Characteristics of the uptake of cysteine-containing leukotrienes by isolated hepatocytes.
Leukotrienes were transported into rat hepatocytes by a temperature- and energy-dependent mechanism. The uptake was saturable with high- and low-affinity sites (Km values approx. 1 and 17 microM). Competition and kinetic experiments indicated that leukotrienes C4, D4 and E4 were transported by a common mechanism. The maximal velocity of transport was about 50% higher for leukotrienes D4 and E4 than for leukotriene C4. Leukotriene B4, glutathione disulfide, and the glutathione-S-conjugate of acetaminophen did not interfere with the transport of leukotriene C into hepatocytes. This suggests that the process is specific for cysteine-containing leukotrienes. It is likely that the transport mechanism described here participates in biliary excretion of leukotrienes. This route was previously found to be a major one for elimination of leukotriene C3 in mice and guinea-pigs.
D000082:Acetaminophen / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D001692:Biological Transport / Q000187:drug effects; D003545:Cysteine; D005978:Glutathione / Q000494:pharmacology; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007700:Kinetics; D007975:Leukotriene B4 / Q000378:metabolism*; D017999:Leukotriene E4; D008099:Liver / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013189:SRS-A / Q000031:analogs & derivatives* / Q000378:metabolism*; D013696:Temperature; D014316:Tritium
D013189:SRS-A; D014316:Tritium; D007975:Leukotriene B4; D000082:Acetaminophen; D017999:Leukotriene E4; D005978:Glutathione; D003545:Cysteine; C034780:3-(glutathion-S-yl)acetaminophen