Hsu L S
Br J Pharmacol. 1982 Nov;77(3):413-7. doi: 10.1111/j.1476-5381.1982.tb09313.x.
1 Slices of rat liver weighing 15-30 mg were incubated at 37 degrees C in 5-fluorourecil (5-FU) solution. 2 The 5-FU taken up was measured by high pressure liquid chromatography. 3 Uptake of 5-FU was found to approximate to Michaelis-Menton kinetics with the values of Kt and Vmax equal to 15.39 mmol 1-1 and 1.96 mumol g-1 min-1 respectively. 4 Transport of 5-FU was saturable with the uptake being much greater in the non-fasting rats. 5 Intracellular concentration of 5-FU after 24 min incubation approached but did not significantly exceed that in the extracellular fluid. 6 Enzymatic destruction of 5-FU at 2 min was negligible but substantial after a long incubation period. 7 2,4-Dinitrophenol was found to inhibit transport of 5-FU significantly. 8 Results suggested that the mechanism of uptake of 5-FU by rat liver is an energy requiring process.
将重量为15 - 30毫克的大鼠肝脏切片在37摄氏度下于5 - 氟尿嘧啶(5 - FU)溶液中孵育。
通过高压液相色谱法测定摄取的5 - FU。
发现5 - FU的摄取近似于米氏动力学,Kt和Vmax值分别等于15.39 mmol 1-1和1.96 mumol g-1 min-1。
5 - FU的转运是可饱和的,非禁食大鼠的摄取量要大得多。
孵育24分钟后,5 - FU的细胞内浓度接近但未显著超过细胞外液中的浓度。
5 - FU在2分钟时的酶促破坏可忽略不计,但在长时间孵育后则很显著。
发现2,4 - 二硝基苯酚可显著抑制5 - FU的转运。
结果表明,大鼠肝脏摄取5 - FU的机制是一个需要能量的过程。