permeating property of peptides were determined. Uncharged peptides with relatively high hydrophilicity, including MANT, TNGQ, and PASL, as well as cationic peptides, including KIPAVF and KMPV, possessed strong mucin-binding activity. Contrarily, uncharged peptides with high hydrophobicity index, including YMSV and QIGLF, exhibited weak mucin-binding activity. Only TNGQ, which has high Boman index and hydrophilicity, showed a high biosimilar mucus-permeating property with a permeability of 96 ± 30% after 60 min. TNGQ showed the potential for high bioavailability due to the high mucin-binding and biosimilar mucus-permeating activities.

Highlights

  • Bioactive peptides, usually consisting of 2–20 amino acid residues, are commonly released from the parent proteins by enzymatic hydrolysis or microbial fermentation [1].In vitro and in vivo studies have demonstrated that bioactive peptides exert health-promoting properties, including antihypertensive, antioxidant, anti-inflammatory, immunomodulatory, antidiabetic, and anticancer activities [1,2]

  • The Caco-2 cell line lacks the mucus layer that is located on the surface of the epithelial membrane and functions as a protective barrier [6]

  • TNGQ was more than 100%, possibly due to the impurity of BSA in the biosimilar mucus rather than targetedremoved peptides by the OPA as method

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Summary

Introduction

Usually consisting of 2–20 amino acid residues, are commonly released from the parent proteins by enzymatic hydrolysis or microbial fermentation [1]. Still not known viatight tight junctions, transcytosis, andtranscellular passive transcellular It ishow stillpeptides not known ho interact with mucin penetrate the mucusthe layers before transporting across the underlying tides interact withand mucin and penetrate mucus layers before transporting across the und epithelium. Mucins are the major functiona the transport of bioactive peptides [11] To date, it is still not well understood how peptides interact mucin the mucus layers before transporting across ponents of with mucus thatand arepenetrate responsible for the viscoelastic properties of the the mucus underlying epithelium, as illustrated in Figure [5]. Boman index indicated the binding potential co-culture monolayers) has been used as a more physiologically relevant model to ate the transport of bioactive peptides [11] To date, it is still not well understood peptides interact with mucin and penetrate the mucus layers before transporting the underlying epithelium, as illustrated in Figure 1 [5].

Physicochemical Properties of Peptides
Determination of Mucin-Binding Activity of Peptides
Quantification
Statistical Analysis
Results andanalysis
Mucus-Permeating Property of Peptides
Biosimilar
Conclusions
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