Table 1. Effect of BI01383298 on the uptake function of different transporters in HepG2 cells monitored with appropriate substrates and experimental conditions.
Substrate | Control | BI01383298 | % Control |
---|---|---|---|
Citrate (7 µM) | 483 ± 13 | 88.2 ± 5.6 | 18 ± 1** |
Nicotinate (8 µM) | 124 ± 3 | 123 ± 4 | 100 ± 3 |
Arginine (5 µM) | 928 ± 31 | 935 ± 51 | 101 ± 5 |
Glutamine (5 µM) | 319 ± 25 | 306 ± 3 | 92 ± 1 |
Tryptophan (5 µM) | 80 ± 2 | 76 ± 3 | 95 ± 3 |
Lactate (3 µM) | 141 ± 14 | 137 ± 7 | 97 ± 5 |
HepG2 cells were preincubated in NaCl buffer with or without 10 μM BI01383298 for 30 min. After washing the cells, uptakes of [14C]-citrate, [14C]-nicotinate, [3H]-arginine, [3H]-glutamine, [3H]-tryptophan, and [14C]-lactate were measured for a given time (which varied for different transporters) in NaCl buffer pH 7.5 (citrate, nicotinate, arginine), NMDG buffer pH 7.5 (glutamine, tryptophan) or NMDG pH 6 (lactate). The units for the uptake activity were pmol/mg of protein/30 min for citrate, pmol/mg of protein/15 min for nicotinate, arginine, glutamine, and tryptophan, and pmol/mg of protein/3 min for lactate. Data represent means ± S.D. ** P < 0.01 compared with the corresponding control uptake.