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Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3.

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Title: Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3.
Authors: Yamaguchi, Hiroaki Browse this author →KAKEN DB
Okada, Masahiro Browse this author
Akitaya, Shou Browse this author
Ohara, Hiroshi Browse this author
Mikkaichi, Tsuyoshi Browse this author
Ishikawa, Haruna Browse this author
Sato, Mayumi Browse this author
Matsuura, Masaki Browse this author
Saga, Toshihide Browse this author
Unno, Michiaki Browse this author
Abe, Takaaki Browse this author
Mano, Nariyasu Browse this author
Hishinuma, Takanori Browse this author
Goto, Junichi Browse this author
Keywords: nitrobenz-2-oxa-1,3-diazole
organic anion-transporting polypeptide 1B1
organic anion-transporting polypeptide 1B3
Issue Date: Jun-2006
Publisher: American Society for Biochemistry and Molecular Biology
Journal Title: Journal of lipid research
Volume: 47
Issue: 6
Start Page: 1196
End Page: 1202
Publisher DOI: 10.1194/jlr.M500532-JLR200
PMID: 16534140
Abstract: This study sought to clarify the contributions of organic anion-transporting polypeptide (OATP) 1B1 and 1B3 to the liver uptake of chenodeoxycholic acid (CDCA). We synthesized a fluorescent version of CDCA, chenodeoxychilyl-(Nepsilon-NBD)-lysine (CDCA-NBD), to characterize transporter-mediated uptake. CDCA-NBD is efficiently transported by OATP1B1 and OATP1B3 with high affinities. The Michaelis-Menten constants for CDCA-NBD uptake by OATP1B1 and OATP1B3 were 1.45 +/- 0.39 microM and 0.54 +/- 0.09 microM, respectively. By confocal laser scanning microscopy, CDCA-NBD, which is taken up by OATP1B1 and OATP1B3, was observed to localize to the cytosol. We also examined the transport of newly synthesized fluorescent bile acids. NBD-labeled bile acids, including cholic acid, deoxycholic acid, lithocholic acid, and ursodeoxycholic acid, were all transported by OATP1B1 and OATP1B3. CDCA-NBD exhibited the highest rate of transport of the five NBD-labeled bile acids examined in OATP1B1- and OATP1B3-expressing cells. Our results suggest that OATP1B1 and OATP1B3 play important roles in CDCA uptake into the liver. Fluorescent bile acids are useful tools to characterize the uptake properties of membrane transporters.
Type: article (author version)
Appears in Collections:薬学研究院 (Faculty of Pharmaceutical Sciences) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 山口 浩明

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