Table 3.
Inhibition parameters of isobavachin against several CYP and UGT isozymes (Mean ± SD). All experiments were performed in triplicate
Isozymes | Substrate | IC50 (μM) | Inhibition type | Ki (μM) | α | R 2 | AIC | SC | Selection |
---|---|---|---|---|---|---|---|---|---|
| |||||||||
CYP2B6 | Bupropion | 5.00 ± 0.48 | Competitive | 0.35 ± 0.11 | – | 0.9111 | 14.65 | 17.64 | |
Non-competitive | 1.93 ± 0.18 | – | 0.9671 | −5.19 | −2.21 | √ | |||
Mixed-type | 1.46 ± 0.62 | 1.49 ± 0.92 | 0.9678 | −3.64 | 0.34 | ||||
CYP2C9 | Tolbutamide | 0.04 ± 0.005 | Competitive | 0.11 ± 0.02 | – | 0.9623 | −136.47 | −133.48 | |
Non-competitive | 0.22 ± 0.02 | – | 0.9793 | −148.48 | −145.49 | √ | |||
Mixed-type | 0.27 ± 0.10 | 0.70 ± 0.49 | 0.9797 | −146.85 | −142.87 | ||||
CYP2C19 | Mephenytoin | 0.27 ± 0.07 | Competitive | 1.55 ± 0.25 | – | 0.9724 | −113.19 | −110.20 | √ |
Non-competitive | 3.34 ± 0.49 | – | 0.9625 | −107.08 | −104.10 | ||||
Mixed-type | 1.55 ± 0.53 | >>1 | 0.9724 | −111.19 | −107.21 | ||||
UGT1A1 | Estradiol | 1.53 ± 0.39 | Competitive | 3.05 ± 0.41 | – | 0.9857 | 225.43 | 228.42 | √ |
Non-competitive | 3.32 ± 0.38 | – | 0.9854 | 225.80 | 228.79 | ||||
Mixed-type | 3.10 ± 1.23 | 8.01 ± 2.56 | 0.9856 | 227.49 | 231.47 | ||||
UGT1A9 | propofol | 1.21 ± 0.30 | Competitive | 0.20 ± 0.03 | – | 0.9676 | 121.43 | 124.42 | |
Non-competitive | 0.44 ± 0.04 | – | 0.9807 | 111.03 | 114.02 | √ | |||
Mixed-type | 0.43 ± 0.14 | 1.05 ± 0.70 | 0.9807 | 113.02 | 117.01 | ||||
UGT2B7 | zidovudine | 0.09 ± 0.01 | Competitive | 0.02 ± 0.00 | – | 0.9511 | 232.70 | 235.68 | |
Non-competitive | 0.05 ± 0.01 | – | 0.9766 | 217.93 | 220.91 | √ | |||
Mixed-type | 0.04 ± 0.01 | 1.80 ± 0.93 | 0.9781 | 218.55 | 222.54 |