Table 1 Inhibitory effects of plumbagin on six CYP isoforms in HLMs and RLMs.
CYP isoform | IC50 (μM) | Ki (μM) | αKi (μM) | α | Type | |
|---|---|---|---|---|---|---|
Humans | 1A2 | 7.49 | 0.15 | 0.16 | 0.94 | non-competitive |
2B6 | 13.10 | 1.62 | 2.92 | 0.55 | mixed-type | |
2C9 | 10.94 | 2.16 | 1.46 | 1.48 | mixed-type | |
2D6 | 10.21 | 1.46 | 2.22 | 0.66 | mixed-type | |
2E1 | 6.54 | 0.65 | 2.64 | 0.25 | mixed-type | |
3A4 | 6.45 | 0.88 | 0.57 | 1.54 | mixed-type | |
Rats | 1A2 | 2.65 | 2.64 | 8.51 | 0.31 | mixed-type |
2B1 | 5.86 | 9.93 | ‒ | ‒ | competitive | |
2C11 | 3.85 | 7.85 | ‒ | ‒ | competitive | |
2D1 | 6.17 | 9.49 | 13.79 | 0.69 | mixed-type | |
2E1 | 3.72 | 6.28 | ‒ | ‒ | competitive | |
3A2 | 8.47 | ‒ | ‒ | ‒ | atypical kinetics |
