Table 2. IC50 and Ki values of MH against human CYP isoforms compared with that of specific inhibitors reported in literature.
CYP | Activity | IC50 (µM) | Ki (µM) | ||
MH | Specific inhibitor/reported valuesa | MH | Specific inhibitor/reported valuesa | ||
CYP1A2 | Phenacetin O-deethylation | 4.47(3.10,6.23)b | FUR/1.4 [27] | 4.56 | FUR/3 [28] |
CYP2A6 | coumarin 7-hydroxylation | >100 | TRA/0.42±0.07 [29] | - | TRA/0.17 [29] |
CYP2C9 | tolbutamide 4-hydroxylation | >100 | SUL/0.3–1.5 [27], [30] | - | SUL/0.3 [28] |
CYP2D6 | metoprolol α-hydroxylation | >100 | QUI/0.02–0.68 [27], [30] | - | SUL/0.027–0.4 [28], [31], [32] |
CYP2E1 | chlorzoxazone 6-hydroxylation | >100 | DIE/21.30 [27] | - | CHL/12 [33] |
CYP2C19 | S-Mephenytoin 4-hydroxylation | 10.91(8.84,13.45)b | TCL/0.52–1.6 [30] | 42.65 | TCL/1.2±0.5 [28] |
CYP3A4 | midazolam 1-hydroxylation | >100 | KET/0.08–0.24 [28] | – | KET/0.015 [28] |
IC50 and Ki values of specific inhibitors were referred to the reported literatures. b represents 95% confidence interval. “–”represents the data that is not calculated. FUR, furafylline; TRA, trans-2-phenylcyclopropylamine hydrochloride; SUL, sulfaphenazole; QUI, quinidine; CHL, chlormethiazole hydrochloride; TIC, ticlopidine hydrochloride; KET, ketoconazole; DIE: diethyldithiocarbamate.