Transport Mechanism of Anthracycline Derivatives in Rat Polymorphonuclear Leukocytes : Uptake of Pirarubicin, Daunorubicin and Doxorubicin

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We performed experiments on the cis-inhibition and trans-stimulation effect on pirarubicin uptake in order to clarify the involvement of a carrier in the pirarubicin, daunorubicin and/or doxorubicin transport systems in rat polymorphonuclear leukocytes. The uptake of daunorubicin and doxorubicin was a saturable concentration-dependent process. Since the apparent kinetic constants, Michaelis constant (K_m) and inhibition constant (K_i), were almost comparable, these drugs presented mutually competitive inhibition. Furthermore, the pirarubicin uptake by polymorphonuclear leukocytes was significantly elevated by increasing the preloaded amount of doxorubicin, indicating that there was a trans-stimulation effect on the pirarubicin transport in the leukocytes. These results suggest that carrier-mediated transport might be involved in the uptake of anthracycline derivatives, pirarubicin, daunorubicin and doxorubicin, by rat polymorphonuclear leukocytes.
公益社団法人日本薬学会の論文
1994-09-15