Abstract:
:The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs. Although the expression and function of this solute carrier transporter is well characterized in the human liver and other tissues, little is known about its localization and functional relevance in the intestine. Thus, it was the aim of this study to investigate its localization and function in the human jejunum and in the frequently used intestinal Caco-2 cell line. The basolateral membrane of jejunal tissue from 6 individuals showed a significant enrichment of OATP2B1 (17-fold) and the known basolateral proteins ABCC3 and Na/K-ATPase compared to the apical membrane as derived from targeted proteomics analysis. On the contrary, apical localization could be confirmed for ABCB1, ABCC2, and PEPT1. Basolateral localization of OATP2B1 could also be verified in Caco-2 cells. Bidirectional transport studies with established OATP2B1 substrates (sulfasalazine and pravastatin) across freshly exercised human jejunum and Caco-2 cell monolayers demonstrated a markedly higher transport from the basal to the apical compartment than in the opposite direction. Our data provide evidence for a basolateral localization of OATP2B1 which may improve our understanding of intestinal drug absorption.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Keiser M,Kaltheuner L,Wildberg C,Müller J,Grube M,Partecke LI,Heidecke CD,Oswald Sdoi
10.1016/j.xphs.2017.04.001subject
Has Abstractpub_date
2017-09-01 00:00:00pages
2657-2663issue
9eissn
0022-3549issn
1520-6017pii
S0022-3549(17)30230-7journal_volume
106pub_type
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