Table 1. The kinetic and inhibition profile of 8-methoxypsoralen on coumarin 7-hydroxylase activity of the wild type CYP2A6, CYP2A6*15, CYP2A6*16, CYP2A6*21 and CYP2A6*22.
CYP Protein | Km (µM) | IC50 (µM) | Fold |
CYP2A6*1 (wild-type) | 10.61±1.58 | 0.19±0.05 | 1 |
CYP2A6*15 | 22.13±1.29** | 2.39±0.0** | 12.58 |
CYP2A6*16 | 10.53±1.45 | 0.43±0.1 | 2.26 |
CYP2A6*21 | 16.39±0.41** | 1.56±0.21** | 8.21 |
CYP2A6*22 | 31.16±2.22** | 1.05±0.21** | 5.53 |
All values are shown as the means ± SD of three independent determinations. The Km values were determined in our previous study [9] and listed here for comparison purpose. The IC50 values were determined in the present studies. The last column represents the fold of change in IC50 relative to the wild type. Degree of statistical differences between the wild-type and the mutants as determined by one-way analysis of variance: the mean difference is significant at 0.05 level (* p<0.05) and highly significant at 0.01 level (** p<0.01).