Enzyme Source | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
DSM (Isoschizandrin) | NIFOX-NIF | TST6β-HTS | MDZ1′-OH-MDZ | |||||||||||
Vmax | Km | CLint | Vmax | Km | CLint | Vmax | S50 | n | CLmaxa | Vmax | Ks | Ksi | CLint | |
HLM | 623 ± 9.9 | 1.6 ± 0.1 | 389 | 4461 ± 59 | 15.3 ± 1.0 | 297 | 5484 ± 90 | 53.1 ± 5.1 | 1.4 ± 0.1 | 56.8 | 119 ± 4.6 | 3.5 ± 0.4 | 228 ± 43 | 33.7 |
RLM | 168 ± 2.4 | 1.4 ± 0.3 | 120 | 1360 ± 16 | 20.3 ± 0.8 | 67.0 | 2563 ± 78 | 61.2 ± 4.0 | 1.2 ± 0.1 | 26.7 | 96.9 ± 3.8 | 6.1 ± 1.7 | 206 ± 41 | 16.1 |
CYP3A4 | 36.7 ± 0.3 | 3.2 ± 0.1 | 11.5 | 35.7 ± 0.7 | 10.2 ± 0.7 | 3.50 | 101 ± 1.1 | 35.1 ± 3.2 | 1.2 ± 0.1 | 1.80 | 5.9 ± 0.2 | 1.3 ± 0.2 | 114 ± 17 | 4.50 |
CYP3A5 | 16.1 ± 2.4 | 4.1 ± 0.1 | 3.90 | 18.4 ± 0.3 | 15.8 ± 0.8 | 1.20 | 44.7 ± 1.3 | 89.5 ± 5.2 | 1.3 ± 0.1 | 0.29 | 34.2 ± 2.5 | 4.1 ± 0.8 | 173 ± 52 | 8.30 |
6β-HTS, 6β-hydroxytestosterone; OX-NIF, oxidized nifedipine
↵a TST clearance was obtained by Vmax/Km corrected with Hill coefficient (Houston and Kenworthy, 2000).