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Volume 3, Issue 2
  • ISSN: 2665-9786
  • E-ISSN: 2665-9794

Abstract

Recent studies suggest that dipeptide-like tyrosine/phenylalanine-conjugated phenolic amide compounds may contain several biological activities, including anti-inflammatory activity. However, there is currently no information about their transport and biotransformation in monocytes/macrophages involved in inflammation process.

The objective of this study was to investigate cell transport and biotransformation of the phenolic amides and esters in monocyte/macrophage-like cells.

Cell transport and biotransformation of the phenolic amides and esters (-coumaroylphenylalanine, -caffeoylphenylalanine, -feruloylphenylalanine, -coumaroyltyrosine, -caffeoyltyrosine, -feruloyltyrosine, and their -methyl esters) were investigated in THP-1 cells and PBMCs using HPLC, cellular, and kinetics methods.

In THP-1 cells, the phenolic amides were not transported significantly, but their -methyl esters were transported significantly ( < 0.02). Also, the transport of the esters was found to be sodium-independent and pH-dependent. Among the tested esters, -feruloylphenylalanine--methyl ester showed the highest uptake (K of 25 µM), and the uptake was inhibited by PepT1/2 substrate and blocker (GlySar and enalapril) in THP-1 cells. Particularly, enalapril competitively inhibited the uptake with K of 560 µM. The data also showed that -feruloylphenylalanine--methyl ester and -feruloyltyrosine--methyl ester could be biotransformed into parent phenolic amides in THP-1 cells. Similarly, these ester compounds were also found to be transported and biotransformed in PBMCs.

The data suggest that dipeptide-like tyrosine/phenylalanine-conjugated phenolic amide esters may be transported and biotransformed in THP-1 cells and PBMCs.

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2022-05-01
2025-01-10

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Efficient Transport and Biotransformation of Dipeptide-like Tyrosine/Phenylalanine-Conjugated Phenolic Amide Esters in THP-1 Cells and PBMCs: A Potential Means for Transporting Compounds Inside Monocytes/Macrophages
Current Nutraceuticals 3, e241221199425 (2022); https://doi.org/10.2174/2665978603666211224121836
/content/journals/cnt/10.2174/2665978603666211224121836
/content/journals/cnt/10.2174/2665978603666211224121836
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  • Article Type:     Research Article
Keyword(s): bioactives, nutraceuticals; biotransformation; Dipeptide-like tyrosine, phenylalanine-conjugated phenolic amide esters; PBMCs; PepT2; THP-1 cells; transport

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