Abstract

A large number of nutrients and bioactive ingredients found in milk play an important role in the nourishment of breast-fed infants and dairy consumers. Some of these ingredients include physiologically relevant compounds such as vitamins, peptides, neuroactive compounds and hormones. Conversely, milk may contain substances—drugs, pesticides, carcinogens, environmental pollutants—which have undesirable effects on health. The transfer of these compounds into milk is unavoidably linked to the function of transport proteins. Expression of transporters belonging to the ATP-binding cassette (ABC-) and Solute Carrier (SLC-) superfamilies varies with the lactation stages of the mammary gland. In particular, Organic Anion Transporting Polypeptides 1A2 (OATP1A2) and 2B1 (OATP2B1), Organic Cation Transporter 1 (OCT1), Novel Organic Cation Transporter 1 (OCTN1), Concentrative Nucleoside Transporters 1, 2 and 3 (CNT1, CNT2 and CNT3), Peptide Transporter 2 (PEPT2), Sodium-dependent Vitamin C Transporter 2 (SVCT2), Multidrug Resistance-associated Protein 5 (ABCC5) and Breast Cancer Resistance Protein (ABCG2) are highly induced during lactation. This review will focus on these transporters overexpressed during lactation and their role in the transfer of products into the milk, including both beneficial and harmful compounds. Furthermore, additional factors, such as regulation, polymorphisms or drug-drug interactions will be described.

Highlights

  • Milk is a complete food, one of the main sources of nutrients and bioactive ingredients in mammals and it plays an important role in health

  • Complex mechanisms are involved in the regulation of the physiological function and development of the mammary gland as well as in the uptake, reuptake and efflux of a large group of compounds including drugs in this organ

  • The influence of ABCG2 in the composition and quality of milk has been studied in depth during the last decades

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Summary

Introduction

Milk is a complete food, one of the main sources of nutrients and bioactive ingredients in mammals and it plays an important role in health. This review will focus on SLC and ABC transporters with increased expression in the mammary gland during lactation and their role in the transfer of compounds into milk, including ingredients with high nutritional interest such as vitamins, peptides, neuroactive compounds or steroids, as well as potentially harmful products such as drugs or contaminants. Additional factors, such as regulation, polymorphisms or drug-drug interactions will be described

Influx Transporters
Efflux Transporters
OATP1A2 and OATP2B1 Polymorphisms
OCT1 and OCTN1 Polymorphisms
PEPT2 Polymorphisms
ABCG2 Polymorphisms
Conclusions

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