Lack of Zonal Uptake of Estrone Sulfate in Enriched Periportal and Perivenous Isolated Rat Hepatocytes
作者： K. Sandy Pang , Eugene Tan , Rommel G. Tirona
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摘要: The zonal uptake of estrone sulfate (E1S; 1 to 400 μM) was investigated in periportal and perivenous rat hepatocytes cells isolated from whole liver (regular hepatocytes). Transport E1S by periportal, perivenous, regular described saturable ( K ms 24 26 μM V maxs 1.8 nmol/min/mg protein) nonsaturable components (2.5 3.2 μl/min/mg that were not different among the regions p > .05, ANOVA). These kinetic constants represented pooled values for entire complement transporters E1S, including two known E1S: Ntcp, Na+-taurocholate cotransporting polypeptide, oatp1, organic anion transporting polypeptide cloned liver. Uptake significantly reduced estradiol 17β-glucuronide (50 bumetanide (200 μM), inhibited strongly competitively pregnenolone with an inhibition constant 6.7 μM. Further segregation as sodium-dependent -independent systems achieved through simultaneous fitting data obtained presence absence sodium parallel hepatocytic studies. For hepatocytes, systems: a transport system, characterized similar (1.1 1.4 (49 55 sodium-independent system comparable (0.70 0.84 (16 22 linear clearance 1.7 2.7 protein (ANOVA, .05) obtained. suggest hepatic involved transporter systems. No heterogeneity observed.
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