Concentrations of metabolites in phase I (cofactor: NADPH) and dual-activity assays (cofactors: NADPH and UDPGA) after incubation of 10 μM licofelone for 30 min Concentration data were converted into biotransformation rates (percentage of initial licofelone concentration; mean ± S.D., n = 3).
Biotransformation | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Metabolite | Cofactors | HLM | CLM | DLM | NZLM | RLM | MLM | |||||
| % | % | % | % | % | % | |||||||
| M1 | NADPH | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | |||||
| NADPH+UDPGA | 7.33 ± 1.14 | 28.3 ± 3.4 | 40.2 ± 3.6 | 25.9 ± 1.6 | 53.9 ± 6.2 | 21.9 ± 0.7 | ||||||
| M2 | NADPH | <a | 2.89 ± 0.16 | N.D. | 8.00 ± 0.46 | 1.11 ± 0.09 | < | |||||
| NADPH+UDPGA | 1.02 ± 0.18 | 0.59 ± 0.11 | N.D. | 4.01 ± 0.33 | 0.24 ± 0.04 | < | ||||||
| M3 | NADPH | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | |||||
| NADPH+UDPGA | 26.8 ± 2.1 | 4.44 ± 0.51 | N.D. | 3.48 ± 0.17 | N.D. | N.D. | ||||||
| M4 | NADPH | 2.05 ± 0.16 | 0.69 ± 0.17 | 2.23 ± 0.14 | 0.18 ± 0.03 | 2.24 ± 0.12 | 0.57 ± 0.03 | |||||
| NADPH+UDPGA | 0.47 ± 0.04 | 0.14 ± 0.02 | 0.15 ± 0.03 | < | 0.48 ± 0.06 | 0.12 ± 0.02 | ||||||
| M5 | NADPH | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | |||||
| NADPH+UDPGA | N.D. | N.D. | N.D. | N.D. | N.D. | N.D. | ||||||
| Total | NADPH | 2.05 ± 0.16 | 3.58 ± 0.18 | 2.23 ± 0.14 | 8.18 ± 0.43 | 3.35 ± 0.18 | 0.57 ± 0.03 | |||||
|
| NADPH+UDPGA | 35.6 ± 1.7 | 33.5 ± 3.9 | 40.4 ± 3.6 | 33.4 ± 2.0 | 54.6 ± 6.3 | 22.0 ± 0.7 | |||||
N.D., not detected
↵ a < = Concentration below limit of quantification