Contribution of CNT1 and ENT1 to ribavirin uptake in human hepatocytes
- Authors
- 최민구; 김민혜; 맹한주; 송임숙
- Issue Date
- May-2015
- Publisher
- 대한약학회
- Keywords
- Ribavirin; Human hepatocytes; CNT1; ENT1; mRNA expression; Relative contribution
- Citation
- Archives of Pharmacal Research, v.38, no.5, pp.904 - 913
- Journal Title
- Archives of Pharmacal Research
- Volume
- 38
- Number
- 5
- Start Page
- 904
- End Page
- 913
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/11591
- DOI
- 10.1007/s12272-014-0437-y
- ISSN
- 0253-6269
- Abstract
- The objective of this study was to investigate thecontributions of a sodium-dependent concentrative nucleosidetransporter (CNT) 1 and an equilibrative nucleosidetransporter (ENT) 1 to ribavirin uptake in human hepatocytes. The initial studies in oocytes expressing CNT1 andENT1 showed increases in ribavirin uptake, indicating thatribavirin was a substrate for both CNT1 and ENT1. TheCNT1- and ENT1-mediated ribavirin uptake showed concentrationdependency with the following kinetics parameters:Km 26.3 lM and Vmax 426.2 fmol/min/oocyte forCNT1; Km 70.5 lM and Vmax 134.3 fmol/min/oocyte forENT1. Ribavirin uptake clearance in six human hepatocytesranged from 21.3 to 300.7 lL/min. Estimation of the contributionsof CNT1 and ENT1 to the hepatic uptake ofribavirin by using a relative activity factor method indicatedthat the relative contribution of ENT1 to the ribavirin uptakewas 82.8 ± 3.9 %. Real-time polymerase chain reactionanalysis of CNT1 and ENT1 expressions in the hepatocytesshowed that ENT1 mRNA expression was closely correlatedwith ribavirin uptake (R = 0.95, P = 0.003) while CNT1was not. The findings indicated that ENT1 was the majortransporter controlling the hepatic uptake of ribavirin.
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