Table 3.
In vitro inhibition, by antibiotics, of human drug metabolizing enzymes and transporters responsible for XueBiJing compounds' elimination.
| Antibiotics (ID) | IC50 values (μmol/L) |
||||
|---|---|---|---|---|---|
| UGT2B15 [X5→X6] | ALDH [PCD→X11] | OAT1 [X8] | OAT2 [X8] | OATP1B3 [X10] | |
| Imipenem (A1) | – | 120±30 | – | – | – |
| Meropenem (A2) | – | 164±39 | – | – | – |
| Ceftriaxone (A6) | – | – | – | – | 201±48 |
| Ceftazidime (A7) | – | 1034±155 | – | – | – |
| Cefoperazone (A8) | 971±130 | – | 49±11 | – | 27±9 |
| Cefotaxime (A9) | – | – | – | – | 68±20 |
| Cefamandole (A11) | – | – | 271±74 | – | 53±20 |
| Piperacillin (A13) | 797±142 | – | 591±154 | 1208±434 | – |
| Ticarcillin (A14) | – | – | 1833±572 | – | – |
| Penicillin G (A15) | 890±128 | 308±68 | 999±363 | – | 56±21 |
| Ampicillin (A16) | – | 2076±283 | – | – | 42±18 |
| Oxacillin (A17) | – | 465±72 | 99±31 | 467±97 | 11±2 |
| Carbenicillin (A18) | – | – | 311±90 | – | – |
| Flucloxacillin (A19) | 336±83 | 45±6 | 173±27 | 729±131 | 26±9 |
| Cefoxitin (A20) | 57±11 | 983±117 | – | – | 26±19 |
| Teicoplanin (A26) | – | – | – | 64±14 | 8±2 |
| Levofloxacin (A31) | – | – | – | 50±9 | – |
| Ciprofloxacin (A32) | – | – | 8±3 | 28±3 | 22±12 |
| Moxifloxacin (A33) | – | – | – | – | 17±2 |
| Erythromycin (A34) | – | – | – | – | 3±1 |
| Clindamycin (A35) | – | – | – | – | 12±2 |
| Trimethoprim (A37) | – | – | – | 667±146 | 378±109 |
| Rifamcin (A39) | – | – | – | – | 2±0 |
| Micafungin (A40) | 3±0 | – | 43±4 | 26±2 | 3±1 |
| Caspofungin (A41) | 39±2 | – | 7±2 | – | 1±0 |
| Amphotericin B (A42) | – | 87±9 | – | – | 1±0 |
| Itraconazole (A44) | – | – | – | – | 4±1 |
| Voriconazole (A45) | 55±6 | – | 189±75 | – | 19±8 |
X5, PCD, X8 and X10 were used as substrates for UGT2B15, ALDH, OAT1/2 and OATP1B3, respectively. X5, senkyunolide I; X6, senkyunolide I-7-O-β-glucuronide; X8, tanshinol; X10, salvianolic acid B; X11, protocatechuic acid; PCD, protocatechuic aldehyde. Data are expressed as the mean ± SD (n = 3).