Functional Expression of Organic Cation/carnitine Transporter 2 (OCTN2/SLC22A5) in Human Brain Capillary Endothelial Cell Line hCMEC/D3, a Human Blood-brain Barrier Model
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- OKURA Takashi
- Laboratory of Drug Disposition & Pharmacokinetics, Faculty of Pharma-Sciences, Teikyo University
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- KATO Sayaka
- Laboratory of Drug Disposition & Pharmacokinetics, Faculty of Pharma-Sciences, Teikyo University
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- DEGUCHI Yoshiharu
- Laboratory of Drug Disposition & Pharmacokinetics, Faculty of Pharma-Sciences, Teikyo University
書誌事項
- タイトル別名
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- Functional Expression of Organic Cation/carnitine Transporter 2 (OCTN2/<i>SLC22A5)</i> in Human Brain Capillary Endothelial Cell Line hCMEC/D3, a Human Blood-brain Barrier Model
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抄録
The aim of this study was to examine whether organic cation/carnitine transporter 2 (OCTN2/SLC22A5) plays a role in the human blood-brain barrier (BBB) by evaluating its functional activity in human brain endothelial cells (hCMEC/D3), which are considered to be a model of the BBB. The uptake of [3H]L-carnitine by hCMEC/D3 cells was time-, extracellular sodium- and concentration-dependent, with a Km value of 15.7 µM. These results are consistent with the properties of OCTN2-mediated L-carnitine transport. hCMEC/D3 cells showed relatively high expression of OCTN2 mRNA, and this expression was effectively decreased at 24–72 h after lipofection of cells with OCTN2 siRNA under optimized conditions. [3H]L-Carnitine uptake was dramatically suppressed by silencing of the OCTN2 gene. The inhibitory effect of OCTN2 gene silencing was similar to that of an excess amount of unlabeled L-carnitine. These results indicate that OCTN2 is involved in L-carnitine transport at the human BBB.<br>
収録刊行物
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- Ｄｒｕｇ Ｍｅｔａｂｏｌｉｓｍ ａｎｄ Ｐｈａｒｍａｃｏｋｉｎｅｔｉｃｓ
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Ｄｒｕｇ Ｍｅｔａｂｏｌｉｓｍ ａｎｄ Ｐｈａｒｍａｃｏｋｉｎｅｔｉｃｓ 29 (1), 69-74, 2014
日本薬物動態学会